Design and Synthesis of New 1,3,4-Oxadiazole – Benzothiazole and Hydrazone Derivatives as Promising Chemotherapeutic Agents
作者:Betül Kaya、Weiam Hussin、Leyla Yurttaş、Gülhan Turan-Zitouni、Hülya Gençer、Merve Baysal、Abdullah Karaduman、Zafer Kaplancıklı
DOI:10.1055/s-0042-119070
日期:2017.5
Looking for new cytotoxic and antimicrobial agents with improved antitumor activity, a series of hydrazide and oxadiazole derivatives were designed and synthesized using 3-methoxyphenol as starting substance. Novel N'-(arylidene)-2-(3-methoxyphenoxy)acetohydrazide derivatives (4a-f)/1-(4-substitutedphenyl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]ethan-1-one derivatives (6a-f)/N-
为了寻找具有改善的抗肿瘤活性的新的细胞毒性和抗菌剂,以3-甲氧基苯酚为起始原料设计并合成了一系列酰肼和恶二唑衍生物。新的N'-(亚芳基)-2-(3-甲氧基苯氧基)乙酰肼衍生物(4a-f)/ 1-(4-取代的苯基)-2-[(5-[(3-甲氧基苯氧基)甲基] -1,3, 4-恶二唑-2-基)硫]乙烷-1-酮衍生物(6a-f)/ N-(6-取代的苯并噻唑-2-基)-2-[(5-[(3-甲氧基苯氧基)甲基] -1获得了,3,4-恶二唑-2-基)硫代]乙酰胺衍生物(7a-e),并评价了它们对各种革兰氏阳性,革兰氏阴性细菌和真菌的体外抗菌活性。与抗革兰氏阳性细菌的潜力相比,发现该化合物对革兰氏阴性细菌的抗菌潜力更高。还,筛选化合物对作为健康细胞系的两种选定的人类肿瘤细胞系,A549肺,MCF7乳腺癌细胞系和小鼠胚胎成纤维细胞系,NIH / 3T3的抗增殖活性。在所评估的化合物中,与1,3,3,3T3细胞系相反,具有1