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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期

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

页码：2497 / 2502

页数：6

共 50 条

[1] The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: Part 2
Cody, WL
Augelli-Szafran, CE
Berryman, KA
Cai, CM
Doherty, AM
Edmunds, JJ
He, JX
Narasimhan, LS
Penvose-Yi, J
Plummer, JS
Rapundalo, ST
Rubin, JR
Van Huis, CA
Leblond, L
Winocour, PD
Siddiqui, MA
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (17) : 2503 - 2508
[2] Design and synthesis of potent and selective macrocyclic thrombin inhibitors
Nantermet, PG
Barrow, JC
Newton, CL
Pellicore, JM
Young, MB
Lewis, SD
Lucas, BJ
Krueger, JA
McMasters, DR
Yan, YW
Kuo, LC
Vacca, JP
Selnick, HG
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (16) : 2781 - 2784
[3] DESIGN AND SYNTHESIS OF POTENT AND HIGHLY SELECTIVE THROMBIN INHIBITORS
HILPERT, K
ACKERMANN, J
BANNER, DW
GAST, A
GUBERNATOR, K
HADVARY, P
LABLER, L
MULLER, K
SCHMID, G
TSCHOPP, TB
VANDEWATERBEEMD, H
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (23) : 3889 - 3901
[4] Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Nantermet, PG
Barrows, JC
Newton, CL
Pellicore, JM
Young, MB
Lewis, SD
Lucas, BJ
Krueger, JA
McMasters, DR
Yan, YW
Kuo, LC
Vacca, J
Selnick, HG
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 225 : U203 - U204
[5] Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Pellicore, JM
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 225 : U214 - U214
[6] The design of potent, selective, non-covalent, peptide thrombin inhibitors utilizing imidazole as a S1 binding element
Wiley, MR
Weir, LC
Briggs, SI
Chirgadze, NY
Clawson, D
Gifford-Moore, DS
Schacht, AL
Smith, GF
Vasudevan, V
Zornes, LL
Klimkowski, VJ
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (18) : 2767 - 2772
[7] Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications
Plummer, JS
Berryman, KA
Cai, C
Cody, WL
DiMaio, J
Doherty, AM
Edmunds, JJ
He, JX
Holland, DR
Levesque, S
Kent, DR
Narasimhan, LS
Rubin, JR
Rapundalo, ST
Siddiqui, MA
Susser, AJ
St-Denis, Y
Winocour, PD
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (23) : 3409 - 3414
[8] Potent and selective bicyclic lactam inhibitors of thrombin:: Part 3:: P1′ modifications
Plummer, JS
Berryman, KA
Cai, CM
Cody, WL
DiMaio, J
Doherty, AM
Eaton, S
Edmunds, JJ
Holland, DR
Lafleur, D
Levesque, S
Narasimhan, LS
Rubin, JR
Rapundalo, T
Siddiqui, MA
Susser, A
St-Denis, Y
Winocour, P
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (06) : 835 - 840
[9] Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: Transition state inhibitors
Bachand, B
Tarazi, M
St-Denis, Y
Edmunds, JJ
Winocour, PD
Leblond, L
Siddiqui, MA
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (03) : 287 - 290
[10] THE DEVELOPMENT OF POTENT AND HIGHLY SELECTIVE THROMBIN INHIBITORS
HILPERT, K
ACKERMANN, J
BANNER, DW
GAST, A
GUBERNATOR, K
SCHMID, G
TSCHOPP, TB
VANDEWATERBEEMD, K
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1995, 30 : S131 - S138

← 1 2 3 4 5 →