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1.
Molecules ; 19(9): 13161-76, 2014 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-25162957

RESUMO

Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis. Globally, tuberculosis is second only to AIDS in mortality and the disease is responsible for over 1.3 million deaths each year. The impractically long treatment schedules (generally 6-9 months) and unpleasant side effects of the current drugs often lead to poor patient compliance, which in turn has resulted in the emergence of multi-, extensively- and totally-drug resistant strains. The development of new classes of anti-tuberculosis drugs and new drug targets is of global importance, since attacking the bacterium using multiple strategies provides the best means to prevent resistance. This review presents an overview of the various strategies and compounds utilized to inhibit glutamine synthetase, a promising target for the development of drugs for TB therapy.


Assuntos
Antituberculosos/uso terapêutico , Glutamato-Amônia Ligase/antagonistas & inibidores , Mycobacterium tuberculosis/efeitos dos fármacos , Tuberculose/tratamento farmacológico , Antituberculosos/química , Descoberta de Drogas , Glutamato-Amônia Ligase/química , Glutamato-Amônia Ligase/metabolismo , Humanos , Mycobacterium tuberculosis/enzimologia , Relação Estrutura-Atividade , Tuberculose/enzimologia , Tuberculose/patologia
2.
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.

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