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2004
Multi-membered N-heterocycles
R 0690
Orally Active CCR5 Antagonists as anti-HIV-1 Agents. Part 2. Synthesis and BioActivities of Anilide Derivatives Containing a Pyridine N-Oxide Moiety.
51- 140 logical
— A series of benzoxepine derivatives of type (III) and (X) is prepared as potential
orally active CCR5 antagonists. Some of the compounds are resolved into their enantiomers. The (S)-enantiomer of (X) shows the most potent CCR5 antagonist activity
and inhibitory effect in the fusion assay, together with good pharmacokinetic properties
in rats. — (SETO*, M.; ARAMAKI, Y.; IMOTO, H.; AIKAWA, K.; ODA, T.;
KANZAKI, N.; IIZAWA, Y.; BABA, M.; SHIRAISHI, M.; Chem. Pharm. Bull. 52
(2004) 7, 818-829; Med. Chem. Lab., Takeda Chem. Ind., Ltd., Yodogawa, Osaka 532,
Japan; Eng.) — M. Bohle
2004
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