The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: Part 1

被引:20
|
作者
Cody, WL [1 ]
Cai, CM
Doherty, AM
Edmunds, JJ
He, JX
Narasimhan, LS
Plummer, JS
Rapundalo, ST
Rubin, JR
Van Huis, CA
St-Denis, Y
Winocour, PD
Siddiqui, MA
机构
[1] Div Warner Lambert Co, Parke Davis Pharmaceut Res, Ann Arbor, MI 48105 USA
[2] BioChem Pharma Inc, Laval, PQ H7V 4A7, Canada
关键词
D O I
10.1016/S0960-894X(99)00418-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Utilizing X-ray crystallography and molecular modeling, highly potent and selective peptidomimetic thrombin inhibitors have been designed containing a rigid piperazinedione template. The synthesis and biological activity of these compounds will be described. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2497 / 2502
页数:6
相关论文
共 50 条
  • [31] Design and development of potent and selective factor IXa inhibitors
    Choudhari, Prafulla B.
    Bhatia, Manish S.
    Jadhav, Swapnil D.
    Kumbhar, Santosh S.
    Ingale, Kundan B.
    Gaikwad, Vinod L.
    JOURNAL OF THE TAIWAN INSTITUTE OF CHEMICAL ENGINEERS, 2016, 68 : 130 - 135
  • [32] Potent bicyclic lactam inhibitors of thrombin:: Part I:: P3 modifications
    St-Denis, Y
    Augelli-Szafran, CE
    Bachand, B
    Berryman, KA
    DiMaio, J
    Doherty, AM
    Edmunds, JJ
    Leblond, L
    Lévesque, S
    Narasimhan, LS
    Penvose-Yi, JR
    Rubin, JR
    Tarazi, M
    Winocour, PD
    Siddiqui, MA
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (22) : 3193 - 3198
  • [33] Beyond Heparinization: Design of Highly Potent Thrombin Inhibitors Suitable for Surface Coupling
    Steinmetzer, Torsten
    Baum, Bernhard
    Biela, Adam
    Klebe, Gerhard
    Nowak, Goetz
    Bucha, Elke
    CHEMMEDCHEM, 2012, 7 (11) : 1965 - 1973
  • [34] Multitarget, Selective Compound Design Yields Potent Inhibitors of a Kinetoplastid Pteridine Reductase 1
    Poehner, Ina
    Quotadamo, Antonio
    Panecka-Hofman, Joanna
    Luciani, Rosaria
    Santucci, Matteo
    Linciano, Pasquale
    Landi, Giacomo
    Di Pisa, Flavio
    Dello Iacono, Lucia
    Pozzi, Cecilia
    Mangani, Stefano
    Gul, Sheraz
    Witt, Gesa
    Ellinger, Bernhard
    Kuzikov, Maria
    Santarem, Nuno
    Cordeiro-da-Silva, Anabela
    Costi, Maria P.
    Venturelli, Alberto
    Wade, Rebecca C.
    JOURNAL OF MEDICINAL CHEMISTRY, 2022, 65 (13) : 9011 - 9033
  • [35] Design and synthesis of potent, selective P4-2-alkoxycarbonylbenzylsulfonamide P3-lactam thrombin inhibitors.
    Semple, JE
    Owens, TD
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1998, 216 : U223 - U223
  • [36] NEW SERIES OF SYNTHETIC THROMBIN-INHIBITORS (OM-INHIBITORS) HAVING EXTREMELY POTENT AND SELECTIVE ACTION
    OKAMOTO, S
    HIJIKATA, A
    IKEZAWA, K
    KINJO, K
    KIKUMOTO, R
    TONOMURA, S
    TAMAO, Y
    THROMBOSIS RESEARCH, 1976, 8 : 77 - 82
  • [37] Design, synthesis, and evaluation of potent and selective nNOS inhibitors.
    Gomez-Vidal, JA
    Silverman, RB
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U693 - U693
  • [38] Design of potent and highly selective inhibitors of human tryptase.
    Slusarchyk, WA
    Bisacchi, GS
    Hartl, KS
    Huang, MH
    Jacobs, G
    Ogletree, ML
    Sutton, J
    Treuner, U
    Zhao, GH
    Zahler, R
    Seiler, SM
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 221 : U44 - U44
  • [39] Design of novel nicotinamides as potent and selective monoamine oxidase a inhibitors
    Shi, Lei
    Yang, Ying
    Li, Zi-Lin
    Zhu, Zhen-Wei
    Liu, Chang-Hong
    Zhu, Hai-Liang
    BIOORGANIC & MEDICINAL CHEMISTRY, 2010, 18 (04) : 1659 - 1664
  • [40] Design and synthesis of potent, selective inhibitors of endothelin converting enzyme
    Jeng, AY
    Savage, P
    Chou, M
    Trapani, AJ
    Moliterni, JA
    Moskal, MA
    Neubert, AD
    Marcopulos, N
    Stamford, LB
    Wallace, EM
    NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1998, 358 (01) : R215 - R215