The discovery of orally available thrombin inhibitors: Studies towards the optimisation of CGH1668

DOI: 10.1016/S0960-894X(98)00640-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3583 - 3588 (1998)

Update date:2022-08-03

Topics:

Authors:

Ambler, John

Baker, Emma

Brown, Lyndon

Butler, Paul

Farr, Dave

Dunnet, Karen

Le Grand, Darren

Janus, Diana

Jones, Darryl

Menear, Keith

Mercer, Mark

Smith, Garrick

Talbot, Mark

Tweed, Morris

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1016/S0960-894X(98)00640-4

The chemical optimisation of CGH1668 1 is described employing an in vivo model of absorption to determine the influence on bioavailability of single point modifications to five key molecular templates. The discovery of an orally bioavailable and selective thrombin inhibitor, 24, highlights the utility of this approach.

Full text of DOI:10.1016/S0960-894X(98)00640-4

Products guided by the article

Product name:N-[2-(4-Aminophenyl)-1(S)-[4-(2-fluoroethyl)piperidin-1-ylcarbonyl]ethyl]-4-[1(S)-benzyl-2-(4-morpholinyl)ethyl]pyridine-3-sulfonamide

Cas No:200270-65-1

R&D Labs maybe for 200270-65-1

Anhui Hope-Chem Co., Ltd.

Contact:86-551-63540590

Address:No 1388 Furong Rd., Hefei, Anhui, China
Nantong LiKai Chemical Co.,Ltd

Contact:+86-513-89068669

Address:Jincheng Science Park
SHANXI JINJIN CHEMICAL INDUSTRIAL CO.,LTD

website:http://www.jinjingroup.com

Contact:86-574-13989382828

Address:Economic And Technological Development Zone,Hejin?City,Shanxi Province?,China
Jinzhou Jiutai Pharmaceutical Co.,Ltd

Contact:+86-0416-5179890

Address:No.41, Taianli, Taihe District, Jinzhou, Liaoning
Watson International Ltd

Contact:+44 (0)2036089360-31

Address:Chanceryhouse,Chancery Lan

Relevant to this article

An effective aza-michael addition of aromatic amines to electron-deficient alkenes in alkaline Al₂O₃

Doi:10.1016/j.tet.2010.05.054
(2010)
Highly diastereoselective hetero-Diels-Alder reactions of alkenyldihydrooxazoles as an approach to novel pyrimidine derivatives

Doi:10.1039/a705571d
(1997)
Synthesis of N-acetyl derivatives of 5- and 6-ethoxy-2-methylthiobenzimidazole and their cardiotonic activity

Doi:10.1007/BF02291796
(1997)
Doi:10.1021/jm00301a034
(1969)
The Generation and Reactivity of Versatile Ruthenium Carbonyl Organometallic Intermediates by Cluster Photochemistry

Doi:10.1039/DT9950002923
(1995)
Experimental and theoretical studies on the hydrogen-bond-promoted enantioselective hetero-Diels-Alder reaction of Danishefsky's diene with benzaldehyde

Doi:10.1021/jo060129c
(2006)

Article Doi