Selectivity in the inhibition of HIV and FIV protease: Inhibitory and mechanistic studies of pyrrolidine-containing. alpha.-keto amide and hydroxyethylamine core …

…, IR Ollmann, A Gustchina, J Kervinen…

Index: Slee; Slee, Deborah H.; Laslo; Laslo, Karen L.; Elder; Elder, John H.; Ollmann; Ollmann, Ian R.; Gustchina; Gustchina, Alla; Kervinen; Kervinen, Jukka; Zdanov; Zdanov, Alexander; Wlodawer; Wlodawer, Alexander; Wong; Wong, Chi-Huey Journal of the American Chemical Society, 1995 ,  vol. 117,  # 48  p. 11867 - 11878

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Citation Number: 130

Abstract

Abstract: This paper describes the development of new pyrrolidine-containing a-keto amide and hydroxyethylamine core structures as mechanism based inhibitors of the HIV and FIV proteases. It was found that the a-keto amide core structure 2 is approximately 300-fold better than the corresponding hydroxyethylamine isosteric structure and 1300-fold better than the corresponding phosphinic acid derivative as an inhibitor of the HIV protease. The ...