M. A. Salem

Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents

In the present investigation, furo[2,3-d]thiazol-5(2H)-one 5 was obtained from reaction of thiosemicarbazone derivative 2 with diethyl acetylene dicarboxylate. A series of newly synthesized 2-(hydrazinyl)thiazol-4(5H)-one 6, 7 &8 and 2-(4-(substituted)-thiazol-2-yl)hydrazono derivatives 9a, b &10 were synthesized from treatment of thiosemicarbazone derivative 2 with appropriate α-halogenated compounds. Also, a one pot synthesis of thiazole derivatives 13 &15 was achieved from three components reaction of hydrazone derivative 11 with phenyl isothiocyanate and α-halogenated compounds catalyzed by DMF/KOH. 4-(4-Morpholino phenyl) thiazol-2-amino 17 was obtained via the reaction of acetophenone derivative 1 with thiourea in presence of iodine. The reactivity of 2-aminothiazole 17 toward some electrophilic reagents was investigated. The structure of the newly compounds was confirmed on the basis of elemental analysis and spectral data. The antibacterial activity towards two Gram negative (Proteus mirabilis &Serratia marcesens) and two Gram positive (Staphylococcus aureus &Bacillus cereus) bacteria was investigated. The anti-inflammatory activity was also investigated and the inhibition of the carrageenin-induced oedema by these compounds was established.

Synthesis and characterization of new types of 2-(6-methoxy-2- naphthyl)propionamide derivatives as potential antibacterial and antifungal agents

A series of novel 2-(6-methoxy-2-naphthyl)propionamide derivatives have been efficiently synthesized in excellent yields via the reaction of naproxenoyl chloride with different amino compounds. Most of the synthesized compounds were screened in vitro for their antibacterial and antifungal activities. Most of the compounds showed significant antibacterial and antifungal activities, reaching, in certain cases, the same level of antimicrobial activity as the standard antibacterial agent Ampicilline and antifungal agent Flucanazole. N-(4-(N-arylsulfamoyl)phenyl)-2-(6-methoxynaphthalen-2-yl)propanamide (4a–c), 4-(4-fluorobenzylidene)-2-(1-(6-methoxynaphthalen-2-yl)ethyl)oxazol-5(4H)-one (10b), 2-(6-methoxynaphthalen-2-yl)-N-((5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl)propanamide (12), and N-((4-amino-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl)-2-(6-methoxynaphthalen-2-yl)propanamide (13) were found to be the most potent compounds against most of the tested strains. The antimicrobial activity was further supported by using MIC technique. Structure activity relationship studies revealed several matching pairs.

Cyanoacetanilides Intermediates in Heterocyclic Synthesis. Part 4: Preparation of Some Hitherto Unknown Thiazolidine and Bisthiazolidine Derivatives

Some novel thiazolidine and bisthiazolidine derivatives were synthesized from the reaction of cyanoacetanilide derivative (2) with isothiocyanates in the presence of potassium hydroxide followed by in situ heterocyclization of the resulting adducts with various α-halogenated reagents.

Overview on the synthetic routes to nicotine nitriles

ABSTRACT The biological and medicinal properties of nicotinonitrile and its analogues have prompted enormous research aimed at developing synthetic routes to these heterocyclic. This review highlights the different synthetic routes to nicotine nitriles. GRAPHICAL ABSTRACT

Diphenic acid derivatives: Synthesis, reactions, and applications

ABSTRACT This review describes the synthesis and reactions of simple diphenic acid derivatives and to highlight the effects of compounds containing the diphenic acid moiety in important applications. GRAPHICAL ABSTRACT

N-Aryl 2-Cyanothioacetamide Intermediates in Heterocyclic Synthesis: Synthesis and AntimicrobialEvaluation of 3-Cyano 2(1H)-Pyridineth-Ione, Chromene-3-Carbothioamide and Chromeno[3,4c]Pyridinethione Derivatives

A novel synthesis of 3-cyano-2(1H)-pyridinethiones, chromene-3-carbothioamide and chromeno[3,4-c]pyridines were obtained through interaction of N-aryl cyanothioacetamide derivatives with some electrophilic reagents. Most of the target compounds were then evaluated for their antimicrobial and antifungal activities.

An overview on synthetic strategies to coumarins

ABSTRACT Coumarins units have recently emerged as a hot topic of research due to their diverse applications. Their synthesis is partly based on classical methodologies such as Pechmann reaction or Knoevenagel condensation, but it also sparked the discovery of completely new pathways. In very recent years so-called vertically expanded coumarins were synthesized, effectively expanding the portfolio of existing architectures. This review serves as a guide through synthesis strategies to coumarins. GRAPHICAL ABSTRACT

Naproxen derivatives: Synthesis, reactions, and biological applications

ABSTRACT This review describes the synthesis and reactions of naproxen derivatives and highlights the effects of compounds containing the naproxen moiety in important biological applications. GRAPHICAL ABSTRACT

Chemistry of 2-cyanomethylene-4-thiazolidinone

ABSTRACT This article is a brief review about the synthesis and chemistry of 2-cyanomethylene-4-thiazolidinone 1. The most significant applications of 4-thiazolidinone 1 in heterocyclic synthesis are due to its two reactive methylenes. The endo-cyclic methylene protons are activated by the neighboring carbonyl moiety and the exo-cyclic methylene protons by the adjacent cyano group. Different types of reactions, such as alkylation, coupling, and Knoevenagel condensation, as well as cyclization reactions are illustrated for the synthesis of different classes of biologically important heterocyclic skeletons from this novel precursor. GRAPHICAL ABSTRACT

Cyanothioacetanilide Intermediates in Heterocyclic Synthesis, Part 1: Synthesis and Biological Evaluation of Some Novel Thiazole, Thiophene, Pyrazole, and Pyrazolo[1,5-a]Pyrimidine Derivatives

Some novel thiophenes (4a,b, 5, and 9a,b) were obtained from the cycloalkylation of the thiocarbamoyl group in the cyanothioacetanilide derivative (1) with α-halocarbonyl compounds. Also, the reaction of cyanothioacetanilide derivative with phenyl isothiocyanate in the presence of potassium hydroxide followed by in situ heterocyclization of the resulting adduct with α-halocarbonyl compounds furnished the corresponding thiazole (12, 14, and 15), pyrazole (19), and pyraozlo[1,5-a]pyrimidine (22, 25, and 26) derivatives. Compounds (4b, 5, 9a, 12, 13, 18, 22, 25, and 26) were tested to evaluate their antimicrobial activity. Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.