Haythem Saadeh

• Doctor of Philosophy
• Faculty Member at University of Jordan

A series of eight N-(1H-benzo[d]imidazol-2-yl)-2-(4-arylpiperazin-1-yl)acetamides was synthesized as potential anticancer agents. Reacting 2-aminobenzimidazole (1) with 2-chloroacetyl chloride in the presence of the base gave N-(1H-benzo[d]imidazol-2-yl)-2-chloroacetamide (2) which then reacted with substituted piperazines 3a-h to give the targeted...

N-arylcyanothioformamides are useful coupling components for building key chemical intermediates and biologically active molecules in an expedited and efficient manner. Similarly, substituted (Z)-2-oxo-N-phenylpropanehydrazonoyl chlorides have been utilized in numerous one-step heteroannulation reactions to assemble the structural core of several d...

Sensitive spectrofluorometric and liquid chromatography with fluorescence detection methods have been developed for detection and determination of naproxen drug in the presence of cucurbit7uril (CB7). Fluorescence signals have been improved with the addition of CB7 to the drug aqueous solution. Fluorescence spectroscopy, mass spectrometry, ¹H-NMR,...

Selenoureas are widespread as useful elements for constructing important species and biologically active molecules. Finding an efficient and straightforward method to prepare this motif and biologically screen derivatives thereof is crucial. Herein, we demonstrate the effectiveness of using ethanol as a solvent in the preparation of various substit...

The author wishes to make the following correction to this paper [...]

A number of novel urea and thiourea derivatives of 8-hydroxyquinoline have been designed, synthesized and evaluated for their anticancer activities. The structures of the new compounds were established by spectroscopic techniques, ¹H NMR, ¹³C NMR, and mass spectrometry. The in vitro cytotoxicity against MCF7, and MDA-MB-231 cell lines were assessed...

A new fluorescent dye (4PBZC) comprising coumarin (C), piperazine (P), and benzimidazole (BZ) was designed, prepared, and complexed to cucurbit[7]uril (CB7) to detect carnosol (CAR), an anti-breast cancer drug, in sub-nanomolar concentrations utilizing the supramolecular indicator displacement assay strategy, the CB7-assisted pKa shift, and the CB7...

A new series of urea and thiourea derivatives containing benzimidazole group as potential anticancer agents have been designed and synthesized. The structures of the synthesized compounds were characterized and confirmed by spectroscopic techniques such as 1H NMR, 13C NMR, and mass spectrometry. In vitro anticancer assay against two breast cancer (...

A novel multifunctional fluorescent molecule (Bz-8HQ) has been designed and synthesized from the linkage of benzimidazole (Bz) and 8-hydroxyquinoline (8HQ). The synthesis was straightforward and involved reacting (piperazin-1-yl)-1H-benzo[d]imidazole with 5-(chloromethyl)quinolin-8-ol...

Compounds containing the 8-hydroxyquinoline (8-HQ) 1 nucleus exhibit a wide range of biological activities, including antimicrobial, anticancer, and antifungal effects. The chemistry and biology of this group have attracted the attention of chemists, medicinal chemists, and professionals in health sciences. A number of prescribed drugs incorporate...

Background Curcumin is a safe, versatile natural product with unlimited number of biological activities and a precursor for various heterocyclic compounds. Objective Present study was aimed to development of a curcumin based antimicrobial reagent with high potency against gram-positive and gram-negative bacteria. Methods Herein we report a simple...

In continuation of our research directed towards development of biologically active alkaloids form natural products, herein we report a simple and convenient one step synthetic method for making 1,4-benzodiazepines via condensation cyclization of various 1,2-phenylenediamine with Curcumin. Following the developed method, a series of new 1,4-benzodi...

The search for synthetic selective compounds for G-protein-coupled receptors has provided a myriad of molecules with high selectivity and therapeutic potential. In some cases, however, selectivity is difficult to obtain. For instance, the selectivity ratio is relatively low for compounds acting on D2 and D3 dopamine receptors, which are targets of...

A novel series of 5-nitroimidazole-piperazines (4a–j) and 5-nitrothiazole-piperazine (7a–j) have been prepared in good yields. The antigiardial and antitrichomonal activities of these new compounds were evaluated. Majority of the compounds was found to be more active against Giardia lamblia as compared to metronidazole at 24 hours of incubation. Af...

We describe here the synthesis, antioxidant capacity, and biological activities on MAO, ChE, and selected GPCRs, of novel 1-(2,5-dimethoxybenzyl)-4-arylpiperazines 1–10, as well as known N-(2-(2-methyl-5-nitro-1H-imidazol-1-yl))-2-(4-arylpiperazin-1-yl) 11–20 and N-(5-nitrothiazol-2-yl)-2-(4-arylpiperazin-1-yl) 21–29. Some of the new 4-arylpiperazi...

Antimicrobial resistance to drugs is a serious threat to public health. Different strategies have been adopted to deal with antimicrobial resistance to known drugs, one such strategy is the use of drug hybrids; this is a promising strategy to address the growing problem of drug resistance. The present review covers the very recent examples of combi...

Absorbent properties of the prepared superabsorbent polymers were evaluated in saline solution and results showed high dependency of the absorbent properties on the cross-linking agent polarity and concentration. Superabsorbent polymers cross-linked with EAS and GDGE showed the highest absorbency under loading and indicated that they formed gels wi...

A number of novel compounds containing 5-nitrothiazole moiety as potential antiparasitic agents have been synthesized through known chemical routes. The structures of the new compounds were confirmed by spectroscopic techniques, 1H NMR, 13C NMR, and mass spectrometry, and by elemental analyses. The prepared compounds were evaluated in vitro for the...

A new series of metronidazole derivatives containing piperazine rings were prepared via the reaction of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)acetyl chloride with selected substituted piperazines in the presence of a base. Structures of the new compounds were confirmed by NMR and MS spectral data and by elemental analyses. The antibacterial and anti...

A number of novel Schiff bases (5a–i) and (7a–d) derived from metronidazole were synthesized. Reaction of 2-(2-methyl-5-nitro-imidazol-1-yl)-ethyl ester toluene-4-sulfonate with 4-hydroxybenzaldehyde and with 3-hydroxybenzaldehyde in the presence of a base afforded 4-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)benzaldehyde (5) and 3-(2-(2-methyl-5...

The effects of metronidazole (MTZ) and novel synthesized MTZ derivatives on in vitro cultured Echinococcus granulosus protoscoleces (PSCs), 30 day old segmentation stage and hydatid cysts (HC) developing secondarily in BALB/c mice were compared to those caused upon treatment with comparable doses of albandazole (ABZ) and mebendazole (MBZ) drugs. Th...

Series of new metronidazole urea and thiourea derivatives have been prepared in good yields through reactions of 2-(2-methyl-5-nitroimidazolyl) ethylamine hydrochloride with various cyanates and isothiocyanates. Similarly, metronidazole hydroxybenzoic acid derivatives were synthesized by reacting 2-(2-methyl-5-nitro-1H-imidazol- 1-yl)ethyl-4-methyl...

Series of new amidrazones Ia-c, IIa-c, and IIIc, incorporating 5-nitroimidazole (a), ciprofloxacin (b), and 7-chloro-4-piperazinylquinoline (c) moieties, were synthesized by reacting hydrazonoyl chlorides I-III, derived from 4-fluoroaniline and 4-chloroaniline with the proper amine, in the presence of triethylamine. Structures of the prepared compo...

The self-assembly of cyclohexylamine dithiocarbamate (C6DTC) on gold (Au) and gold nanoparticles (AuNPs) was studied electrochemically using cyclic voltammetry (CV). Cyclic voltammetry was used to study the system at the electrode surface of (C6DTC/Au) and (C6DTC/AuNPs). The application of the resulting chemically modified surface as a selective se...

A series of novel Schiff bases; compounds 3a–j were prepared by reacting 1-(2-aminoethyl)-2-methyl-5-nitroimidazole dihydrochloride monohydrate (1) with different aldehydes. The structures of these compounds were confirmed through different spectroscopic methods such as 1H-NMR, 13C-NMR and mass spectrometry and also by elemental analyses. The prepa...

Title compounds [A, B and C; x = 0-5, y = 0-5, z = 0-4] were prepared by Suzuki coupling reaction in good yields. Coupling chlorobenzeneboronic acids with 1,2- or 1,3-dibromochlorobenzenes gave A and B respectively. Coupling chlorobromobenzenes with 1,4-benzenediboronic acids or chlorobenzeneboronic acids with 1,4-dibromochlorobenzenes gave C.

A novel polymeric ligand having 2,2′:6′,2″-terpyridine as pendant group was prepared through a Williamson type etherification approach for the reaction between 4′-hydroxy-2,2′: 6′,2″-terpyridine and the commercially available 4-chloromethyl polystyrene. The chelating properties of the new polymer toward the divalent metal ions (Cu2+, Zn2+, Ni2+, an...

Herein we describe the synthesis of a new series of copolymers (PSeBx) containing selenopheno[3,4-b]selenophene and benzodiselenophene, which exhibited a high power conversion efficiency (PCE) of 6.87% in a bulk heterojunction (BHJ) solar cell device (PSeB2/ PC71BM). In comparison with its thiophene analogue, PTB9, the new p olyse len ophen o [3,4-...

In this study, the screening of five anthraquinones (purpurin, xanthopurpurin, rubiadin, kermisic acid and flavokermisic acid), for their free radical scavenging and antioxidant effects was carried out, using three complementary methods. DPPH (2,2'-diphenyl-1-picrylhydrazyl) revealed that purpurin has a scavenging effect with IC50 = 3.491 ± 0.014 µ...

A number of new compounds derived from metronidazole and amino acids and their esters have been synthesized through a reaction between 2-(2-methyl-5-nitro-1H-imidazol-1-yl)acetic acid and a number of amino acid esters in the presence of N,N′carbonyldiimidazole (CDI). Hydrolysis of the esters derivatives with sodium hydroxide (4%) followed by acidif...

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AbstractNew 1,2,4-triazole-3-thiol metronidazole derivatives have been synthesized by treating 1,2,4-triazole-3-thiols with metronidazole tosylate (toluene-4-sulfonic acid 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester) in DMF and in the presence of potassium carbonate as a base. S-alkylated and N-alkylated products were obtained, with the S-alky...

A number of peptidyl metronidazole derivatives were synthesized in 99% yield through solid phase peptide synthesis. The newly prepared compounds were tested against Entamoeba histolytica and Giardia intestinalis and were found to be much less active than metronidazole against the aforementioned parasites; apparently the introduction of the peptide...

A no. of peptidyl metronidazole derivs. were synthesized in 99 % yield through solid phase peptide synthesis. The newly prepd. compds. were tested against Entamoeba histolytica and Giardia intestinalis and were found to be much less active than metronidazole against the aforementioned parasites; apparently the introduction of the peptide moiety on...

Three novel new compounds derived from antiparasitic precursors have been synthesized and tested for their antiamoebic and antigiardial activities. The condensation of 2-(2-methyl-5-1H-nitroimidazolyl)ethylamine (6) with 5-nitro-2-furylacrylic acid (7) gave 3-(5-nitrofuran-2-yl)-N-[2-(5-nitroimidazol-1-yl)ethyl]acrylamide (8). Condensation of 7 wit...

A number of 5-aryl-1-methyl-4-nitroimidazoles 5a-f have been synthesized in good yields by the Suzuki coupling reaction between 5-chloro-1-methyl-4-nitroimidazole (3) and arylboronic acids 4a-f, aided by dichlorobis-(triphenylphosphine)palladium(II), K2CO3, and tetrabutylammonium bromide in water at 70-80 °C. Compounds 5a-f were characterized by el...

A number of new benzofuran derivatives, ethyl 3-[(alkylamino)methyl]-6-methoxy-1-benzofuran-2-carboxylates (5a-i), were obtained via the reaction between ethyl 3-(bromomethyl)-6-methoxy-1-benzofuran-2-carboxylate (3) and amines or amino acid ethyl esters. In addition, 1,4-bis[(ethyl 6-methoxy-1-benzofuran-3-yl-2-carboxylate)methyl]piperazine (9), N...

The Stille coupling reaction was explored to synthesize novel polymers with a pending NLO chromophore exhibiting a large μβ value but high chemical sensitivity. This approach enabled the synthesis of aromatic polyimides through the careful design of dibromo monomers bearing NLO chromophores. The resulting polyimide was shown to possess a glass tran...

A novel series of amorphous molecular materials containing carbazole and methine dyes have been synthesized and characterized for photorefractive applications.

This paper summarizes our research effort in developing polyimides functionalized with nonlinear optical chromophores for applications in second order nonlinear optical devices. In the past several years, we have developed several general synthetic approaches to these materials. Detailed physical characterization indicated that these materials are...

To synthesize nonlinear optical polyimides exhibiting high nonlinearity and high thermal stablity, a new monomer bearing phenylenediamine and a diazo benzene-type nonlinear optical chromophore (compound 1) was synthesized and polymerized with 4,4‘-(hexafluoroisopropylidene)diphthalic anhydride. This diazo chromophore possesses a microscopic optical...

A new polyphenylene-co-furan (PPF) and a polyhenylene-co-thiophene (PPT) have been synthesized utilizing the Stille coupling reaction and their luminescence properties characterized. The UV−vis, electroluminescence (EL), photoluminescence (PL), and current−field (I−F) characteristics, as well as the stability of the emission of light, were studied...

Molecules of the title compound, methyl 1-benzyl-4-nitro-5-imidazolylthioacetate, C13H13N3O4S, can be viewed as an arrangement of three intersecting planes of atoms. The plane of the imidazole ring and its bonded atoms (r.m.s.d. = 0.030 Angstrom) intersects the plane of the benzyl group (r.m.s.d. = 0.004 Angstrom) at an angle of 89.0(5)degrees. The...

Selected series of 6-substituted 4-aryl-3-heteroaryl-1-methyl-1,2,3,4-tetrahydro-s-tetrazines (V;1-12) were synthesized via direct interaction between appropriate nitrile imine and model methylhydrazones. The extent of "ring-chain" tautomerism, as evidenced from nmr spectral data of V, is dependent on the nature of substituents at N-4, C-3, and C-6...

The kinetics of the acid and base hydrolysis of salicylhydroxamic acid (SHAM) and O-acetyl-salicylhydroxamic acid (OAc-SHAM) were studied using High Performance Liquid Chromatography with UV-Detection (HPLC-UV). The effect of temperature and pH values on the hydrolysis was investigated. It was found that both SHAM and OAc-SHAM were more stable in b...