Galal Elgemeie

• PhD, DSc
• Professor at Helwan University

Benzothiazole derivatives have garnered considerable attention owing to their versatile chemical scaffold and remarkable biological activities. The article provides an in-depth analysis of the diverse structural modifications and strategies employed to enhance the anticancer potential of these compounds from the period of 2020 to 2024. It discusses...

In the structure of the title compound, C19H13ClN4OS, the four atoms of the pyridinic ring that are not fused with the thia­zole, including the sp³ C atom, lie significantly outside the benzo­thia­zole plane. A short intra­molecular S⋯O contact of 2.5992 (4) Å is observed. The amide NH2 group is planar, whereas the amine NH2 group is pyramidalized....

Novel N-arylacetamides 2a–f were synthesized based on benzo[d]thiazole scaffold. The compounds 2a–c underwent Knoevenagel condensation through green synthetic method with different aromatic aldehydes and pyrazole-7-carbaldehydes delivered the respective arylidenes with efficient yields. Arylidenes 4 reacted with malononitrile affording the correspo...

The compounds 2′,3′,4′,6′-tetra-O-acetyl-β-d-gluco­pyranosyl N′-cyano-N-phenyl­carbamimido­thio­ate (C22H25N3O9S, 5a), 2′,3′,4′,6′-tetra-O-acetyl-β-d-galacto­pyranosyl N′-cyano-N-phenyl­carbamimido­thio­ate, (C22H25N3O9S, 5b), 2′,3′,4′,6′-tetra-O-acetyl-β-d-galacto­pyranosyl N′-cyano-N-methyl­carbamimido­thio­ate (C17H23N3O9S, 5c), and 2′,3′,4′,6′-...

The structure of the title compound, C23H21BrN4O, contains two independent mol­ecules connected by hydrogen bonds of the type Namide—H⋯N≡C to form a dimer. The configuration at the exocyclic C=C double bond is E. The mol­ecules are roughly planar except for the isopropyl groups. There are minor differences in the orientations of these groups and th...

Cancer remains a global health concern, demanding the development of new therapeutic medicines. This research focuses on the synthesis, in vitro evaluation, and in silico analysis of new 2-substituted benzothiazole derivatives as possible anticancer drugs. Hybrid molecules comprising benzothiazole and pyridinone rings 10a-d and 14a-d were also synt...

Tuberculosis (TB) is a global pandemic killing millions of people every year. Yet, resistant strains make curing TB quite challenging. Herein, a series of new pyrazole-linked benzothiazole hybrids was synthesized and evaluated for their anti-TB activity against three Mycobacterium tuberculosis strains (drug sensitive (DS), multidrug-resistant (MDR)...

Novel approach for synthesizing triazine sulfonamide derivatives is accomplished via reacting the sulfaguanidine derivatives with N-cyanodithioiminocarbonate. Further reaction of the novel triazine sulfonamide analogues with various secondary amines and anilines generated various substituted triazine sulfonamide analogues of promising broad-spectru...

In the structure of the title compound, C22H22N4O4·C3H7NO·H2O, the entire tricyclic system is approximately planar except for the carbon atom bearing the two methyl groups; the meth­oxy­phenyl ring is approximately perpendicular to the tricycle. All seven potential hydrogen-bond donors take part in classical hydrogen bonds. The main mol­ecule and t...

N-Phenyl-2-(phenyl­sulfan­yl)acetamide, C14H13NOS, was synthesized and structurally characterized. In the crystal, N—H⋯O hydrogen bonding leads to the formation of chains of mol­ecules along the [100] direction. The chains are linked by C—H⋯π inter­actions, forming a three-dimensional network. The crystal studied was twinned by a twofold rotation a...

In the title compound, C12H11N3OS, the inter­planar angle between the pyrazole and benzo­thia­zole rings is 3.31 (7)°. In the three-dimensional mol­ecular packing, the carbonyl oxygen acts as acceptor to four C—H donors (with one H⋯O as short as 2.25 Å), while one methyl hydrogen is part of the three-centre system H⋯(S, O). A double layer structure...

Novel approach for synthesizing triazine sulfonamide derivatives is accomplished via reacting the sulfaguanidine derivatives with N-cyanodithioiminocarbonate. Further reaction of the novel triazine sulfonamide analogues were reacted with various secondary amines, anilines and 2-aminothiazole to generate various substituted triazine sulfonamide anal...

The title compound, C10H11N5O2S2, consists of an unexpected tautomer with a protonated nitro­gen atom in the triazine ring and a formal exocyclic double bond C=N to the sulfonamide moiety. The ring angles at the unsubstituted nitro­gen atoms are narrow, at 115.57 (12) and 115.19 (12)°, respectively, whereas the angle at the carbon atom between thes...

In the structure of the title compound, C19H19N3O5S·C4H8O2, the two independent dioxane mol­ecules each display inversion symmetry. The pyrazole ring is approximately parallel to the aromatic ring of the oxy-ethanone group and approximately perpendicular to the tolyl ring of the sulfonyl substituent. An extensive system of classical and ‘weak’ hydr...

A novel series of benzothiazolyl-pyridine hybrids 8a–h and 14a–e were produced from the reaction of enamine derivative 4 with each of the arylcyanoacetamides 5a–h and cyanoacetohydrazides 9a–e. The new products were characterized by spectral techniques (IR, ¹H NMR, ¹³C NMR, and MS). Biological evaluation of 8a–h and 14a–e in vitro against H5N1 and...

In the structure of the title compound, C17H14N4O2, the triazole ring exhibits inter­planar angles of 63.86 (2) and 76.96 (2)° with the phenyl and benzo­thia­zole planes, respectively. The C—C—C angle at the methyl­ene group is rather wide at 114.28 (4)°. The packing involves three borderline C—H⋯N contacts, two of which combine to form layers para...

In the structure of the title compound, C15H19N3O5S2, the bond lengths at the linking sulfur atom are significantly different [1.7473 (17) and 1.811 (2) Å], and the angle at the exocyclic nitro­gen atom is wide at 128.45 (18)°. The inter­planar angle between the tolyl and thia­diazole rings is 9.2 (1)°. The complex hydrogen-bonding pattern, involvi...

This study revealed the design and preparation of new 3-(benzo[d]thiazol-2-yl)-2H-chromen-2-one derivatives 9a-h. The structures of the synthesized products were elucidated by their spectroscopic data and X-ray crystallography for compounds 9a and 9d. The prepared new compounds were measured for their fluorescence, and a good result indicated that...

The mol­ecule of the title compound, C17H11NO2S, is almost planar, with an inter­planar angle of 3.01 (3)° between the benzo­thia­zole and chromene ring systems. A short intra­molecular S⋯O=C contact of 2.727 (2) Å is observed. The crystal packing involves a layer structure parallel to (211), containing dimeric inversion-symmetric units connected b...

The title compound, C23H15BrN2OS, was the unexpected product in an attempted synthesis of the isomeric 3-(benzo[d]thia­zol-2-yl)-6-bromo-1-p-tolyl­quinolin-2(1H)-one. The Cchromene=N—C angle is wide [125.28 (8)°]. The benzo­thia­zole and chromene ring systems are almost coplanar, with their planes parallel to (1 0); the toluene ring system is rotat...

In this study we made of reaction of 11H‐indeno[1,2‐b]quinoxalin‐11‐one with hydrazine hydrate and phenyl hydrazine to afford the corresponding hydrazineylidenes 3 a, b in good yield. A series of a novel Schiff's bases of isatin and aldehydes were synthesized by condensation of them with 11‐hydrazineylidene‐11H‐indeno[1,2‐b]quinoxaline. A number of...

The title compounds, C15H14N2OS (1a), C16H16N2OS (1b), and C17H18N2OS (1c), form a homologous series in which the size of the saturated ring increases from six- to eight-membered (with four, five and six methyl­ene groups respectively). For 1b and 1c, the central (CH2) n moieties are all displaced to the same side of their ring, and the CH2—CH2—CH2...

A series of new pyrimidine derivatives were synthesized, including sulfapyrimidines and pyrazolo[1,5-a]pyrimidines. In basic medium, pyrimidine compounds were produced by reacting sulfa guanidine with either 2-cyano-3-(dimethylamino)-N-acrylamides or N-(4-chlorophenyl)-2-cyano-3-(4-aryl)-acrylamides. The reaction of 5-amino-1H-pyrazole-4-carboxamid...

The drug-resistance problem is widely spread and becoming more common in community-acquired and nosocomial strains of bacteria. Therefore, finding new antimicrobial agents remains an important drug target. From this perspective, new derivatives of benzothiazole were synthesized and evaluated for their antimicrobial activity and ability to inhibit t...

An error in the interpretation of a reference in the paper by Hammad et al. [Acta Cryst. (2018), E74, 853–856] is corrected.

Background Medicinal chemistry of pyrazolopyrimidine scaffolds substituted with different heterocyclic nuclei has attracted great attention due to their wide range of biological activities that have been reported. Pyrazolopyrimidine scaffold is an important privileged heterocycle nucleus in drug discovery. Methods All pharmacological activities of...

Novel derivatives of benzothiazole-2-thiophene S-glycoside were synthesized and tested for their antiviral and anticancer potency and NS3/4A and USP7 enzyme inhibitions. The ring system was formed by first synthesizing new derivatives of 5-mercaptothiophene substituted with the benzothiazole moiety, followed by coupling with various halo sugar deri...

N-Sulfonylaziridines have received special attention in organic synthesis due to the superior electro N-withdrawing ability of the attached sulfonyl group as well as their ring stain. This ring system is reactive to various types of useful transformations. In this chapter, we will summarize new and interesting synthetic strategies for the cleavage...

The N-tosyl moiety is a robust constituent of numerous pharmaceutical molecules. It has drawn enormous attention to exploring the efficient hybridization of N-tosyl moiety with nitrogen-containing five-membered heterocyclic rings. In this chapter, we focus on N-sulfonated five-membered rings which include five important classes named N-sulfonated-p...

Six membered heterocycles containing nitrogen are valuable compounds, particularly in medicinal chemistry, however, their N-sulfonated derivatives, for example, analogs of diazines such as pyrazine, pyridazines, and pyrimidine 1,2,4-triazines and triazine analogs as 1,2,3-triazines, 1,2,4-triazines, 1,2,5-triazines, and 1,3,5-triazines have been id...

It is well known that N-sulfonyl azepine derivatives have some inhibitory activity. As a result, several methodologies for the synthesis of N-sulfonyl azepine derivatives have been developed. This chapter discusses the various synthetic strategies for N-sulfonyl azepine derivatives including dihydroazepines and tetrahydroazepines. In general, the s...

The medicinal application is undoubtfully one of the most aspects of any chemical scaffold. The different structural features of any chemical entity are what entails its biological activity. As such, the present chapter explores the structural aspects of various N-sulfonyl heterocycles such as N-sulfonyl aziridine, N-sulfonyl azetidine, N-sulfonyl...

N-sulfonyl triazole is an intermediate in organic synthesis and has been proven to be an excellent nitrogen source for the construction of many heterocycles. Due to its more favorable pharmacokinetic properties, tetrazole has also been proven to be a suitable bioisostere derived from a carboxylic acid and cisamide units. This chapter summarizes the...

N-Sulfonated benzoazoles rings serve as core structures in several important classes of bioactive natural and synthetic products. Among the N-sulfonated benzodiazoles introduced in this chapter, the N-sulfonated benzopyrazoles have been reported to display significant biological properties such as antiinflammatory, antiviral, and antitrypanosoma. A...

It demonstrates that the construction of aziridines has still attracted great attention for the reason of their promising use as intermediates in complex synthesis, in addition to the interesting biological potencies of many compounds containing aziridinyl ring-like natural products. Such a chapter particularly covers the published reports regardin...

A brief discussion concerned with the medicinal use and the reported synthetic routes for some selected N-sulfonyl benzoazines including N-sulfonyl-cinnolines, phthalazines, quinolines, isoquinolines, quinolones, and quinoxalines. The different reactions utilized to obtain the target N-sulfonyl benzoazines such as; condensation, Reissert-type react...

N-Sulfonyl benzoazoles are a kind of ubiquitous core structural motif, which can be found in various bioactive molecules and pharmaceuticals. Consequently, displaying efficient synthetic methods to deliver the structurally diverse N-sulfonyl benzoazoles such as indoles, benzoxazoles and benzothiazoles represent an important objective in our chapter...

N-Sulfonyl pyridine motifs are well-known features of bioactive small molecules, and therefore a synthesis of these and related 6-membered heterocycles has received a lot of attention. Many N-sulfonyl pyridine derivatives, such as pyrdinone, pyridine, oxazine, and thiazine derivatives, as well as their corresponding benzene fused derivatives, are c...

Imidazole is one of the most prominent, five-membered, nitrogen-containing, heterocyclic scaffolds, and its ring forms the main structure of several well-known components of the human organisms, such as amino acid histidine, a component of DNA base structure and purines, histamine, and biotin. A large number of pyrazoles have been synthesized and a...

Sulfonyl-activated azetidines and azetidin-2-ones are two types of activated four-membered aza-heterocycles that have gotten a lot of attention because of its superior electron-withdrawing ability of sulfonyl groups bearing nitrogen atoms, which enabled nucleophilic ring-opening reactions as well as their participation in living aza-anionic polymer...

Cyclin dependent kinases (CDKs) enzymes regulate cell proliferation and transcriptional processes and can be considered as important targets for the development of anticancer and antimicrobial drugs. In this work, novel benzothiazolyl pyrazolopyrimidine carboxamide and benzothiazolyl pyrazolopyrimidine carbonitrile derivatives were synthesized and...

Abu-Zaied MA, Loutfy SA, Hassan AE, Elgemeie GH. Drug Des Devel Ther. 2019;13:2437–2457. The Editor and Publisher of Drug Design, Development and Therapy wish to retract the published article. Concerns were raised regarding the duplication of images in Figure 5. Specifically, Figure 5A, image for compound 4, appears to have been duplicated with Fi...

A novel series of pyridine, cytosine, and uracil thioglycoside analogs (4a-i, 9a,b, and 13a,b, respectively) and their corresponding phosphoramidates (6a-I, 10a,b, and 14a,b, respectively) were synthesized and assessed for their antiviral inhibitory activities in a dual-pathogen screening protocol against SARS-CoV-2 and influenza A virus (IAV). MTT...

New Strategies Targeting Cancer Metabolism: Anticancer Drugs, Synthetic Analogues and Antitumor Agents presents up-to-date synthetic strategies for three categories of antimetabolites: antifolates, purines and pyrimidines, the main classes of antimetabolites which are integrated into various pharmaceutical agents. Many of these antimetabolites are...

In the title compound, C 22 H 20 N 2 O 2 , both six-membered rings of the fused heterocyclic system display envelope conformations; the two carbon atoms bearing the methyl groups and the naphthyl substituent both lie outside the planes of the other atoms of each ring. In the crystal, the amino group forms hydrogen bonds of the types N—H...O=C and N...

In the title compound, C32H29BrN2O10S3, the benzo­thia­zole and thio­phene ring systems subtend an inter­planar angle of 7.43 (12)°. The NH2 group forms intra­molecular hydrogen bonds to Nthia­zole and Ocarbon­yl. The Sgalactose—Cthio­phene bond is short [1.759 (2) Å]. The mol­ecules are connected to form ribbons parallel to the b axis by two ‘weak...

Cyclin dependent kinases (CDKs) are a group of enzymes involved in different phases of the cell cycle. In addition, it has been reported that CDK9 could be used as a crucial target for the development of antiviral drugs such as purine analogues; roscovitine and dinaciclib. A new series of benzothiazolyl pyrazolopyrimidine carboxamide derivatives we...

In the title compound, C16H9NO2S, the inter­planar angle is 6.47 (6)°. An intra­molecular S⋯O=C contact of 2.727 (2) Å is observed. The packing is determined by several types of weak inter­action (‘weak’ hydrogen bonds, S⋯S contacts and π–π stacking).

The title compound, C15H13NO2S, was synthesized efficiently in the solid state by exploiting pepsin catalysis. The ring systems are nearly coplanar [inter­planar angle of 5.38 (2)°] with an associated intra­molecular S⋯O=C short contact of 2.7082 (4) Å. The packing involves C—H⋯O, C—H⋯π and π–π contacts.

In the title compound, C14H14N2S3, the double-bond system of the acrylo­nitrile moiety is significantly non-planar, with absolute cis torsion angles of 13.9 (2) and 15.1 (2)°. The ring system and the double bond system subtend an inter­planar angle of 11.16 (4)°. The wide angle C—C(CN)=C of 129.40 (12)° may be associated with a balance between plan...

Aims: The current study aimed to synthesize novel pyrazolo[1,5-a]pyrimidines based on 5- aminopyrazoles 3, evaluate their antimicrobial activity, and study the minimum inhibitory concentration (MIC) for the most active compounds. In addition, molecular docking studies and RNA polymerase inhibitory activity were determined. Background: Starting w...

In this study, olefin adducts were synthesized from Wittig reactions on carbonyl group and stereo-identity of the alkene products. The reaction of 11H-Indeno[1,2-b]quinoxalin-11-one with few stabilized phosphonium ylides yielded a combination of the corresponding E and Z olefins in each case. On the other hand, the reaction of 11H-indeno[1,2-b]quin...

Alkylating agents are considered as the oldest antineoplastic drugs that have significant effects. Novel synthetic strategies for many anticancer alkylating agents, including nitrogen mustards, chlorambucil, melphalan, ifosamide, oxaliplatin, and temozolomide, were accomplished.

Pyrimidine nucleosides are effective compounds that have pivotal effects in medicinal chemistry. They endowed with diverse pharmacological activities. Novel synthetic strategies for many anticancer pyrimidine nucleosides, including ribonucleosides, pyranose nucleosides, phosphonated nucleosides, and a variety of modified pyrimidine nucleosides, wer...

Purine nucleoside analogs are effective compounds have a significant and pivotal effects in several fields. Novel synthetic strategies for many anticancer purine nucleoside analogs were reported.

Purine drugs are significant chemotherapeutic agents and are universally accepted as one of the principal categories of antimetabolites. Many purine-based drugs such as mercaptopurine, thioguanine, azathioprine, pentostatin, cladribine, fludarabine phosphate, clofarabine, and nelarabine are depicted in this chapter.

Natural products (NP) have offered some of the most significant drugs for treating cancer. They provide a variant type of contribution that is also essential for modern drug discovery and development. A wide variety of anticancer drugs currently in clinical utility are derived from natural products such as camptothecins, vinca alkaloids, derivative...

Antifolates possess an indispensable role in medicinal chemistry as they exhibit valuable pharmacological activities. Their benefits have continued to expand in an intense pace. Recognizing their importance in surmounting critical diseases such as cancer, novel synthetic strategies for antifolates were addressed. Antifolates are the key parts of th...

Antifolates, which are inhibitors of the folate biosynthetic pathway, have been shown to be effective in inhibiting the growth of proliferating malignant mammalian cells as well as proliferating bacterial and protozoal infections. Drugs that target the folate pathway have a substantial impact on cancer therapy. The development of new antifolate-bas...

An outline of the biochemistry of nucleotide metabolism is provided in this chapter. Synthesis and degradation of nucleotides were emphasized. Targets for chemotherapeutic agents and inhibition of biosynthetic pathways are depicted. Most of the anticancer agents synthesized during decades of intensive research were structural analogs of various pyr...

Pyrimidine-based anticancer drugs, including analogs of cytosine such as cytarabine, elacytarabine, fazarabine, azacitidine, gemcitabine, sapacitabine, or uracil as fluorouracil, capecitabine, floxuridine, doxifluridine, tegafur, carmofur, and trifluridine, demonstrate an antineoplastic activity.

Antimetabolites are effective compounds having significant and pivotal effects in medicinal chemistry. They remain as mainstays in cancer chemotherapeutics as well as many nonmalignant diseases. Selected approaches from our researches which comprise new synthetic strategies of novel antimetabolic analogs are accomplished in this chapter including t...

In the title compound, C 18 H 17 N 3 O 4 S, the pyrazole ring is planar, with the sulfur atom lying 0.558 (1) Å out of the ring plane. The NH 2 group is involved in an intramolecular hydrogen bond to a sulfonyl oxygen atom; its other hydrogen atom forms an asymmetric three-centre hydrogen bond to the two oxygen atoms of the —O—CH 2 —C=O— grouping,...

In the mol­ecule of the title compound, C16H13N3O2S, one hydrazinic nitro­gen atom is essentially planar, but the other is slightly pyramidalized. The torsion angle about the hydrazinic bond is 66.44 (15)°. Both hydrazinic hydrogen atoms lie anti­periplanar to the oxygen of the adjacent carbonyl group. The mol­ecular packing is a layer structure de...

A class of pyrimidine thioglycoside analogs (6a–h) were synthesized from a reaction of 2-cyano-3,3-dimercapto-N-arylacrylamide (2a–d) and thiourea to produce the corresponding 4-amino-2-mercapto-N-arylpyrimidine-5-carboxamide derivatives (3a–d), and stirring of compounds (3a–d) with peracylated α-d-gluco- and galacto-pyranosyl bromides (4a,b) in DM...

Aims Producing novel pyrazolotriazines such as pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[5,1-c][1,2,4]triazine derivatives and evaluate their biological activity as antimicrobial agents followed by the Minimum Inhibitory Concentration (MIC) for the most active compounds. Moreover, study the molecular docking and the RNA polymerase inhibitory acti...

In the title compound, C14H17N3O5S, the five-membered ring is essentially planar. The substituents at the nitro­gen atoms subtend a C—N—N—S torsion angle of −95.52 (6)°. The amino group forms an intra­molecular hydrogen bond to a sulfonyl oxygen atom; two inter­molecular hydrogen bonds from the amino group, to the other S=O group and to the oxo sub...

The title compounds 3a, C14H13N5OS, and 3b, C13H12N6OS, both show an E configuration about the N=C bond and a planar NH2 group. The mol­ecules, which only differ in the presence of a phenyl (in 3a) or pyridyl (in 3b) substituent, are closely similar except for the different orientations of these groups. The amino hydrogen atoms form classical hydro...

Purpose This study aims to represent a successful simple method for the synthesis of some novel dyes based on thiazole derivatives and their applications in textile printing. Design/methodology/approach 2-(benzo[d]thiazol-2-ylmethyl)thiazol-4(5H)-one compound is prepared by convention heating and microwave technique then used as a coupling agent,...

Novel class of amino pyrimidine thioglycoside derivatives were designed from sodium 2-cyano-3-(arylamino)prop-1-ene-1,1-bis(thiolate) 1a-d and guanidine hydrochloride 2 to afford the corresponding sodium 2,6-diamino-5-aryl-1,2-dihydropyrimidine-4-thiolate 3a-d, which in coupling with peracylated α-D-gluco- and galactopyranosyl bromides 5a,b in DMF...

In this article, a series of benzothiazole-bearing N-sulfonamide 2-pyridone derivatives were synthesized via the reaction of benzothiazole sulfonylhydrazide with sodium salts of both (hydroxymethylene) cycloalkanones and unsaturated ketones, as well as ethoxymethylene derivatives. The structures of the resultant compounds were confirmed using IR, ¹...

This study describes a new route to the synthesis of novel benzamide-based 5-aminopyrazoles and their corresponding pyrazolo[1,5-a]pyrimidine and pyrazolo[5,1-c][1,2,4]triazine derivatives. Benzamide-based 5-aminopyrazoles were prepared through a reaction of benzoyl isothiocyanate with malononitrile in KOH-EtOH followed by alkylation with alkyl hal...

A series of pyrimidine and pyrimidine thioglycoside derivatives were newly synthesized using sodium 2-cyano-3-(arylamino)prop-1-ene-1,1-bis(thiolates) and urea to give the corresponding sodium 6-amino-5-aryl-2-oxo-1,2-dihydropyrimidine-4-thiolates. Stirring of the latter with peracetylated α-d-gluco- and galacto-pyranosyl bromides in DMF afforded t...

This research reports a novel method for synthesizing a new class of indeno[1,2-b]pyridine thioglycosides. This series of indenopyridine thioglycosides was designed by the reaction of (E)-2-cyano-3-(furan/or thiophene-2-yl)prop-2-enethioamide 1a or 1b with 1-indanone 2 to give the corresponding 2-thiooxo-1H-indeno[1,2-b]pyridine-3-carbonitriles 3a,...

The synthesis and antiviral screening of the first reported series of pyridine- and pyrimidine-based thioglycoside phosphoramidates are herein reported. They were prepared through two synthetic steps: The first step is via coupling of mercapto-derivatized heterocyclic bases with the appropriate α-bromo per-acetylated sugars. The second one is the h...

Sulfonamides and trimethoprim (TMP) drugs are normally used to inhibit the action of dihydropteroate synthase (DHPS) and dihydrofolate reductase (DHFR) enzymes, respectively. In this work, a new series of N-sulfonamide 2-pyridone derivatives that combine the inhibitory activities of DHPS and DHFR into one molecule were synthesized and evaluated for...

In the title compound, C13H15N3O5S, the two rings face each other in a ‘V′ form at the S atom, with one N—H⋯O=S and one C—H⋯O=S contact from the pyrazolyl substituents to the sulfonyl group. Two classical hydrogen bonds from the amine group, one of the form N—H⋯O=S and one N—H⋯O=Coxo, link the mol­ecules to form layers parallel to the bc plane.

A series of novel substituted 2-pyrimidylbenzothiazoles incorporating either sulfonamide moieties or the amino group at C2 of the pyrimidine ring were synthesized and evaluated for its antiviral potency. The novel synthesis of the ring system was carried out by reacting guanidine or N-arylsulfonated guanidine with different derivatives of ylidene b...

Benzothiazole compounds are the most used heterocyclic compounds in medicinal chemistry, a common and complementary feature of many pharmaceuticals. Benzothiazole derivatives and their metal complexes offer a variety of pharmacological properties, and a high degree of structural diversity that has proven important for the search for new therapeutic...

In the title com­pound, C20H26N2O9S, the S atom is attached equatorially to the sugar ring. The C—S bond lengths are unequal, with S—Cs = 1.8018 (13) Å and S—Cp = 1.7662 (13) Å (s = sugar and p = pyrimid­yl). In the crystal, a system of three weak hydrogen bonds, sharing an oxygen acceptor, links the mol­ecules to form chains propagating parallel t...

The synthesis of novel pyrido[2,1-b]benzothiazole and pyrido[2,1-b]benzoimidazole derivatives was achieved via the reaction of N-aryl-2-cyano-3,3-bis(methylthio)acrylamide with benzothiazoleylacetonitrile and benzoimidazoleylacetonitrile, respectively, while N-substituted 2-pyridylbenzothiazole derivatives were synthesized by reacting 2-(benzo[d]th...

N-sulfonylamino azinones has attracted the interest of numerous researchers and extensive investigations on their biological activities have been done. The present review provides an overview of the patents and reports filed during the last few years pertaining to the synthesis N-sulfonyl azinones as well as their biological and preclinical studies...

Abu-Zaied MA, Loutfy SA, Hassan AE, Elgemeie GH. Drug Des Devel Ther. 2019;13:2437–2457. The Editor and Publisher of Drug Design, Development and Therapy wish to retract the published article. Concerns were raised regarding the duplication of images in Figure 5. Specifically, Figure 5A, image for compound 4, appears to have been duplicated with Fig...

Spent bleaching earth (SBE) recycling and utilization as an adsorbent to eliminate dyes from aqueous solution was studied. Organic solvents and subsequent thermal treatment were carried out to recover and reactivate the SBE. The effect of pH, temperature, dye's initial concentration, and contact time on the dye removal using recycled spent bleachin...

The title compound, C10H11N3O, crystallizes in the triclinic space group P with Z′ = 2. The two independent mol­ecules (A and B) differ in the orientation of the phenyl rings with respect to the plane of the triazine ring, with an interplanar angle of 11.45 (6)° in mol­ecule A and 19.71 (5)° in mol­ecule B, in the opposite sense. In the crystal, cl...

This study reports a novel and efficient method for the synthesis of the first reported novel class of pyrazole thioglycosides 6a–h. These series of compounds were designed through the reaction of sodium 2-cyano-3-oxo-3-(4-substitutedphenylamino)prop-1-ene-1,1-bis(thiolate) salts 2 with hydrazine hydrate in ethanol at room temperature to give the c...

A synthesis of novel bis(aminopyrazoles) by the reaction of hydrazine hydrate with the appropriate bis(2‐cyanoketene‐S,N‐acetals) was reported. The latter compounds were prepared by treatment of bis(cyanoacetamides) with phenyl isothiocyanate in KOH/EtOH and subsequent alkylation with methyl iodide. The utility of bis(2‐cyanoketene‐S,S‐acetals) as...

Pyrimidine and purine nucleosides have a remarkable and comprehensive impact on medicinal chemistry and pharmaceutical industries. They become key parts of the growing interdisciplinary area of antimetabolites. The paramount importance of the nucleoside analogs triggered their broader use in treatment of critical diseases such as cancer, malignanci...

The title compound, K⁺·C18H14N5O2S3⁻·C3H7NO·0.5H2O, was obtained in a reaction designed to deliver a neutral 2-pyrimidylbenzo­thia­zole. The anion is deprotonated at the sulfonamide nitro­gen. The asymmetric unit of the title compound contains two potassium cations, two anions, two mol­ecules of DMF and one of water. The anions display some conform...