Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors

被引：15

作者：

Powell, NA ^{[1
]}

Clay, EH ^{[1
]}

Holsworth, DD ^{[1
]}

Bryant, JW ^{[1
]}

Ryan, MJ ^{[1
]}

Jalaie, M ^{[1
]}

Edmunds, JJ ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Michigan Labs, Ann Arbor, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期

关键词：

renin inhibitor; hypertension; topliss tree;

D O I：

10.1016/j.bmcl.2005.07.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of renin enzymatic activity by a series of ketopiperazine-based compounds containing a C6 benzyloxymethyl substituent correlated with a +(pi + sigma) effect. A 3-pyridinyloxymethyl substituent was also found to be equipotent as higher molecular weight analogs, and exhibited decreased CYP3A4 inhibition levels and improved pharmacokinetic properties. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4713 / 4716

页数：4

共 50 条

[1] Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors
Powell, NA
Clay, EH
Holsworth, DD
Bryant, JW
Ryan, MJ
Jalaie, M
Zhang, E
Edmunds, JJ
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (09) : 2371 - 2374
[2] Ketopiperazine-based renin inhibitors: Optimization of the "C" ring
Holsworth, DD
Cai, CM
Cheng, XM
Cody, WL
Downing, DM
Erasga, N
Lee, C
Powell, NA
Edmunds, JJ
Stier, M
Jalaie, M
Zhang, EL
McConnell, P
Ryan, MJ
Bryant, J
Li, TS
Kasani, A
Hall, E
Subedi, R
Rahim, M
Maiti, S
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (09) : 2500 - 2504
[3] Ketopiperazine-based renin inhibitors. 4. SAR of C ring benzyl ethers.
Powell, NA
Clay, E
Holsworth, DD
Jalaie, M
Bryant, J
Ryan, M
Li, TS
Karsana, A
Maiti, S
Edmunds, JJ
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2004, 228 : U957 - U957
[4] Discovery of novel non-peptidic ketopiperazine-based renin inhibitors
Holsworth, DD
Powell, NA
Downing, DM
Cai, C
Cody, WL
Ryan, JM
Ostroski, R
Jalaie, M
Bryant, JW
Edmunds, JJ
[J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (07) : 2657 - 2664
[5] Ketopiperazine-based renin inhibitors - 2. Optimization of the "C" ring.
Powell, NA
Holsworth, DD
Cody, WL
Cheng, XM
Lee, C
Erasga, N
Downing, DM
Cai, CM
Clay, E
Jalaie, M
Zhang, EL
Bryant, J
Ryan, M
Edmunds, JJ
Li, TS
Kasani, A
Hai, E
Subedi, R
Rahim, M
Maiti, S
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2004, 228 : U956 - U956
[6] Ketopiperazine-based renin inhibitors: Optimization of the "C" ring: Incorporation of indole rings
Cai, Cuiman
Bryant, John
Cheng, Xue Min
Cody, Wayne L.
Collard, Wendy
Downing, Dennis M.
Erasga, Noe
Ferreira, Suzie
Hall, Eric
Holsworth, Daniel D.
Jalaie, Mehran
Kasani, Aparna
Lee, Chitase
Li, Tingsheng
Maiti, Samarendra
McConnell, Patrick
Powell, Noel A.
Rahim, Mohammad
Ryan, Michael
Stier, Michael A.
Subedi, Rajandra
Zhang, Erli
Edmunds, Jeremy J.
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2006, 231
[7] Quantitative Structure-Activity Relationships of Renin Inhibitors
Gupta, Satya P.
[J]. MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2003, 3 (04) : 315 - 321
[8] Ketopiperazine-based renin inhibitors. 3. The S-enantiomer is also active.
Powell, NA
Clay, E
Ciske, FL
Holsworth, DD
Lee, C
Jalaie, M
Bryant, J
Ryan, M
Edmunds, JJ
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2004, 228 : U957 - U957
[9] Structure- and Ligand-Based Structure-Activity Relationships for a Series of Inhibitors of Aldolase
Ferreira, Leonardo G.
Andricopulo, Adriano D.
[J]. CURRENT COMPUTER-AIDED DRUG DESIGN, 2012, 8 (04) : 309 - 316
[10] STRUCTURE-ACTIVITY RELATIONSHIPS FOR BENZYL ALCOHOLS
TINLAND, B
[J]. RESEARCH COMMUNICATIONS IN CHEMICAL PATHOLOGY AND PHARMACOLOGY, 1973, 5 (03): : 855 - 857

← 1 2 3 4 5 →