Literature DB >> 14592500

Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.

Nancy J Kevin1, Joseph L Duffy, Brian A Kirk, Kevin T Chapman, William A Schleif, David B Olsen, Mark Stahlhut, Carrie A Rutkowski, Lawrence C Kuo, Lixia Jin, Jiunn H Lin, Emilio A Emini, James R Tata.   

Abstract

HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P(3) position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir to hinder their metabolism by the cyctochrome P450 3A4 isozyme and allow for in vivo PK assessment.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 14592500     DOI: 10.1016/j.bmcl.2003.08.049

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Discovery and optimisation studies of antimalarial phenotypic hits.

Authors:  Alka Mital; Dinakaran Murugesan; Marcel Kaiser; Clive Yeates; Ian H Gilbert
Journal:  Eur J Med Chem       Date:  2015-09-09       Impact factor: 6.514

  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.