A Facile Protocol for Synthesis of Some Novel 2-phenethyl-1H-benzimidazole Derivatives and Screening of In-Vitro Anti-inflammatory and Antimicrobial Activities

R. Shastri, S. Jadhav
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Abstract

: A convenient and efficient method for the preparation of some novel 2-phenethyl-1 H benzimidazole derivatives (4a-h) has been achieved by the condensation of phenyl propionic acids (2a-h) with o -phenylenediamine (3) in POCl 3 . The advantages of this method is excellent yields, short reaction time, no side reaction and operational simplicity and ease product isolation The structure of all the synthesized compounds were characterized by FT-IR, 1 H NMR and MS data. Furthermore, compounds (4a-h) were screened for their antibacterial activity against gram negative ( E. coli ) and gram positive ( B.subtilis ) bacteria, antifungal activity against Aspergillusniger and Penicillium chrysogenum and anti-inflammatory activities. Some of the compounds exhibited promising antibacterial, antifungal and anti-inflammatory activities.
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一些新型2-苯乙基- 1h -苯并咪唑衍生物的合成及体外抗炎和抗菌活性筛选的简易方案
采用苯基丙酸(2a-h)与邻苯二胺(3)在POCl - 3中缩合的方法,制备了一种简便、高效的新型2-苯乙基-1 H苯并咪唑衍生物(4a-h)。该方法具有收率高、反应时间短、无副反应、操作简单、易于分离等优点。所有合成化合物的结构均通过FT-IR、1h NMR和MS数据进行了表征。此外,筛选化合物(4a-h)对革兰氏阴性(大肠杆菌)和革兰氏阳性(枯草芽孢杆菌)的抑菌活性,对黑曲霉和青霉菌的抑菌活性和抗炎活性。其中一些化合物具有良好的抗菌、抗真菌和抗炎活性。
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