Kamble Atulkumar, Kamble Ravindra, Dodamani Suneel, Jalalpure Sunil, Rasal Vijaykumar, Kumbar Mahadev, Joshi Shrinivas, Dixit Sheshagiri
Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad, Karnataka, 580003, India.
Dr. Prabhakar Kore Basic Science Research Center, KLE University, Belagavi, Karnataka, 590010, India.
Arch Pharm Res. 2017 Apr;40(4):444-457. doi: 10.1007/s12272-017-0887-0. Epub 2017 Jan 12.
In the present paper 5-[4'-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles (5a-g) and [2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h-q) have been designed and synthesized. These compounds were subjected to docking (against AT receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.
在本论文中，已设计并合成了5-[4'-({4-[(4-芳氧基)甲基]-1H-1,2,3-三唑-1-基}甲基)[1,1'-联苯]-2-基]-1H-四唑（5a - g）和[2'-(1H-四唑-5-基)[1,1'-联苯]-4-基]甲基取代的1-碳二硫代酸酯（11h - q）。对这些化合物进行了对接（针对与赖诺普利复合的AT受体蛋白酶）、体外血管紧张素转换酶抑制、抗增殖、抗炎筛选（通过卵白蛋白变性抑制和红细胞膜稳定测定），最后进行了抗真菌活性分析。其中一些化合物显示出显著的药理特性。
