Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives

被引：53

作者：

Goncalves, Raoni S. B. ^{[1
,2
]}

Kaiser, Carlos R. ^{[2
]}

Lourenco, Maria C. S. ^{[3
]}

de Souza, Marcus V. N. ^{[1
,2
]}

Wardell, James L. ^{[4
]}

Wardell, Solange M. S. V. ^{[5
]}

da Silva, Adilson D. ^{[6
]}

机构：

[1] FioCruz Fundacao Oswaldo Cruz, Inst Tecnol Farmacos Far Manguinhos, BR-21041250 Rio De Janeiro, Brazil

[2] Univ Fed Rio de Janeiro, Inst Quim, Programa Posgrad Quim, BR-21945970 Rio De Janeiro, Brazil

[3] IPEC, Rio De Janeiro, Brazil

[4] Fiocruz MS, Fundacao Oswald Cruz, CDTS, BR-21040900 Rio De Janeiro, Brazil

[5] CHEMSOL, Aberdeen AB15 5NY, Scotland

[6] Univ Fed Juiz de Fora, Inst Ciencias Exatas, Dept Quim, BR-36036900 Juiz De Fora, MG, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 12期

关键词：

Tuberculosis; Quinoline; Mefloquine; MYCOBACTERIUM-TUBERCULOSIS; FLUOROQUINOLONES;

D O I：

10.1016/j.ejmech.2010.09.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this work, we report the synthesis and the antitubercular evaluation of 16 new mefloquine derivatives, formed from reactions between mefloquine and benzaldehydes, with the activity expressed as the minimum inhibitory concentration (MIC) in mu M. The compounds were non-cytotoxic and exhibited an important activity (12.6 mu M). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti-TB compounds. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：6095 / 6100

页数：6

共 41 条

[1] [Anonymous], ANTIMICROB AGENTS CH
[2] BERMUDEZ LE, 1999, F, V43, P1870
[3] BERMUDEZ LE, 2004, F, V48, P3556
[4] Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives
Candea, Andre L. P.
Ferreira, Marcelle de L.
Pais, Karla C.
Cardoso, Laura N. de F.
Kaiser, Carlos R.
Henriques, Maria Das Gracas M. de O.
Lourenco, Maria C. S.
Bezerra, Flavio A. F.
de Souza, Marcus V. N.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (22) : 6272 - 6274
[5] CANETTI J, 1963, REV TUBERC PNEUMOL, V27, P212
[6] CARVALHO MV, 2006, F, V14, P48
[7] DANELISHVILI L, 2005, F, V49, P3707
[8] 3-[(E)-(7-Chloro-4-quinolyl)hydrazonomethyl]benzonitrile monohydrate
de Ferreira, Marcelle L.
de Souza, Marcus V. N.
Howie, R. Alan
Tiekink, Edward R. T.
Wardell, James L.
Wardell, Solange M. S. V.
[J]. ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2009, 65 : O3239 - U1888
[9] 7-Chloro-4-[(E)-2-(2-methoxybenzylidene)hydrazin-1-yl]quinoline monohydrate
de Souza, Marcus V. N.
Howie, R. Alan
Tiekink, Edward R. T.
Wardell, James L.
Wardell, Solange M. S. V.
Kaiser, Carlos R.
[J]. ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O698 - U5702
[10] 7-Chloro-4-[(E)-N′-(4-fluorobenzylidene)hydrazinyl]quinoline monohydrate
de Souza, Marcus V. N.
Howie, R. Alan
Tiekink, Edward R. T.
Wardell, James L.
Wardell, Solange M. S. V.
[J]. ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O152 - U2413

← 1 2 3 4 5 →