Effect of substituents on diarylmethanes for antitubercular activity

被引:75
作者
Panda, Gautam
Parai, Maloy Kumar
Das, Sajal Kumar
Shagufta
Sinha, Manish
Chaturvedi, Vinita
Srivastava, Anil K.
Manju, Y. S.
Gaikwad, Anil N.
Sinha, Sudhir
机构
[1] Cent Drug Res Inst, Mat & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Microbiol, Lucknow 226001, Uttar Pradesh, India
[3] Cent Drug Res Inst, Drug Target Discovery & Dev Div, Lucknow 226001, Uttar Pradesh, India
关键词
antitubercular agents; diarylmethanes; phenanthrenes;
D O I
10.1016/j.ejmech.2006.09.020
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Aminoalkyl derivatives of diarylmethanes were prepared using Grignard, Friedel-Crafts arylation and aminohydrochloride chain fort-nation reactions. These series of compounds were evaluated against Mycobacterium tuberculosis H37R nu, and showed the activity in the range of 6.25-925 mu g/mL. Effect of heteroaryl, anthracenyl and phenanthrene groups on diarylmethane pharmacophores for antitubercular activity is described. (c) 2006 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:410 / 419
页数:10
相关论文
共 40 条
[1]   A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis [J].
Andries, K ;
Verhasselt, P ;
Guillemont, J ;
Göhlmann, HWH ;
Neefs, JM ;
Winkler, H ;
Van Gestel, J ;
Timmerman, P ;
Zhu, M ;
Lee, E ;
Williams, P ;
de Chaffoy, D ;
Huitric, E ;
Hoffner, S ;
Cambau, E ;
Truffot-Pernot, C ;
Lounis, N ;
Jarlier, V .
SCIENCE, 2005, 307 (5707) :223-227
[2]   New small-molecule synthetic antimycobacterials [J].
Ballell, L ;
Field, RA ;
Duncan, K ;
Young, RJ .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2005, 49 (06) :2153-2163
[3]   Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity [J].
Barbachyn, MR ;
Hutchinson, DK ;
Brickner, SJ ;
Cynamon, MH ;
Kilburn, JO ;
Klemens, SP ;
Glickman, SE ;
Grega, KC ;
Hendges, SK ;
Toops, DS ;
Ford, CW ;
Zurenko, GE .
JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (03) :680-685
[4]   Progress in tuberculosis vaccine development [J].
Baumann, Sven ;
Eddine, Ali Nasser ;
Kaufmann, Stefan H. E. .
CURRENT OPINION IN IMMUNOLOGY, 2006, 18 (04) :438-448
[5]   Selective anti-tubercular purines:: Synthesis and chemotherapeutic properties of 6-aryl- and 6-heteroaryl-9-benzylpurines [J].
Brændvang, M ;
Gundersen, LL .
BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (23) :6360-6373
[6]   Treatment of HIV-related tuberculosis in the era of effective antiretroviral therapy [J].
Burman, WJ ;
Jones, BE .
AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 2001, 164 (01) :7-12
[7]   Microplate Alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium [J].
Collins, LA ;
Franzblau, SG .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (05) :1004-1009
[8]  
COREY A, 1991, CANCER COMMUN, V3, P207
[9]  
de Souza AO, 1999, ARZNEIMITTEL-FORSCH, V49, P1025
[10]  
Dutt AK, 1999, TUBERCULOSIS NONTUBE, P3