Synthesis of Dipeptide-Type Human Immunodeficiency Virus (HIV) Protease Inhibitors with a Binding Unit to GP120
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概要
- 論文の詳細を見る
Some dipeptide-type human immunodeficiency virus (HIV) protease inhibitors derived from KNI-102,with a N-carbomethoxycarbonylprolyl-phenylalanine benzyl ester (CPF) moiety as a binding site to gp120,were synthesized. Compounds 11a showed 7-100 times higher HIV protease-inhibitory activity (11a; IC_<50>=0.90 μg/ml, 1.1 μM) than the standard compound 3 or 4 (3; IC_<50>=3.7 μg/ml, 7.7 μM, 4; IC_<50>=75 μg/ml, 155 μM). Generally, the compounds substituted at the o-position of the phenoxyacetyl group 7a, 11a, 16a and 12a showed several times higher inhibitory activity than 3.
- 公益社団法人日本薬学会の論文
- 1998-05-15
著者
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Achiwa Kazuo
School Of Pharmaceutical Sciences University Of Shizuoka
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ASAGARASU Akira
School of Pharmaceutical Sciences, University of Shizuoka
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TAKAYANAGI Nao
School of Pharmaceutical Sciences, University of Shizuoka
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Takayanagi Nao
School Of Pharmaceutical Sciences University Of Shizuoka
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Asagarasu Akira
School Of Pharmaceutical Sciences University Of Shizuoka
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