Studies on Orally Available Inhibitors of HIV Protease. Peptidyl Aldehydes and Trifluoromethyl Ketones-Reference-Cited by-同舟云学术

Studies on Orally Available Inhibitors of HIV Protease. Peptidyl Aldehydes and Trifluoromethyl Ketones

Published:1994-08 Issue:4 Volume:5 Page:257-262
ISSN:2040-2066
Container-title:Antiviral Chemistry and Chemotherapy
language:en
Short-container-title:Antivir Chem Chemother

Author:

Hodge C. N.¹,Aldrich P. E.¹,Fernandez C. H.¹,Otto M. J.²,Rayner M. M.²,Wong Y. N.³,Erickson-Viitanen S.²

Affiliation:

1. Department of Chemical and Physical Sciences, The DuPont Merck Pharmaceutical Co., Wilmington, DE, 19880, USA

2. Department of Virology Research, The DuPont Merck Pharmaceutical Co., Wilmington, DE, 19880, USA

3. Department of Drug Metabolism, The DuPont Merck Pharmaceutical Co., Wilmington, DE, 19880, USA

Abstract

Low-molecular-weight peptidyl aldehyde inhibitors of HIV protease that reach in vivo plasma concentrations after oral administration substantiailly in excess of the antiviral IC90 are described. We also report efforts to improve the potency and stability of these compounds that culminated in a series of peptidyl trifluoromethyl ketones with increased potency but decreased bioavailability.

Publisher

SAGE Publications

Link

http://journals.sagepub.com/doi/pdf/10.1177/095632029400500407

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