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Fragment-based approach to novel bioactive purine derivatives
Pure and Applied Chemistry ( IF 1.8 ) Pub Date : 2020-09-25 , DOI: 10.1515/pac-2019-1214
Victor P. Krasnov 1, 2 , Galina L. Levit 1 , Vera V. Musiyak 1 , Dmitry A. Gruzdev 1, 2 , Valery N. Charushin 1, 2
Affiliation  

Abstract Using purine as a scaffold, the methods for preparation of novel 2-aminopurine and purine derivatives substituted at position C 6 by the fragments of natural amino acids, short peptides, and N-heterocycles, including enantiopure ones, have been proposed. The methods for determination of the enantiomeric purity of the obtained chiral compounds have been developed. Conjugates exhibiting high antimycobacterial or anti-herpesvirus activity against both laboratory and multidrug-resistant strains were revealed among the obtained compounds.

中文翻译:

基于片段的新型生物活性嘌呤衍生物的方法

摘要 以嘌呤为支架,提出了制备新型 2-氨基嘌呤和 C 6 位被天然氨基酸、短肽和 N-杂环(包括对映体纯)片段取代的嘌呤衍生物的方法。已开发出测定所得手性化合物对映体纯度的方法。在获得的化合物中揭示了对实验室和多重耐药菌株表现出高抗分枝杆菌或抗疱疹病毒活性的缀合物。
更新日期:2020-09-25
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