acetamido]thio-4H-1,2,4-triazole Derivatives. -Triazoles incorporating a thiazole ring system, and additionally in some cases an ester residue, are synthesized and evaluated for antifungal and antibactrial activity. Five triazolinethiones (V) and fifteen new thioether derivatives of (V) are prepared. Thiotriazoles are more active than their thioether derivatives, especially the tolyloxy derivatives (Vb) and (Ve), the triazoles are more active towards fungi than bacteria. The antibacterial assessment reveals only a slight or moderate activity. -(TURAN-ZITOUNI*, G.; KAPLANCIKLI, Z. A.; YILDIZ, M. T.; CHEVALLET, P.; KAYA, D.; Eur. J. Med. Chem. 40 (2005) 6, 607-613; Dep. Pharm. Chem., Fac. Pharm., Anadolu Univ., TR-26470 Eskisehir, Turk.; Eng.) -H. Hoennerscheid 42-147
thioacetylamino]thiazole Derivatives and Their Antimicrobial Activity and Toxicity. -All compounds tested show significant antifungal activity against C. albicans. The only non-toxic derivative (IIIe) is one of the most effective compounds against C. albicans and bacteria. -(TURAN-ZITOUNI*, G.; DEMIRAYAK, S.; OEZDEMIR, A.; KAPLANCIKLI, Z. A.; YILDIZ, M. T.; Eur.
The increasing clinical importance of drug-resistant fungal and bacterial pathogens has lent additional urgency to microbiological research and new antibacterial compound development. For this purpose, new tert-butyl[1-benzyl-2[(4-aryl-2-thiazolyl)hydrazono]ethyl]carbamate derivatives were synthesized and evaluated for antibacterial activity. The reaction of Boc-L-phenylalaninal with thiosemicarbazide gave the thiosemicarbazone which furnished the title compounds by reaction with phenacyl bromides. The newly synthesized compounds were screened for antibacterial activity and toxicity. While microdilution broth susceptibility assay was used for the antibacterial activity evaluation of the compounds against the strains E. coli (NRRL B-3704), M. luteus (NRRL B-4375), B. cereus (NRRL B-3711), P. aeruginosa (NRRL B-23), and S. fecalis (NRRL B-14617), the Artemia salina 96-well assay was used to determine cytotoxicities of the compounds. Observations obtained from the bioassays showed that some of the compounds are highly active against E. coli, M. luteus, and B. cereus when compared with the control agent and showed low toxicity.
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