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.
MeSH terms
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Administration, Oral
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Animals
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / pharmacokinetics
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Anti-HIV Agents / pharmacology*
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Area Under Curve
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CCR5 Receptor Antagonists*
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Chemical Phenomena
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Chemistry, Physical
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HIV-1 / drug effects*
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Half-Life
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / pharmacokinetics
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Heterocyclic Compounds / pharmacology
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Humans
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Injections, Intravenous
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Intestinal Absorption
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Molecular Conformation
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Piperazines / chemical synthesis*
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Piperazines / pharmacokinetics
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Piperazines / pharmacology*
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Rats
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Receptors, Muscarinic / drug effects
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Structure-Activity Relationship
Substances
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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Heterocyclic Compounds
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Piperazines
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Receptors, Muscarinic