2-hydroxyphenacyl azoles and related azolium derivatives as antifungal agents

被引：98

作者：

Emami, Saeed ^{[1
]}

Forournadi, Alireza ^{[2
,3
,5
]}

Falahati, Mehraban ^{[4
]}

Lotfali, Ensieh ^{[4
]}

Rajabalian, Saeed ^{[5
]}

Ebrahimi, Soltan-Ahmed ^{[4
]}

Farahyar, Shirin ^{[4
]}

Shafiee, Abbas ^{[2
,3
]}

机构：

[1] Mazandaran Univ Med Sci, Fac Pharm, Dept Med Chem, Sari 48175, Iran

[2] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran 14174, Iran

[3] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran

[4] Iran Univ Med Sci, Fac Med, Dept Parasitol, Tehran, Iran

[5] Kerman Univ Med Sci, Kerman Neurosci Res Ctr, Kerman, Iran

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

azole; imidazole; 1,2,4-triazole; 2-hydroxyacetophenone; antifungal activity; cytotoxicity;

D O I：

10.1016/j.bmcl.2007.10.111

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Hydroxyphenacyl azole and 2-hydroxyphenacyl azolium compounds have been described as a new class of azole antifungals. Most target compounds showed significant in vitro antifungal activities against tested fungi (Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum) with low MICs values included in the range of 0.25-32 mu g/mL comparable to reference drug fluconazole. The most active compounds were also assessed for their cytotoxicity using MTT colorimetric assay on normal mouse fibroblast (NIH/3T3) cells. The results of antifungal activity and toxicity tests indicated that these compounds display antifungal activity at non-cytotoxic concentrations. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：141 / 146

页数：6

共 18 条

[1] SYNTHESIS OF 1-ALKYL-1,2,4-TRIAZOLES - A NEW ONE-POT REGIOSPECIFIC PROCEDURE
ASTLEFORD, BA
GOE, GL
KEAY, JG
SCRIVEN, EFV
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1989, 54 (03) : 731 - 732
[2] BALASUBRAMANIAN M, 1994, HETEROCYCLES, V37, P1951
[3] Study on the substituents' effects of a series of synthetic chalcones against the yeast Candida albicans
Batovska, D.
Parushev, St.
Slavova, A.
Bankova, V.
Tsvetkova, I.
Ninova, M.
Najdenski, H.
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2007, 42 (01) : 87 - 92
[4] SYNTHESIS OF THE 7-CHLORO-DERIVATIVES OF CHROMONE, FLAVONE, AND ISOFLAVONE
BRYAN, JD
GOLDBERG, AA
WRAGG, AH
[J]. JOURNAL OF THE CHEMICAL SOCIETY, 1960, (MAR): : 1279 - 1281
[5] IMIDAZOLYL DERIVATIVES OF THE CHROMAN RING .1.
COZZI, P
MONGELLI, N
PILLAN, A
[J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1984, 21 (02) : 311 - 315
[6] British Society for Medical Mycology proposed standards of care for patients with invasive fungal infections
Denning, DW
Kibbler, CC
Barnes, RA
[J]. LANCET INFECTIOUS DISEASES, 2003, 3 (04) : 230 - 240
[7] Dimmock JR, 1999, CURR MED CHEM, V6, P1125
[8] Emami S, 2001, HETEROCYCLES, V55, P2059
[9] Emerging novel antifungal agents
Fostel, JM
Lartey, PA
[J]. DRUG DISCOVERY TODAY, 2000, 5 (01) : 25 - 32
[10] GARBER G, 2001, DRUGS S1, P1

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