1026430-54-5Relevant articles and documents
Aminodiol HIV protease inhibitors. Synthesis and structure - Activity relationships of P1/P1′ compounds: Correlation between lipophilicity and cytotoxicity
Chen, Ping,Cheng, Peter T. W.,Alam, Masud,Beyer, Barbara D.,Bisacchi, Gregory S.,Dejneka, Tamara,Evans, Adelaide J.,Greytok, Jill A.,Hermsmeier, Mark A.,Humphreys, W. Griffith,Jacobs, Glenn A.,Kocy, Octavian,Lin, Pin-Fang,Lis, Karen A.,Marella, Michael A.,Ryono, Denis E.,Sheaffer, Amy K.,Spergel, Steven H.,Sun, Chong-Qing,Tino, Joseph A.,Vite, Gregory,Colonno, Richard J.,Zahler, Robert,Barrish, Joel C.
, p. 1991 - 2007 (2007/10/03)
A series of novel aminodiol inhibitors of HIV protease based on the lead compound 1 with structural modifications at P1′ were synthesized in order to reduce the cytotoxicity of 1. We have observed a high degree of correlation between the lipophilicity and the cytotoxicity of this series of inhibitors. It was found that appropriate substitution at the para position of the P1′ phenyl group of 1 resulted in the identification of equipotent (both against the enzyme and in cell culture) compounds (101, 10m, 10n, and 15c) which possess significantly decreased cytotoxicity.
AMINO ACIDS AND PEPTIDES. VII. PREPARATION AND APPLICATION OF A WATER-SOLUBLE ACTIVE ESTER, p-TRIMETHYLAMMONIOPHENYL ESTER
Tsuji, Toshiki,Okusada, Satoshi,Maeda, Mitsuko,Kawasaki, Koichi
, p. 2214 - 2217 (2007/10/02)
A water-soluble active ester, p-trimethylammoniophenyl ester iodide, and its nitro derivative were prepared from N-procteted amino acid and the corresponding phenol derivative by the dicyclohexylcarbodiimide method.The synthetic esters were applied to the synthesis of Leuenkephalin.Keywords--water-soluble active ester; p-trimethylammoniophenyl ester iodide; Leuenkephalin; peptide synthesis