… . Synthesis and Biological Activities of Masked Amidines as Prodrugs of 2-[(3S)-4-[(2S)-2-(4-Amidinobenzoylamino)-3-(4-methoxyphenyl) propanoyl]-3-(2-methoxy-2- …

…, T Miyawaki, M Kawamura, Z Terashita…

Index: Kitamura; Fukushi; Miyawaki; Kawamura; Terashita; Naka Chemical and Pharmaceutical Bulletin, 2001 , vol. 49, # 3 p. 268 - 277

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Citation Number: 33

Abstract

To improve the in vivo potency of the potent GPIIb/IIIa antagonist 2-[(3S)-4-[(2S)-2-(4- amidinobenzoylamino)-3-(4-methoxyphenyl) propanoyl]-3-(2-methoxy-2-oxoethyl)-2- oxopiperazinyl] acetic acid (4), the amidino group was converted to an oxadiazole ring, thiadiazole ring or substituted amidoxime group. These groups were expected to be metabolized to an amidino group in vivo. The compounds synthesized were evaluated for ...