Literature DB >> 11591514

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.

J J Hale1, R J Budhu, E B Holson, P E Finke, B Oates, S G Mills, M MacCoss, S L Gould, J A DeMartino, M S Springer, S Siciliano, L Malkowitz, W A Schleif, D Hazuda, M Miller, J Kessler, R Danzeisen, K Holmes, J Lineberger, A Carella, G Carver, E Emini.   

Abstract

Investigations of the structure-activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable compounds with the ability to inhibit HIV replication in vitro.

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Year:  2001        PMID： 11591514     DOI： 10.1016/s0960-894x(01)00545-5

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


  6 in total

1.  Inhibition of human immunodeficiency virus envelope glycoprotein- mediated single cell lysis by low-molecular-weight antagonists of viral entry.

Authors:  Navid Madani; Amy M Hubicki; Ana Luisa Perdigoto; Martin Springer; Joseph Sodroski
Journal:  J Virol       Date:  2006-08-30       Impact factor: 5.103

2.  Antibody binding in proximity to the receptor/glycoprotein complex leads to a basal level of virus neutralization.

Authors:  Xinzhen Yang; Inna Lipchina; Michelle Lifton; Liping Wang; Joseph Sodroski
Journal:  J Virol       Date:  2007-05-30       Impact factor: 5.103

Review 3.  Structural Analysis of Chemokine Receptor-Ligand Interactions.

Authors:  Marta Arimont; Shan-Liang Sun; Rob Leurs; Martine Smit; Iwan J P de Esch; Chris de Graaf
Journal:  J Med Chem       Date:  2017-03-10       Impact factor: 7.446

Review 4.  HIV entry inhibitors and their potential in HIV therapy.

Authors:  Keduo Qian; Susan L Morris-Natschke; Kuo-Hsiung Lee
Journal:  Med Res Rev       Date:  2009-03       Impact factor: 12.944

5.  Discovery of Novel CCR5 Ligands as Anticolorectal Cancer Agents by Sequential Virtual Screening.

Authors:  Mariam A El-Zohairy; Darius P Zlotos; Martin R Berger; Hassan H Adwan; Yasmine M Mandour
Journal:  ACS Omega       Date:  2021-04-16

6.  Soluble CD4 and CD4-mimetic compounds inhibit HIV-1 infection by induction of a short-lived activated state.

Authors:  Hillel Haim; Zhihai Si; Navid Madani; Liping Wang; Joel R Courter; Amy Princiotto; Aemro Kassa; Marciella DeGrace; Kathleen McGee-Estrada; Megan Mefford; Dana Gabuzda; Amos B Smith; Joseph Sodroski
Journal:  PLoS Pathog       Date:  2009-04-03       Impact factor: 6.823
  6 in total

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