Bioorganic and Medicinal Chemistry Letters p. 1531 - 1536 (1998)
Update date:2022-08-04
Topics: Selectivity Clinical Trials Lead Optimization Regulatory Approval Toxicity and Safety Assessment Toxicity and Safety Formulation Functional Group Introduction Lipophilicity and Solubility Metabolic Stability Phenylpiperazine Scaffold Bioisosteric Replacement Synthesis of the Phenylpiperazine Core Scale-Up and Preclinical Testing
Van Maarseveen, Jan H.
Den Hartog, Jack A.J.
Tipker, Koos
Reinders, Jan-Hendrik
Brakkee, Joost
Schoen, Uwe
Kehrbach, Wolfgang
Kruse, Chris G.
The design and synthesis of an orally active LMW non-peptide GPIIb/IIIa antagonist, based on a N,N'-bisphenylpiperazine scaffold, is described. The optimal compound showed a high in vitro binding potency (pIC50=8.7) in combination with potent oral antithrombotic activity (30-40% inhibition of thrombus growth at 0.3-3 mg/kg) with a duration of action of >90 min. in a hamster cheek pouch model.
View MoreJIAXING SUNS INTERNATIONAL TRADE CO LTD
Contact:18367306858
Address:No.123,Huixin Avenue,Huimin Dist
Shao Xing Empire Import&Export CO.,ltd
Contact:86-575-82127757
Address:11#, Weiwu Road, Shangyu Industrial Park, Hangzhou Bay, Hangzhou, Zhejiang Province, China
Shanghai Bocimed Pharmaceutical Co., Ltd.
website:http://www.bocimed.com
Contact:+86-21-68861632
Address:Building 1, Lane 647, Songtao Road, Zhangjiang High-Tech Park, Shanghai
Tianjin Chemsyntech Chemical Co., Ltd
Contact:+86-22-60872258
Address:Haitai green industry base in Tianjin, K1,5-601
website:http://www.sigmaaldrich.com
Contact:800 558-9160
Address:Industriestrasse 25CH-9471 Buchs SGSwitzerland
Doi:10.1021/ja711120r
(2008)Doi:10.1002/1099-0690(200107)2001:13<2535::AID-EJOC2535>3.0.CO;2-V
(2001)Doi:10.1039/b101312m
(2001)Doi:10.1021/jm00268a004
(1973)Doi:10.1021/jo00235a005
(1987)Doi:10.1021/acs.orglett.0c02294
(2020)