Fungicide Activity of 5-(4-Chlorobenzylidene)-(Z)-2-dimethylamino-1,3-thiazol-4-one against Cryptococcus Neoformans

被引：12

作者：

Insuasty, Braulio ^{[1
]}

Gutierrez, Alexander ^{[2
]}

Quiroga, Jairo ^{[1
]}

Abonia, Rodrigo ^{[1
]}

Nogueras, Manuel ^{[3
]}

Cobo, Justo ^{[3
]}

Svetaz, Laura ^{[4
]}

Raimondi, Marcela ^{[4
]}

Zacchino, Susana ^{[4
]}

机构：

[1] Univ Valle, Dept Quim, Grp Invest Compuestos Heterocicl, Cali 25360, Colombia

[2] Univ Tecnol Choco, Dept Biol & Chem, Quibdo, Colombia

[3] Univ Jaen, Dept Inorgan & Organ Chem, Jaen, Spain

[4] Univ Nacl Rosario, Fac Biochem & Pharmaceut Sci, RA-2000 Rosario, Santa Fe, Argentina

来源：

ARCHIV DER PHARMAZIE | 2010年 / 343卷 / 01期

关键词：

Antifungal activity; 5-Arylidenerhodanines; Cryptococcus neoformans; Dimethylamino-5-arylidene[1,3]-thiazol-4-one; ANTIFUNGAL; INHIBITORS; IDENTIFICATION; MICRODILUTION; EPIDEMIOLOGY; RESISTANCE;

D O I：

10.1002/ardp.200900187

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes using the microbroth dilution method. Compounds 4a and 4c showed antifungal activity, with compound 4a being the most active one. Compound 4a demonstrated to be fungicidal rather than fungistatic and selective activity against Cryptococcus neoformans and dermatophytes. MIC100, MIC80, and MIC50 of 4a were determined against a panel of clinical isolates of C. neoformans showing ranges of MICs between 2 and 16 mu g/mL.

引用

页码：48 / 53

页数：6

共 36 条

[1] Abdel-Halim A.M., 1994, INDIAN J HETROCYCLIC, V4, P45
[2] ABDELGHANI E, 1999, J CHEM RES SYNOP, V3, P174
[3] Synthesis and cardiotonic activity of imidazo[2,1-b]thiazoles bearing a lactam ring
Andreani, A
Rambaldi, M
Leoni, A
Locatelli, A
Bossa, R
Chiericozzi, M
Galatulas, I
Salvatore, G
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1996, 31 (05) : 383 - 387
[4] SYNTHESIS OF LACTAMS WITH POTENTIAL CARDIOTONIC ACTIVITY
ANDREANI, A
RAMBALDI, M
LOCATELLI, A
LEONI, A
BOSSA, R
CHIERICOZZI, M
GALATULAS, I
SALVATORE, G
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1993, 28 (10) : 825 - 829
[5] [Anonymous], 2002, Metodo de Referencia para Testes de Diluicao em Caldo para a Determinacao da Sensibilidade a Terapia Antifungica dos Fungos Filamentosos: Norma Aprovada, V22, P1
[6] [Anonymous], ACTA CIENC INDICA CH
[7] [Anonymous], INDIAN J PHARMSCI
[8] [Anonymous], B FAC PHARM CAIRO U
[9] Captan G., 1996, FARMACO, V51, P729
[10] Novel antifungal drugs
DiDomenico, B
[J]. CURRENT OPINION IN MICROBIOLOGY, 1999, 2 (05) : 509 - 515

← 1 2 3 4 →