Structure–activity relationship of HIV-1 protease inhibitors containing α-hydroxy-β-amino acids. Detailed study of P 1 site

…, Y Ozawa, R Yagi, I Yamamoto, T Shibayama…

Index: Takashiro, Eiji; Hayakawa, Ichiro; Nitta, Tamayo; Kasuya, Atsushi; Miyamoto, Shuichi; Ozawa, Yuji; Yagi, Ryuichi; Yamamoto, Ikue; Shibayama, Takahiro; Nakagawa, Akihiko; Yabe, Yuichiro Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 9 p. 2063 - 2072

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Citation Number: 45

Abstract

The structure–activity relationship of HIV-1 protease (HIV-1 PR) inhibitors containing α- hydroxy-β-amino acids is discussed. We demonstrated that substituent groups on the P1 aromatic rings of the inhibitors exert significant influence on their biological activity. Inhibitors bearing an alkyl or a fluorine atom at the meta and para position on their P1 benzene ring were found to be good inhibitors. We also discovered that the substitution positions of the ...