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Qiao, Jennifer X; Wang, Tammy C; Ruel, Réjean; Thibeault, Carl; L’Heureux, Alexandre; Schumacher, William A; Spronk, Steven A; Hiebert, Sheldon; Bouthillier, Gilles; Lloyd, John; Pi, Zulan; Schnur, Dora M; Abell, Lynn M; Hua, Ji; Price, Laura A; Liu, Eddie; Wu, Qimin; Steinbacher, Thomas E; Bostwick, Jeffrey S; Chang, Ming; Zheng, Joanna; Gao, Qi; Ma, Baoqing; McDonnell, Patricia A; Huang, Christine S; Rehfuss, Robert; Wexler, Ruth R; Lam, Patrick Y. S
Journal of medicinal chemistry, 11/2013, Letnik: 56, Številka: 22Journal Article
Preclinical antithrombotic efficacy and bleeding models have demonstrated that P2Y1 antagonists are efficacious as antiplatelet agents and may offer a safety advantage over P2Y12 antagonists in terms of reduced bleeding liabilities. In this article, we describe the structural modification of the tert-butyl phenoxy portion of lead compound 1 and the subsequent discovery of a novel series of conformationally constrained ortho-anilino diaryl ureas. In particular, spiropiperidine indoline-substituted diaryl ureas are described as potent, orally bioavailable small-molecule P2Y1 antagonists with improved activity in functional assays and improved oral bioavailability in rats. Homology modeling and rat PK/PD studies on benchmark compound 3l will also be presented. Compound 3l was our first P2Y1 antagonist to demonstrate a robust oral antithrombotic effect with mild bleeding liability in the rat thrombosis and hemostasis models.
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Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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