吡喃半乳糖基氨基醇作为一类新型抗结核和抗真菌药物的合成。
Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents.
作者信息
Tewari Neetu, Tiwari V K, Tripathi R P, Chaturvedi V, Srivastava A, Srivastava R, Shukla P K, Chaturvedi A K, Gaikwad A, Sinha S, Srivastava B S
机构信息
Division of Medicinal Chemistry, Central Drug Research Institute, -226001, Lucknow, India.
出版信息
Bioorg Med Chem Lett. 2004 Jan 19;14(2):329-32. doi: 10.1016/j.bmcl.2003.11.020.
The galactopyranosyl amino alcohols (3-16) were synthesised by regioselective oxirane ring opening of compound 2 with variety of amines and screened for antitubercular and antifungal activities. One of the compounds (16) showed potent activity against Mycobacterium tuberculosis H37 Rv in vitro and also displayed activity in MDR TB. The compound (16) was found to be superior to ethambutol clinically used anti TB drug in in vitro screen.
通过化合物2与多种胺进行区域选择性环氧乙烷开环反应合成了吡喃半乳糖基氨基醇（3-16），并对其抗结核和抗真菌活性进行了筛选。其中一种化合物（16）在体外对结核分枝杆菌H37 Rv显示出强效活性，并且在耐多药结核病中也表现出活性。在体外筛选中发现化合物（16）优于临床使用的抗结核药物乙胺丁醇。
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