Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors
Y St-Denis, S Lévesque, B Bachand…
Index: St-Denis, Yves; Levesque, Sophie; Bachand, Benoit; Edmunds, Jeremy J.; Leblond, Lorraine; Preville, Patrice; Tarazi, Micheline; Winocour, Peter D.; Siddiqui, M. Arshad Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 8 p. 1181 - 1184
Full Text: HTML
Citation Number: 14
Abstract
The potency and selectivity of a previous series of low molecular weight thrombin inhibitors were improved through modifications of the P1 and P3 residues. Introduction of diphenyl substituted sulfonamides in the P3 moiety led to highly efficacious compounds. By correctly selecting the combination of P1 and P3 residues, high levels of potency, selectivity and in vivo efficacy were obtained.
Related Articles:
[Mori, Mattia; Massaro, Assunta; Calderone, Vito; Fragai, Marco; Luchinat, Claudio; Mordini, Alessandro ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 6 p. 565 - 569]
[Sohmiya, Hajime; Kimura, Takahide; Fujita, Mitsue; Ando, Takashi Tetrahedron, 1998 , vol. 54, # 45 p. 13737 - 13750]
[Mori, Mattia; Massaro, Assunta; Calderone, Vito; Fragai, Marco; Luchinat, Claudio; Mordini, Alessandro ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 6 p. 565 - 569]
[Mori, Mattia; Massaro, Assunta; Calderone, Vito; Fragai, Marco; Luchinat, Claudio; Mordini, Alessandro ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 6 p. 565 - 569]
Mechanisms in the chlorinolysis of sulfinyl chlorides
[Ahern, Terence Patrick; Haley, Michael Francis; Langler, Richard Francis; Trenholm, June Ellen Canadian Journal of Chemistry, 1984 , vol. 62, p. 610 - 614]