New platelet fibrinogen receptor glycoprotein IIb-IIIa antagonists: Orally active series of N-alkylated amidines with a 6, 6-bicyclic template

…, Y Aoki, H Yamashita, E Tanaka, S Banba…

Index: Okumura, Kunio; Shimazaki, Toshiyuki; Aoki, Yoji; Yamashita, Hiroyuki; Tanaka, Eishi; Banba, Shinichi; Yazawa, Kouhei; Kibayashi, Kenji; Banno, Hitoshi Journal of Medicinal Chemistry, 1998 , vol. 41, # 21 p. 4036 - 4052

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Citation Number: 33

Abstract

The design, synthesis, and pharmacological evaluation of (S)-(-)-ethyl [6-[4-( morpholinoformimidoyl) benzamido]-3, 4-dihydro-2 H-1-benzopyran-3-yl] acetate hydrochloride ((S)-4⊙ HCl, MS-180), an orally active glycoprotein IIb-IIIa (GPIIb-IIIa) antagonist, are reported. Pharmacophore mapping of amidino and carboxyl groups of already known GPIIb-IIIa antagonists led to the synthesis of nine amidino acids containing ...