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1.
J Chem Biol ; 7(1): 29-35, 2013 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-24432136

RESUMO

Fungal infections pose a continuous and serious threat to human health and life. The intrinsic resistance has been observed in many genera of fungi. Many fungal infections are caused by opportunistic pathogens that may be endogenous (Candida infections) or acquired from the environment (Cryptococcus and Aspergillus infections). So, new therapeutic strategies are needed to combat various fungal infections. Fluconazole shows good antifungal activity with relatively low toxicity and is preferred as first line antifungal therapy, but it has suffered from severe drug resistance. So, there is a need to design novel analogues by modification of fluconazole-like structure. A novel series of phenyl(2H-tetrazol-5-yl)methanamine derivatives were synthesized by reaction of α-amino nitrile with sodium azide and ZnCl2 in presence of isopropyl alcohol. They were evaluated for antifungal activity against Candida albicans and Aspergillus niger and subjected to docking study against 1EA1.

2.
Bioorg Med Chem ; 20(19): 5678-98, 2012 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-22902032

RESUMO

In recent years their has been an increased use of antifungal agents and has resulted in the development of resistance to drugs. Currently, use of standard antifungal therapies can be limited because of toxicity, low efficacy rates. Different types of mechanisms contribute to the development of resistance to antifungals. This has given raise to search for a new heterocycle with distinct action or multitargeted combination therapy. This review addresses the areas such as the underlying mechanisms, eight different targets such as ergosterol synthesis, chitin synthesis, ergosterol disruptors, glucan synthesis, squalene epoxidase, nucleic acid synthesis, protein synthesis, microtubules synthesis. The clinically employed drugs along with the current research work going on worldwide on different heterocycles are discussed. In recent advances various heterocycles including imidazole, benzimidazole etc., twenty three scaffolds and their lead identification are discussed.


Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Fungos/efeitos dos fármacos , Micoses/tratamento farmacológico , Animais , Antifúngicos/uso terapêutico , Azóis/química , Azóis/farmacologia , Azóis/uso terapêutico , Fungos/metabolismo , Humanos , Imidazóis/química , Imidazóis/farmacologia , Imidazóis/uso terapêutico
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