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

Tohru Asari; Shigetaka Ishikawa; Toshiki Sasaki; Jun Katada; Yoshio Hayashi; Takeo Harada; Mako Yano; Emiko Yasuda; Isao Uno; Iwao Ojima

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

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

Tohru Asari
, Shigetaka Ishikawa
, Toshiki Sasaki
, Jun Katada
, Yoshio Hayashi
, Takeo Harada
, Mako Yano
, Emiko Yasuda
, Isao Uno
, Iwao Ojima

Chemistry

Nippon Steel Corporation

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	2099-2104
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	7
Issue number	16
DOIs	https://doi.org/10.1016/S0960-894X(97)00366-1
State	Published - Aug 19 1997

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

abstract = "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.",

author = "Tohru Asari and Shigetaka Ishikawa and Toshiki Sasaki and Jun Katada and Yoshio Hayashi and Takeo Harada and Mako Yano and Emiko Yasuda and Isao Uno and Iwao Ojima",

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T1 - Development of new non-peptide GPIIb-IIIa antagnosts, NSL-95315 and NSL-95317, isosteres of NSL-95300

AU - Asari, Tohru

AU - Ishikawa, Shigetaka

AU - Sasaki, Toshiki

AU - Katada, Jun

AU - Hayashi, Yoshio

AU - Harada, Takeo

AU - Yano, Mako

AU - Yasuda, Emiko

AU - Uno, Isao

AU - Ojima, Iwao

PY - 1997/8/19

Y1 - 1997/8/19

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/0030739850

U2 - 10.1016/S0960-894X(97)00366-1

DO - 10.1016/S0960-894X(97)00366-1

M3 - Article

AN - SCOPUS:0030739850

SN - 0960-894X

VL - 7

SP - 2099

EP - 2104

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

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

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