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An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798).
Stupple PA, Batchelor DV, Corless M, Dorr PK, Ellis D, Fenwick DR, Galan SR, Jones RM, Mason HJ, Middleton DS, Perros M, Perruccio F, Platts MY, Pryde DC, Rodrigues D, Smith NN, Stephenson PT, Webster R, Westby M, Wood A. Stupple PA, et al. Among authors: dorr pk. J Med Chem. 2011 Jan 13;54(1):67-77. doi: 10.1021/jm100978n. Epub 2010 Dec 3. J Med Chem. 2011. PMID: 21128663
Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity.
Dorr P, Westby M, Dobbs S, Griffin P, Irvine B, Macartney M, Mori J, Rickett G, Smith-Burchnell C, Napier C, Webster R, Armour D, Price D, Stammen B, Wood A, Perros M. Dorr P, et al. Antimicrob Agents Chemother. 2005 Nov;49(11):4721-32. doi: 10.1128/AAC.49.11.4721-4732.2005. Antimicrob Agents Chemother. 2005. PMID: 16251317 Free PMC article.
CCR5 pharmacology methodologies and associated applications.
Mansfield R, Able S, Griffin P, Irvine B, James I, Macartney M, Miller K, Mills J, Napier C, Navratilova I, Perros M, Rickett G, Root H, van der Ryst E, Westby M, Dorr P. Mansfield R, et al. Methods Enzymol. 2009;460:17-55. doi: 10.1016/S0076-6879(09)05202-1. Methods Enzymol. 2009. PMID: 19446719
CCR5 inhibitors in HIV-1 therapy.
Dorr P, Perros M. Dorr P, et al. Expert Opin Drug Discov. 2008 Nov;3(11):1345-61. doi: 10.1517/17460441.3.11.1345. Expert Opin Drug Discov. 2008. PMID: 23496169
18 results