This study is concerned with the synthesis of new 1,2,4-triazoles, 1,3,4-thiadiazoles, and 1,3,4-thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole 1 with the appropriate aldehyde. Compounds 4a-i were synthesized in a one pot reaction involving compounds 3a-i, formaldehyde, and morpholine. Condensation of compound 1 with the appropriate acids or 4-substituted phenacyl bromide gave compounds 6a-d and 8a-f respectively. The chemical structures of the newly synthesized derivatives were elucidated using different spectral and elemental methods of analysis. All compounds were evaluated for their anti-inflammatory activity and the most potent derivatives were tested for their analgesic activity using indomethacin as a reference drug. In addition, ulcerogenicity and LD(50) for the most active compounds were evaluated. Moreover, the antibacterial activities of the newly synthesized derivatives were investigated.
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1,4-Disubstituted thiosemicarbazides
1b-f reacted with ethenetetracarbonitrile (5) in dimethylformamide with formation of 2-substituted 5-phenyl-1,3,4-thiadiazoles 2a-f and 2-substituted 5-phenyl-1,3,4-oxadiazoles 4a-f. Upon addition of 5 to 1c-e in
The synthesis and reactions of 5-aminouracil and its derivatives are comprehensively reviewed. A brief survey of biological activities, especially chemotherapeutic and pharmacological properties, is also reported.
Phenyl isothiocyanate reacts with 2-cyanoacetohydrazide (1) to yield the corresponding 1-cyanoacetyl-4-phenylthiosemicarbazide (3), via acid hydrolysis of the intermediate 2 whereas cyclization of 3 gave the 1,2,4-triazoles 4, 1,3,4thiadiazoles 7 and 1,3,4-thiadiazine-5-ones 9; compound 4a was reacted with phenyl isothiocyanate, dicyandiamide, sulfanylacetic acid and benzaldehyde to afford 11, 13, 14 and 15, respectively.
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