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

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Tallant MD,Duan M,Freeman GA,Ferris RG,Edelstein MP,Kazmierski WM,Wheelan PJ

doi

10.1016/j.bmcl.2011.01.030

subject

Has Abstract

pub_date

2011-03-01 00:00:00

pages

1394-8

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00043-6

journal_volume

21

pub_type

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