Solid phase synthesis of benzylamine-derived sulfonamide library

被引:29
作者
Kim, SW [1 ]
Hong, CY [1 ]
Lee, K [1 ]
Lee, EJ [1 ]
Koh, JS [1 ]
机构
[1] LG Chem Ltd, Biotech Res Inst, Taejon 305380, South Korea
关键词
D O I
10.1016/S0960-894X(98)00114-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Using solid phase synthesis, a library has been constructed of benzylamine-derived sulfonamides which have strong inhibitory activity against the blood coagulant thrombin. The library compounds were obtained in good yield and high purity; four of these thrombin inhibitors showed nanomolar potency (Ki 600-10 nM). (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:735 / 738
页数:4
相关论文
共 25 条
[11]   Rational design of selective thrombin inhibitors [J].
Kim, S ;
Hwang, SY ;
Kim, YK ;
Yun, M ;
Oh, YS .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, 7 (07) :769-774
[12]   Solid phase synthesis of hydantoin library using a novel cyclization and traceless cleavage step [J].
Kim, SW ;
Ahn, SY ;
Koh, JS ;
Lee, JH ;
Ro, S ;
Cho, HY .
TETRAHEDRON LETTERS, 1997, 38 (26) :4603-4606
[13]  
KIM SW, 1998, IN PRESS MOL DIVERSI
[14]   The ''one-bead-one-compound'' combinatorial library method [J].
Lam, KS ;
Lebl, M ;
Krchnak, V .
CHEMICAL REVIEWS, 1997, 97 (02) :411-448
[15]   The current status of heterocyclic combinatorial libraries [J].
Nefzi, A ;
Ostresh, JM ;
Houghten, RA .
CHEMICAL REVIEWS, 1997, 97 (02) :449-472
[16]  
OH YS, 1996, Patent No. 739886
[17]   SOLID-PHASE SYNTHESIS OF STRUCTURALLY DIVERSE 1,4-BENZODIAZEPINE DERIVATIVES USING THE STILLE COUPLING REACTION [J].
PLUNKETT, MJ ;
ELLMAN, JA .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (11) :3306-3307
[18]   A linker for amidines in solid phase synthesis [J].
Roussel, P ;
Bradley, M ;
Matthews, I ;
Kane, P .
TETRAHEDRON LETTERS, 1997, 38 (27) :4861-4864
[19]   Discovery of sequence-selective peptide binding by synthetic receptors using encoded combinatorial libraries [J].
Still, WC .
ACCOUNTS OF CHEMICAL RESEARCH, 1996, 29 (03) :155-163
[20]   THROMBIN INHIBITORS - A NEW-GENERATION OF ANTITHROMBOTICS [J].
STONE, SR .
TRENDS IN CARDIOVASCULAR MEDICINE, 1995, 5 (04) :134-140