Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.


Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
15 08 2020
Historique:
received: 16 12 2019
revised: 21 02 2020
accepted: 28 02 2020
pubmed: 29 4 2020
medline: 29 5 2021
entrez: 29 4 2020
Statut: ppublish

Résumé

A series of 4, 4-disubstituted proline analogs were designed, synthesized, and tested for selective inhibition of blood coagulation factor XIa in search of new non-vitamin K antagonists based oral anticoagulants for potential prevention and treatment of thrombotic diseases. Starting from a potent thrombin (FIIa) inhibitor chemotype with FIIa IC

Identifiants

pubmed: 32340773
pii: S0960-894X(20)30150-5
doi: 10.1016/j.bmcl.2020.127072
pii:
doi:

Substances chimiques

Anticoagulants 0
Proline 9DLQ4CIU6V
Factor XIa EC 3.4.21.27

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

127072

Informations de copyright

Copyright © 2020 Elsevier Ltd. All rights reserved.

Auteurs

Zahid Hussain (Z)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Andrew J Cooke (AJ)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Santhosh Neelamkavil (S)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Lindsay Brown (L)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Emma Carswell (E)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Wayne M Geissler (WM)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Zhuyan Guo (Z)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Brian Hawes (B)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Terri M Kelly (TM)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Yasuko Kiyoi (Y)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

KehDih Lai (K)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Charles Lesburg (C)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Eleanor Pow (E)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Yi Zang (Y)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Harold B Wood (HB)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Scott D Edmondson (SD)

Merck & Co., Inc., Kenilworth, NJ 07033, United States.

Weiguo Liu (W)

Merck & Co., Inc., Kenilworth, NJ 07033, United States. Electronic address: wieguo_liu@merck.com.

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Classifications MeSH