Design, Biologic Evaluation, and SAR of Novel Pseudo??peptide Incorporating Benzheterocycles as HIV??1 Protease Inhibitors

…, H Zhang, X Yao, M Eckart, E Zuo…

文献索引：He, Meizi; Zhang, Hang; Yao, Xiaojian; Eckart, Michael; Zuo, Elizabeth; Yang, Ming Chemical Biology and Drug Design, 2010 , vol. 76, # 2 p. 174 - 180

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被引用次数: 7

摘要

A series of novel HIV-1 protease inhibitors based on the (hydroxyethylamino)-sulfonamide isostere incorporating substituted phenyls and benzheterocycle derivatives bearing rich hydrogen bonding acceptors as P 2 ligands were synthesized. Prolonged chain linking the benzhereocycle to the carbonyl group resulted in partial loss of binding affinities. Introduction of a small alkyl substituent with appropriate size to the -CH 2 - of P 1 -P 2 linkage as a side chain resulted in ...