Abstract

New hydrazinylidene derivatives were synthesized under appropriate conditions and in excellent yields, by the reaction between a new [1,3]thiazolo[3,2-a]benzimidazol-2(3H)-one substrate and a series of aryldiazonium salts bearing groups with different electronic effect. The structures of the synthesized compounds were verified by FT-IR, ¹H NMR and mass spectra. The pharmacological study including determining antimicrobial activity, cytotoxicity LD50 and histological study for compound ethyl 4-[(2Z)-2-(2-oxo[1,3]thiazolo[3,2-a] benzimidazol-3(2H)-ylidene)hydrazinyl]benzoate have been fulfilled. All chemical and biological result show possibility of using the compound ethyl 4-[(2Z)-2-(2-oxo[1,3]thiazolo[3,2-a] benzimidazol-3(2H)-ylidene)hydrazinyl]benzoate as a new topical antibiotic.

中文翻译：

---

以苯并咪唑为支架的新型肼基衍生物的合成、结构解析及药理研究

摘要

通过新的[1,3]噻唑并[3,2 - a ]苯并咪唑-2(3H)-one底物和一系列带有基团的芳基重氮盐之间的反应，在适当的条件下以优异的收率合成了新的亚肼衍生物。不同的电子效应。合成化合物的结构通过FT-IR、¹ H NMR和质谱进行验证。化合物乙基4-[(2 Z )-2-(2-氧代[1,3]噻唑并[3,2 - a ]苯并咪唑-3(2 H )的药理研究包括抗菌活性测定、细胞毒性LD50和组织学研究-亚基)肼基]苯甲酸酯已得到满足。所有的化学和生物学结果都表明使用化合物乙基 4-[(2 Z)-2-(2-oxo[1,3]thiazolo[3,2 - a ] benzimidazol-3(2 H )-ylidene)hydrazinyl]benzoate 作为一种新的局部抗生素。