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新型N-取代-2-(4-苯乙炔基-苯基)-1H-苯并咪唑和N-取代-2-[4-(4,4-二甲基硫代色满-6-基-乙炔基)-苯基]-1H-苯并咪唑的合成、抗菌、抗哮喘和抗糖尿病活性

Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.

作者信息

Vinodkumar Ramanatham, Vaidya Sanjay Dashrath, Siva Kumar Bobba Venkata, Bhise Umesh Nanasaheb, Bhirud Shekhar Bhaskar, Mashelkar Uday Chandrakant

机构信息

Glenmark Research Center, Plot No. A-607, T.T.C. Industrial Area, M.I.D.C. Mahape, Navi Mumbai 400 709, India.

出版信息

Eur J Med Chem. 2008 May;43(5):986-95. doi: 10.1016/j.ejmech.2007.06.013. Epub 2007 Jul 10.

Abstract

Synthesis of a series of novel and functionalized benzimidazole derivatives by the condensation of OPDA with 4-bromobenzoic acid and subsequent reactions of the product obtained with phenylacetylene and 6-ethynyl-4,4-dimethylthiochroman utilising Sonogashira coupling has been reported. The Sonogashira coupling products were then alkylated at the benzimidazole -NH with different electrophilic reagents leading to functionalized derivatives. All the compounds synthesized were screened for their potential anti-bacterial, anti-asthmatic and anti-diabetic properties, which exhibited moderate activities in screening studies in vitro.

摘要

据报道,通过OPDA与4-溴苯甲酸缩合,随后利用Sonogashira偶联反应使所得产物与苯乙炔和6-乙炔基-4,4-二甲基硫代色满反应,合成了一系列新型功能化苯并咪唑衍生物。然后,通过用不同的亲电试剂使Sonogashira偶联产物在苯并咪唑-NH处烷基化,得到功能化衍生物。对所有合成的化合物进行了潜在抗菌、抗哮喘和抗糖尿病特性的筛选,这些化合物在体外筛选研究中表现出中等活性。

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