Obaid-ur-Rahman Abid

Hazara University · Department of Chemistry

Inflammation is a complex physiological response associated with the onset and progression of various disorders, including diabetes. In this study, we synthesized a series of diclofenac acid derivatives and evaluated their potential anti-diabetic and anti-inflammatory activities. The compounds were specifically assessed for their ability to inhibit...

In this study, chitosan, polyvinyl alcohol (PVA), and polyvinyl pyrrolidone (PVP) were used to create ternary blends reinforced with organically modified montmorillonite nanoclay. Tramadol was used as a model drug to assess the efficacy of these ternary blends as drug delivery systems. The current work demonstrated the highly controlled release of...

In search of new α-glucosidase and urease inhibitors, a series of naproxen-derived 1,3,4-oxadiazole-containing ketones 6a-e and their Schiff-base derivatives 7a-o were synthesized. The isolated compounds were identified by HRMS (EI), 1 H NMR and 13 C NMR spectroscopic techniques. Among the series, compounds 7j, 7i, 7e, 7d and 7o were found to be si...

Cancer is one of the most fatal diseases globally, however, advancement in the field of nanoscience specifically novel nanomaterials with nano-targeting of cancer cell lines has revolutionized cancer diagnosis and therapy and has thus attracted the attention of researchers of related fields. Carbon Dots (CDs)–C-based nanomaterials–have emerged as h...

A series of Schiff bases(3-8) were synthesized by the reaction of cefradine with six different aldehydes/ketones. These Schiff bases(3-8) were treated with different bases/salt (NaOH, KOH, Ca(OH)2, Ba(OH)2, Ag(NO)3) to get their metal salts. Structures of the products were ascertained by spectroscopic data. The synthesized compounds were tested for...

Drug design and delivery is primarily based on the hunt for new potent drug candidates and novel synthetic techniques. Recently, saturated heterocycles have gained enormous attention in medicinal chemistry as evidenced by the medicinal drugs listed in the FDA Orange Book. Therefore, the demand for novel saturated heterocyclic syntheses has increase...

This study aim to synthesize new 1,3,4-oxadiazole derivatives incorporating mefenamic acid as promising α-glucosidase and urease inhibitors, potentially leading to the treatment of postprandial hyperglycemia as well as H. pylori related disorders. In this regards, we have designed a series of Mefenamic acid derivatives. The synthetic compounds were...

Enzyme inhibitors are vital aspects for studying enzymes and are employed as drugs to treat certain disorders, thus implying pivotal role in drug discovery. In the current study, a series of triazole compounds 4(a-o) were synthesised to explore their inhibitory potential against α-glucosidase and urease enzymes. These derivatives with dichloropheny...

In this study, ternary blends based on chitosan, polyvinyl alcohol, and polyethylene glycol reinforced with organically modified montmorillonite (nanoclay) clay were synthesized. These ternary blends were evaluated as transdermal drug delivery patches using tramadol as a model drug. The FTIR study showed interaction among important functional group...

Inflammation is the immune system's adaptive response to tissue dysfunction or homeostatic imbalance, inducing fever, pain, physiological and biochemical changes via the cyclooxygenase (COX) and lipoxygenase (LOX) pathways. NSAIDs (non-steroidal anti-inflammatory drugs), such as diclofenac acid and naproxen, are the most common inhibitors of the CO...

This study reports the synthesis of a series of ibuprofen derivatives, including thiosemicarbazides 4a–f, 1,3,4‐oxadiazoles 5a–f, 1,3,4‐thiadiazoles 6a–f, 1,2,4‐triazoles 7a–f, and their S‐alkylated derivatives 8a–d. All of the newly synthesized derivatives were analyzed using 1H NMR, 13C NMR spectroscopy, and high‐resolution mass spectra (electron...

A series of 28 novel naproxen derivatives (4a-f, 5a-f, 6a-d, 7a-f, and 8a-f) have been designed, synthesized, and characterized. The synthesized derivatives were assessed as dual inhibitors for 15-lipoxygenase (LOX) and α-glucosidase enzymes and checked for cytotoxicity and ADME studies. The inhibitory potential of naproxen derivatives for 15- LOX...

Present study aimed at the discovery of new non-sugar α-glucosidase inhibitors includes synthesis of a series of 1,3,4-oxadiazole based Schiff base derivatives of ibuprofen. Initially oxadiazoles from ibuprofen were synthesized by treating ibuprofen hydrazide with carbon disulfide. Oxadiazoles upon treatment with different substituted phenacyl brom...

Methanol–water system possesses unusual interactions, which may affect surfactant self‐assembly. The main objective of this study was to investigate the interactions and aggregation behavior of ionic surfactants sodium dodecyl sulfate (SDS) and cetyltrimethylammonium bromide (CTAB) and their equimolar catanionic binary mixtures (CAM) and their tern...

A series of piperonal-based imines (3a–c) and bis-imines (5a-o) have been synthesized in search of new urease inhibitors. Synthesized compounds were characterized by ¹H NMR, ¹³C NMR and EI-MS. These derivatives were subjected to evaluation of urease inhibitory potential, which exhibited a varied degree of potential, ranging from 41.7 ± 5.8 to 353.6...

The aim of the present study is to search out nontoxic silver nanoparticles synthesized from the leaf extract of two plants Ajuga parviflora Benth and Digera muricata for antimicrobial activity. The plants used in this investigation are rich in alkaloids, flavonoids, steroids, terpenoids, protein, amino acids, carbohydrate, quninones, phenols and t...

This article expansively summarizes the development of polyamide and polyhedral oligomeric silsesquioxane (POSS)-based nanocomposites. The general formula of POSS is (RSiO1.5)n, where R is the organic vertex group for polyhedral molecules. Mono- or multifunctional POSSs have been synthesized by modification of their reactive organic functional grou...

Hydrazones 6a-6n were synthesized from different amino acids with various aldehydes under reflux in methanol/ethanol. The structures of synthesized compounds were ascertained by elemental analysis and spectroscopic techniques. A comparative study of the antimicrobial activity and cytotoxicity was carried out of the N-protected amino acids, their es...

A series of hydrazones 5a–i were synthesized by the condensation of hydrazides derived from dichlorophenylacetic acids with different aromatic aldehydes and ketones. Their structures were confirmed by spectroscopic data and elemental analysis. Hydrazones 5a–i were evaluated for α-glucosidase and urease inhibition activities. Five compounds exhibite...

Bis-thiobarbiturate derivatives 1-15 have been synthesized, Characterized by 1HNMR and EI-MS and screened for urease inhibition. All compounds showed various degree of urease inhibitory activity with IC50 values ranging 7.45 ± 0.12-74.24 ± 0.81 μmol/L while the standard thiourea behaved normally (IC50 = 21.10 ± 0.12). Compounds 1 (IC50 = 7.45 ± 0.1...

Bis-Schiff bases of iosophthalaldehyde were synthesized by reacting isophthalaldehyde with hydrazine hydrate in 1:2 ratio in ethanol for 2-3 h under reflux. Product of first step was again reacted in 1:2 ratio with different aldehyde or acetophenone yielding bis-Schiff bases (1-16). All compounds were characterized by EI-MS and 1H NMR. All analogs...

Five novel triorganotin (IV) compounds have been synthesized and characterized. The tin atom is penta-coordinated to assume trigonal-bipyramidal geometry. Using in silico derived parameters; the objective of our study is to design and synthesize promiscuous antibacterials potent enough to combat resistance. Among various synthesized organotin (IV)...

Five novel triorganotin (IV) compounds have been synthesized and characterized. The tin atom is penta-coordinated to assume trigonal-bipyramidal geometry. Using in silico derived parameters; the objective of our study is to design and synthesize promiscuous antibacterials potent enough to combat resistance. Among various synthesized organotin (IV)...

The palladium(0)-catalyzed Suzuki cross-coupling reaction of the bis(triflates) of methyl 2,5-dihydroxybenzoate and methyl 2,4-dihydroxybenzoate afforded para- and meta-terphenyls, respectively. The reactions proceeded with very good site selectivity in favor of the sterically less hindered carbon atom.The palladium(0)-catalyzed Suzuki cross-coupli...

Some new transition metal complexes with monomethyl succinate are reported. Several physical techniques, such as elemental analysis and melting point, and in addition various spectroscopic techniques including 1H-, 13C-NMR and UV/visible and infrared spectroscopy were used to study the chemical structure of the prepared complexes. The octahedral ge...

A novel series of triorganotin(IV) complexes has been prepared, physically and spectrally investigated by elemental analyses, IR, 1H, 13C, 119Sn NMR, and 119mSn Mössbauer techniques respectively. 1:1 stoichiometry is confirmed through these results showing trigonalbipyramidale geometry. The synthesized complexes have been monitored against various...

The palladium(0)-catalyzed Suzuki cross-coupling reaction of the bis(triflates) of methyl 2,5-dihydroxybenzoate and methyl 2,4-dihydroxybenzoate afforded para- and meta-terphenyls, respectively. The reactions proceeded with very good site selectivity in favor of the sterically less hindered carbon atom.

A variety of fluorinated isocoumarins and dihydroisocoumarins, e.g. (III), (V), and thioisocoumarins like (VI) are prepared via construction of the isocoumarin skeleton, alkaline hydrolysis, reduction of the resulting keto acids, and cyclodehydration of the hydroxy acids formed to provide the dihydroisocoumarins (V).

Synthesis of some fluorinated isocoumarins and 3,4-dihydroisocoumarins is reported. Structures of the synthesized compounds were confirmed by spectral and elemental analysis. All the synthesized compounds were evaluated for their antimetastatic activity and anti-cancer activity against breast cell line (MCF-7). Among all the tested compounds 3h [3-...

The Suzuki-Miyaura reaction of phenyl 1,4-bis(trifluoromethylsulfonyloxy)-2-naphthoate and ethyl 3,5-bis(trifluoromethylsulfonyloxy)-2-naphthoate afforded various 1,4- and 3,5-diaryl-2- naphthoates with very good site-selectivity, respectively. The first attack occurred at the sterically more hindered positions C-1 and C-3, respectively. The select...

Palladium(0)-catalyzed Suzuki cross-coupling reactions of the bis(triflates) of 2′,4-dihydroxybenzophenones afforded 2′,4-diarylbenzophenones. The reactions proceeded with very good site selectivity in favour of the 4-position.

Aryl-substituted pyridines and pyrimidines were prepared by [4+2] cycloadditions of alkynyl-substituted pyridines and -pyrimidines with electron-rich dienes. The reactions proceed by formation of a bridged cycloadduct and subsequent thermal extrusion of ethylene. The pyridine moiety plays a crucial role for the success of the reaction.

An efficient procedure is elaborated for the synthesis of dihydropyranones (III) from readily available diketones (I).

The Me(3)SiOTf-mediated condensation of 1-ethoxy-2-fluoro-1,3-bis(trimethylsilyloxy) 1,3-dienes with 3-cyanochromones afforded 3-cyano-2-(4-ethoxy-3-fluoro-2,4-dioxobutyl)chroman-4-ones. Their reaction with triethylamine afforded fluorinated azaxanthones or biaryls. The product distribution depends on the structure of the diene. The formation of th...

The Suzuki-Miyaura reaction of the bis(triflate) of 3,4-dihydroxybenzophenone with two equivalents of boronic acids gave 3,4-diarylbenzophenones. The reaction with one equivalent of arylboronic acids resulted in site-selective attack onto carbon atom C-4. 3,4-Diarylbenzophenones containing two different aryl groups were prepared by sequential addit...

The palladium(0)-catalyzed Suzuki cross-coupling reaction of the bis(triflates) of phenyl 1,4-dihydroxy-2-naphthoate afforded various 1,4-diaryl-2-naphthoates. The reactions proceeded with very good site-selectivity. Due to electronic reasons, the first attack occurred at the sterically more hindered position C-1.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Ureases are important in both agriculture and human health. Bacterial ureases are directly involved in many farm-field problems and pathological conditions. Here, we report a structure-based virtual screening of an in-house compound bank of about 6000 molecular entities by computational docking and binding free energy calculations followed by in vi...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

The Suzuki-Miyaura reaction of N-methyl-2,3-dibromoindole with two equivalents of boronic acids gave symmetrical 2,3-diarylindoles. The reaction with one equivalent of arylboronic acid resulted in site-selective formation of 2-aryl-3-bromoindoles. The one-pot reaction of 2,3-dibromoindole with two different arylboronic acids afforded unsymmetrical...

The [4+2] cycloaddition of 1-ethoxy-2-chloro-1,3-bis(trimethylsilyloxy)-1,3-diene with dimethyl acetylenedicarboxylate (DMAD) afforded dimethyl 4-chloro-3,5-dihydroxyphthalate. Site-selective Suzuki–Miyaura reactions of its bis(triflate) provide a convenient approach to 3,5-diaryl-4-chlorophthalates containing two different aryl groups.

The palladium(0)-catalyzed Suzuki cross-coupling reaction of the bis(triflates) of methyl 2,5-dihydroxybenzoate afforded p-terphenyls. The reactions proceeded with very good site selectivity. The first attack occurred at carbon atom C-5.

The [4+2] cycloaddition of 1-ethoxy-2-fluoro-1,3-bis(trimethylsilyloxy)-1,3-diene with dimethyl acetylenedicarboxylate (DMAD) afforded dimethyl 4-fluoro-3,5-dihydroxyphthalate. Site-selective Suzuki-Miyaura reactions of its bis(triflate) provide a convenient approach to 3,5-diaryl-4-fluorophthalates.

The asymmetric unit of the title compound, C16H11FO2, contains two independent mol­ecules. The isochromene ring systems are planar and are oriented with respect to the fluoro­benzene rings at dihedral angles of 87.15 (3) and 87.85 (3)° in the two mol­ecules.

The asymmetric unit of the title compound, C16H11FO2, contains two independent mol­ecules. The isochromene ring systems are planar and are oriented with respect to the fluoro­benzene rings at dihedral angles of 87.15 (3) and 87.85 (3)° in the two mol­ecules.

The title compound, C16H13ClO3, is an important intermediate in the conversion of isocoumarin to 3,4-dihydroisocoumarin. The two aromatic rings are oriented at a dihedral angle of 67.18 (3)°. In the crystal structure, intermolecular O—H...O hydrogen bonds link the molecules into centrosymmetric dimers. There is also a C—H...π contact between the be...

In the title compound, C15H9ClINO2, which possesses anticonvulsant activity, the iodoindoline ring system is essentially planar (maximum deviation 1.245 Å) and is oriented with respect to the 3-chlorobenzyl ring at a dihedral angle of 76.59 (3)°. In the crystal, there is a π–π contact between iodoindoline ring systems [centroid–centroid distance =...

In the title compound, C15H9ClINO2, which possesses anticonvulsant activity, the iodo­indoline ring system is essentially planar (maximum deviation 1.245 Å) and is oriented with respect to the 3-chloro­benzyl ring at a dihedral angle of 76.59 (3)°. In the crystal, there is a π–π contact between iodo­indoline ring systems [centroid–centroid distance...

The title compound, C16H13ClO3, is an important inter­mediate in the conversion of isocoumarin to 3,4-dihydro­isocoumarin. The two aromatic rings are oriented at a dihedral angle of 67.18 (3)°. In the crystal structure, inter­molecular O—H⋯O hydrogen bonds link the mol­ecules into centrosymmetric dimers. There is also a C—H⋯π contact between the be...

The asymmetric unit of the title compound, C16H11ClO2, a chemically synthesized isocoumarin, contains three independent mol­ecules. The benzopyran and benzene rings are approximately perpendicular to each other, forming dihedral angles ranging from 83.08 (14) to 87.43 (11)°. In the crystal structure, mol­ecules are linked by inter­molecular C—H⋯O h...

The title compound, C10H10O2, is an important inter­mediate for the preparation of biologically active compounds. The mol­ecule is planar and weak C—H⋯O hydrogen bonding helps to stabilize the crystal structure.

In the title compound, C16H11ClO2, an unnaturally occurring isocoumarin, the benzene ring is nearly perpendicular to the planar isocoumarin ring system. The crystal packing is stabilized by intra- and inter­molecular C—H⋯Cl and C—H⋯O hydrogen bonds.