Imidazolylchromanones containing non-benzylic oxime ethers: Synthesis and molecular modeling study of new azole antifungals selective against Cryptococcus gattii

Q1 · MEDICINE

Article

Author: Afsarian, Mohammad Hosein ; Irannejad, Hamid ; Emami, Saeed ; Babazadeh-Qazijahani, Mojtaba ; Badali, Hamid

A series of imidazolylchromanone oximes containing phenoxyethyl ether moiety, as found in omoconazole, were synthesized and evaluated against yeasts (Candida albicans and Cryptococcus gattii) and filamentous fungi (Aspergillus fumigatus and Exophiala dermatitidis). Although the title compounds showed marginal activity against filamentous fungi but all of them exhibited potent activity against C. gattii (MIC values ≤4 μg/mL). Among them, (3-chlorophenoxy)ethyl analog 7c with MIC value of 0.5 μg/mL was the most potent compound. Further molecular docking studies provided a better insight into the binding of designed compounds within the homology modeled active site of CnCYP51 (Cryptococcus CYP51-14α-demethylase).

01 Jul 2012·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Synthesis and biological evaluation of vinyl ether-containing azole derivatives as inhibitors of Trichophyton rubrum

Q4 · MEDICINE

Article

Author: Kai Wang ; Wenge Yang ; Fei Shen ; Lulu Wang ; Jing Zhu ; Yonghong Hu

In an attempt to search for many target compounds with excellent activities, a series of vinyl ether-containing azole derivatives were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against Trichophyton rubrum in vitro indicated that most of the synthesized compounds showed excellent activities. In comparison with fluconazole, itraconazole, voriconazole, omoconazole and amphotericin B, several compounds (such as 7d, 7g and 7h) exhibited more potent inhibitory activities, suggesting that they were promising leads for the development of novel antifungal agents.

01 Sep 1997·Journal of Antimicrobial ChemotherapyQ2 · MEDICINE

Therapeutic effects of omoconazole nitrate on experimental tinea pedis, an intractable dermatophytosis, in guinea-pigs

Q2 · MEDICINE

Article

Author: Uchida, Katsuhisa ; Yamaguchi, Hideyo ; Itoyama, Toshio ; Fujita, Shigeru

The therapeutic efficacy of omoconazole nitrate was investigated in an experimental tinea pedis model produced by topical inoculation with Trichophyton mentagrophytes in guinea-pigs, which is pathologically similar to naturally infected tinea pedis in humans. Treatment with omoconazole nitrate cream was started on week 2 postinfection and continued for 3 or 4 weeks. Once-a-day application of 1% omoconazole nitrate to the site of infection exhibited an excellent therapeutic efficacy, and was superior to 1% bifonazole cream in culture result. This result suggests that omoconazole nitrate has a potential usefulness for the treatment of tinea pedis in humans.

100 Deals associated with Omoconazole Nitrate

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KEGG	Wiki	ATC	Drug Bank
D01664	Omoconazole Nitrate	G01AF16 D01AC13	-

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Indication	Country/Location	Organization	Date
Candidiasis	-	-	-
Skin Diseases, Infectious	-	-	-

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