59777-95-6Relevant articles and documents
AMIDO ANTI-VIRAL COMPOUNDS
-
Page/Page column 75, (2008/12/05)
Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R3, X, V, W, T, Z, R, Y1, and p are as defined herein.
2-(3-pyridyl)thiazolidine-4-carboxamide derivatives. III. Synthesis of metabolites and metabolism of 2-(3-pyridyl)thiazolidine-4-carboxamides YM461 and YM264 as platelet-activating factor (PAF) receptor antagonists
Suzuki, Takeshi,Nagaoka, Hitoshi,Hara, Hiromu,Takeuchi, Makoto,Saito, Munetoshi,Yamada, Toshimitsu,Tomioka, Kenichi,Matsumoto, Hisao,Takanuki, Kenichi,Mase, Toshiyasu
, p. 165 - 170 (2007/10/03)
The metabolism of 2-(3-pyridyl)thiazolidine-4-carboxamides YM4614) and YM2645) was investigated, and their metabolites were compared with separately synthesized materials by measuring 1H-NMR spectra, mass spectra, and HPLC retention times, and evaluated for platelet activating factor (PAF) antagonistic activity. YM461 was metabolized by two different metabolic pathways (cleavage of the thiazolidine ring and oxidation of the benzyl position), whereas YM264 was metabolized by three metabolic pathways. The minor metabolite M7 from YM264 possessed potent PAF antagonistic activity, as strong as YM264 and this existed as an active metabolite. From pharmacokinetics studies, YM264 was almost completely absorbed from the gastrointestinal tract, but readily metabolized in rats. In dogs, pharmacokinetic parameters of YM264 were significantly improved compared to those in rats, and YM264 tended to show better pharmacokinetics than YM461 due to an extension of the half-life period.
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a Novel Series of Platelet Activating Factor Antagonists
Sheppard, George S.,Pireh, Daisy,Carrera, George M.,Bures, Mark G.,Heyman, H. Robin,et al.
, p. 2011 - 2032 (2007/10/02)
(2RS,4R)-3-(2-(3-pyridinyl)thiazolidin-4-oyl)indoles represent a new class of potent, orally active antagonists of platelet activating factor (PAF). The compounds were prepared by acylation of the magnesium or zinc salts of substituted indoles with (2RS,4R)-2-(3-pyridinyl)-3-(tert-butoxycarbonyl)thiazolidin-4-oyl chloride. The 3-acylindole moiety functions as a hydrolytically stabilized and conformationally restricted anilide replacement, which imparts a considerable boost in potency to the series. Structure-activity relationships observed for substitution on the indole ring system are discussed. Members of the series compare favorably with other reported PAF antagonists.