New piperazinyl polyazacyclophane scaffolds, libraries and biological activities

被引：16
作者：
An, HY [1 ]
Haly, BD [1 ]
Cook, PD [1 ]
机构：
[1] ISIS Pharmaceut, Carlsbad, CA 92008 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 17期
关键词：
D O I：
10.1016/S0960-894X(98)00424-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Four novel unsymmetric piperazinyl polyazacyclophane scaffolds 1-4 were synthesized in high yields by an efficient cyclization strategy. Twenty-six libraries 12-37 (total 16000 compounds) were generated by a solution-phase combinatorial approach from 1-4 and thirty-eight functional groups. Potent antibacterial and HIV-1 tat/TAR protein-RNA disrupting activities were discovered. (C) 1998 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2345 / 2350
页数：6
相关论文
共 42 条
[1]   Solution phase combinatorial chemistry .1. Synthesis of polyazacyclophane scaffolds and tertiary amine libraries [J].
An, HY ;
Cook, PD .
TETRAHEDRON LETTERS, 1996, 37 (40) :7233-7236
[2]   Solution phase combinatorial chemistry. Discovery of 13- and 15-membered polyazapyridinocyclophane libraries with antibacterial activity [J].
An, HY ;
Wang, TM ;
Mohan, V ;
Griffey, RH ;
Cook, PD .
TETRAHEDRON, 1998, 54 (16) :3999-4012
[3]   Solution phase combinatorial chemistry. Synthesis of novel linear pyridinopolyamine libraries with potent antibacterial activity [J].
An, HY ;
Haly, BD ;
Fraser, AS ;
Guinosso, CJ ;
Cook, PD .
JOURNAL OF ORGANIC CHEMISTRY, 1997, 62 (15) :5156-5164
[4]   Solution phase combinatorial chemistry. Discovery of novel polyazapyridinophanes with potent antibacterial activity by a solution phase simultaneous addition of functionalities approach [J].
An, HY ;
Cummins, LL ;
Griffey, RH ;
Bharadwaj, R ;
Haly, BD ;
Fraser, AS ;
WilsonLingardo, L ;
Risen, LM ;
Wyatt, JR ;
Cook, PD .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1997, 119 (16) :3696-3708
[5]   Discovery of novel pyridinopolyamines with potent antimicrobial activity: Deconvolution of mixtures synthesized by solution-phase combinatorial chemistry [J].
An, HY ;
Haly, BD ;
Cook, PD .
JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (05) :706-716
[6]  
[Anonymous], ANGEW CHEM INT EDIT, DOI DOI 10.1002/ANIE.199622881
[7]   Multiple-component condensation strategies for combinatorial library synthesis [J].
Armstrong, RW ;
Combs, AP ;
Tempest, PA ;
Brown, SD ;
Keating, TA .
ACCOUNTS OF CHEMICAL RESEARCH, 1996, 29 (03) :123-131
[8]   A convenient procedure for the solution phase preparation of 2-aminothiazole combinatorial libraries [J].
Bailey, N ;
Dean, AW ;
Judd, DB ;
Middlemiss, D ;
Storer, R ;
Watson, SP .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (12) :1409-1414
[9]   Generation of targeted C-2-symmetrical compound libraries by solution-phase combinatorial chemistry [J].
Boger, DL ;
Ozer, RS ;
Andersson, CM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, 7 (14) :1903-1908
[10]   Generalized dipeptidomimetic template: Solution phase parallel synthesis of combinatorial libraries [J].
Boger, DL ;
Tarby, CM ;
Myers, PL ;
Caporale, LH .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (08) :2109-2110
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