Literature DB >> 12270193

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.

Christopher L Lynch1, Jeffrey J Hale, Richard J Budhu, Amy L Gentry, Sander G Mills, Kevin T Chapman, Malcolm MacCoss, Lorraine Malkowitz, Martin S Springer, Sandra L Gould, Julie A DeMartino, Salvatore J Siciliano, Margaret A Cascieri, Anthony Carella, Gwen Carver, Karen Holmes, William A Schleif, Renee Danzeisen, Daria Hazuda, Joseph Kessler, Janet Lineberger, Michael Miller, Emilio A Emini.   

Abstract

A series of alpha-(pyrrolidin-1-yl)acetic acids is presented as selective and potent antivirals against HIV. Several of the pyrrolidine zwitterions demonstrated reasonable in vitro properties, enhanced antiviral activities and improved pharmacokinetic profiles over pyrrolidine 1.

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Year:  2002        PMID: 12270193     DOI: 10.1016/s0960-894x(02)00606-6

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


  1 in total

1.  Synthesis and in vitro antimicrobial activity of some pyrazolyl-1-carboxamide derivatives.

Authors:  Essam Mohamed Sharshira; Nagwa Mohamed Mahrous Hamada
Journal:  Molecules       Date:  2011-09-09       Impact factor: 4.411

  1 in total

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