Title of article
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
Author/Authors
Stuart W. McCombie، نويسنده , , Jayaram R. Tagat، نويسنده , , Susan F. Vice، نويسنده , , Sue-Ing Lin، نويسنده , , Ruo Steensma، نويسنده , , Anandan Palani، نويسنده , , Bernard R. Neustadt، نويسنده , , Bahige M. Baroudy، نويسنده , , Julie M. Strizki، نويسنده , , Michael Endres، نويسنده , , Kathleen Cox، نويسنده , , Niya Dan، نويسنده , , Chuan-Chu Chou، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
5
From page
567
To page
571
Abstract
The unsymmetrical nicotinamide-N-oxide moiety in compound 1 was replaced with symmetrical isonicotinamides as well as 4,6-dimethyl pyrimidine-5-carboxamides. Compound 16 from the latter set reduced the number of rotamers, improved potency of inhibiting UIV entry, slightly diminished the affinity for the muscarine receptors and showed very good oral absorption.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792967
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