Synthesis, antimycobacterial activities and cytotoxicity on V79 of 3-[4′-Y-(1,1′-biphenyl)-4-yl]-N,N-dimethyl-3-(4-X-phenyl)-2-propen-1-amine derivatives

被引:10
作者
de Souza, AO
Junior, RRS
Ferreira-Júlio, JF
Rodriguez, JA
Melo, PS
Haun, M
Sato, DN
Durán, N
机构
[1] Univ Estadual Campinas, Inst Quim, Biol Chem Lab, BR-13083970 Campinas, SP, Brazil
[2] Inst Adolfo Lutz Registro, Ribeirao Preto, Brazil
[3] Univ Talca, Talca, Chile
[4] Univ Estadual Campinas, Inst Biol, Cell Culture Lab, Campinas, SP, Brazil
[5] Univ Mogi Cruzes, NCA, Mogi Das Cruzes, SP, Brazil
关键词
synthesis; cytotoxicity; V79; cells; antimycobacterial activity; 2-propen-1-amine;
D O I
10.1016/S0223-5234(01)01263-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The derivatives of 3-(4'-bromo-[1,1'-biphenyl]-4-yl)-3-(4-X-phenyl)-N,N-dimethyl-2-propen-1-amine (5a-m) were synthesised through a Friedel-Crafts acylation followed by Wittig reaction. The effects of the compounds on standard strains or Mycobacterium sp. (ATCC) and V. tuberculosis isolated from clinical specimens were evaluated. Also the toxicity was determined on V79 cells line using neutral red uptake (NRU), nucleic acid content (NAC) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction to measure the cellular viability. (C) 2001 Editions scientifiques et medicales Elsevier SAS.
引用
收藏
页码:843 / 850
页数:8
相关论文
共 20 条
[1]  
Bleed D, 2000, WHOCDSTB2000275, P1
[2]  
Borenfreund E., 1984, J. Tissue Cult. Methods, V9, P7, DOI [10.1007/BF01666038, DOI 10.1007/BF01666038]
[3]   CHOICE AND STANDARDIZATION OF TEST PROTOCOLS IN CYTOTOXICOLOGY - A MULTICENTER APPROACH [J].
CINGI, MR ;
DEANGELIS, I ;
FORTUNATI, E ;
REGGIANI, D ;
BIANCHI, V ;
TIOZZO, R ;
ZUCCO, F .
TOXICOLOGY IN VITRO, 1991, 5 (02) :119-125
[5]   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
[6]  
De Conti R, 1998, IN VITRO MOL TOXICOL, V11, P153
[7]   In-vitro activity of N,N-dimethyl-2-propen-1-amines against Mycobacterium tuberculosis [J].
De Souza, AO ;
Aily, DCG ;
Sato, DN ;
Durán, N .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1998, 42 (03) :407-408
[8]  
DeConti R, 1996, MICROBIOS, V85, P83
[9]  
DECONTI R, 1996, EUR J MED CHEM, V31, P1
[10]   RAPID COLORIMETRIC ASSAY FOR CELL-GROWTH AND SURVIVAL - MODIFICATIONS TO THE TETRAZOLIUM DYE PROCEDURE GIVING IMPROVED SENSITIVITY AND RELIABILITY [J].
DENIZOT, F ;
LANG, R .
JOURNAL OF IMMUNOLOGICAL METHODS, 1986, 89 (02) :271-277