Development of new non-peptide GPIIb-IIIa antagnosts, NSL-95315 and NSL-95317, isosteres of NSL-95300

DOI: 10.1016/S0960-894X(97)00366-1

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2099 - 2104 (1997)

Update date:2022-08-04

Topics:

Authors:

Asari, Tohru

Ishikawa, Shigetaka

Sasaki, Toshiki

Katada, Jun

Hayashi, Yoshio

Harada, Takeo

Yano, Mako

Yasuda, Emiko

Uno, Isao

Ojima, Iwao

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Article abstract of DOI:10.1016/S0960-894X(97)00366-1

The synthetic and structure-activity relationship (SAR) studies of new non-peptide GPIIb/IIIa antagonists (1a-f and 3) were conducted by replacing one amide bond of NSL-95300 (2) with an (E)-double bond or an enone group. NSL-95315 (1a) and NSL-95317 (3) showed the inhibitory activity for collagen-induced human platelet aggregation with IC₅₀ values of 0.25 μM and 0.21 μM, respectively.

Full text of DOI:10.1016/S0960-894X(97)00366-1

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