… . 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…

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

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被引用次数: 33

摘要

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 ...