Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist.

Administration, Oral Animals Anti-HIV Agents/adverse effects,chemical synthesis,pharmacology Biological Availability Brain/drug effects CCR5 Receptor Antagonists Cation Transport Proteins/drug effects Digestive System/drug effects Ether-A-Go-Go Potassium Channels HIV-1/drug effects,isolation & purification Humans In Vitro Techniques Leukocytes, Mononuclear/drug effects,virology Macaca fascicularis Piperazines/adverse effects,chemical synthesis,chemistry,pharmacology Piperidines/chemical synthesis,chemistry,pharmacology Potassium Channels/drug effects Potassium Channels, Voltage-Gated Pyrimidines/adverse effects,chemical synthesis,chemistry,pharmacology Rats Stereoisomerism Structure-Activity Relationship

Anti-HIV Agents CCR5 Receptor Antagonists Cation Transport Proteins Ether-A-Go-Go Potassium Channels KCNH6 protein, human Piperazines Piperidines Potassium Channels Potassium Channels, Voltage-Gated Pyrimidines vicriviroc