Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1

Autor:	Matthew David Tallant, Wieslaw M. Kazmierski, Pat Wheelan, Maosheng Duan, George Andrew Freeman, Mark P. Edelstein, Robert G. Ferris
Rok vydání:	2011
Předmět:	Benzimidazole Tertiary amine Anti-HIV Agents medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science HIV Infections Carboxamide CCR5 receptor antagonist Biochemistry Chemical synthesis Cell Line Rats Sprague-Dawley Inhibitory Concentration 50 chemistry.chemical_compound Drug Discovery Putrescine medicine Animals Potency Molecular Biology Alkaloid Organic Chemistry Tropane Rats Disease Models Animal chemistry CCR5 Receptor Antagonists HIV-1 Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:1394-1398
ISSN:	0960-894X
Popis:	We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68dbee409884703c0fdfed425864b7bb https://doi.org/10.1016/j.bmcl.2011.01.030 Zobrazit plný text záznamu Full Text from ScienceDirect