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Mycobacterial tuberculosis Enzyme Targets and their Inhibitors

Author(s):

Anil Kumar Saxena* and Anamika Singh   Pages 1 - 19 ( 19 )

Abstract:


Background: Tuberculosis (TB) is a major health problem worldwide. Mycobacterium tuberculosis has a unique ability to survive within the host, alternating between active and latent disease states, and escaping the immune system defences. There is an urgent need for new antibiotics active against drug-resistant organisms and that can shorten standard therapy due to the extended duration of anti-TB regimens and the increasing prevalence of multidrug- (MDR) and extensively drug-resistant (XDR) M. tuberculosis. The recent introduction of bedaquiline to treat MDR-TB and XDR-TB may improve the current status of the TB treatment.

Objectives:- The target enzymes in anti-tb drugs discovery program play a key role, hence efforts have been made to review the work on molecules incuding anti TB drugs acting on different enzyme targets including the recent one ATP synthase the target for bedaquiline.

Method:- literature search has been carried out to find the different chemical molecules including drugs and their enzyme targets responsible for their antitubercular activities in recent years.

Results:- This review provides an overview of the chemical structures with their antitubercular activities and enzyme targets like InhA, ATP synthase, Lip Y, Transmembrane transport protein large (MmpL3), Decaprenylphospho-b-D-ribofuranose 2-oxidase, (DprE1). The major focus has been on the new target ATP synthase.

Conclusions: Such an attempt may be useful in designing of new chemical entities (NCEs) for specific and multi -drug targeting against the M.Tb.

Keywords:

Mycobacterium tuberculosis, enzyme targets, inhibitors, minimum inhibitory concentration (MIC)

Affiliation:

Division of Medicinal and Process Chemistry, CSIR Central Drug Research Institute, Lucknow 226 001, Division of Medicinal and Process Chemistry, CSIR Central Drug Research Institute, Lucknow 226 001



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