6-Carbethoxy-5-(3'-bromophenyl)-3-aryl-2-cyclohexenones 2a-j were obtained from the1-Aryl-3-(3'-bromophenyl)-2-propene-1-ones 1a-j by Micheal addition of ethyl acetoacetate, followed by internal Claisen condensation. Reaction of 2a-j with hydrazine hydrate afforded the corresponding 6-Aryl-4-(3'-bromophenyl)-3-oxo-2,3a,4,5-tetrahydro-2H-indazoles 3a-j. The structures of newly synthesized compou...

Some derivatives of biphenyl-4-carboxylic acid 2-(aryl)-4-oxo-thiazolidin-3-yl –amide were synthesized and studied for their antimicrobial activity. These compounds were prepared from biphenyl-4-carboxylic-acid hydrazides. Biphenyl-4-carboxylic-acid hydrazides 1 on refluxing with aryl aldehydes in the presence of catalytic amount of glacial acetic acid furnish the biphenyl-4-carboxylic acid hyd...

A convenient and general method for the synthesis in 26-73% yields of a new series of 7-alkyl(aryl/heteroaryl)-2-amino-5-trifluoromethyl-1,8-naphthyridines from direct cyclocondensation reactions of 4-alkoxy-1,1,1-trifluoroalk-3-en-2-ones [CF₃C(O)CH=C(R¹)OR, where R¹ = H, Me, Ph, 4-MePh, 4-OMePh, 4-FPh, 4-BrPh, 4-NO₂Ph, 2-furyl, 2-thienyl and R = Me, Et] with 2,6-diaminopyridine (2,6-DAP), unde...

A series of new N ′ -[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine-4-carbohydrazide derivatives were synthesized. Starting from ethyl piperidine-4-carboxylate (a), first ethyl 1-(phenylsulfonyl)piperidine-4-carboxylate (1), second 1-(phenylsulfonyl)piperidine-4-carbohydrazide (2), and finally N ′ -[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine4-carbohydrazides (4a–n) were synthesized...

The clinical relevance: The assessment of the antigenicity of an injectable molecule for the human organism requires human patient sera due to the inherent variability of antibodies from person to person, and the inherent variation of bioactivity of antibodies within a single individual. Antibodies produced experimentally in animals give little information with regard to clinical effects of the...

An alternative strategy for the synthesis of 1-aryl- and 1-alkyl-2-methylsulfanyl-4-(4-fluorophenyl)-5-(pyridin-4-yl)imidazoles as potential p38α mitogen-activated protein kinase inhibitors is reported. The regioselective N-substitution of the imidazole ring was achieved by treatment of α-aminoketones with different aryl or alkyl isothiocyanates. In contrast to previously published synthesis ro...

Sarcoidosis is a multisystemic granulomatous disorder of unknown aetiology typically affecting the lungs and lymph nodes. Less frequently, the kidneys may also be affected. Postmortem analysis suggests that 20 percent of patients have histologic changes in the kidney. However, clinical involvement of the kidney is a relatively uncommon condition. Renal failure may occur associated with hypercal...

Objective(s) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...

Some 5-aryl-2-mercapto-1,3,4-oxadiazole (I) reacted with maleic anhydride, maleic acid and p-benzoquinone affording 2-(5-aryl-1,3,4-oxadiazol-2-ylthio)succinic anhydrides (II), 2-(5-aryl-1,3,4-oxadiazol-2-ylthio)succinic acids (III) and 2-(2,5-dihydroxyphenylthio)-5-aryl-l,3,4-oxadiazoles (IV), respectively. Treatment of 2-methylthio-5-phenyl-l,3-oxadiazole (V) with amines gives 2-[(alkyl or ar...