Recent progress in the drug development of coumarin derivatives as potent antituberculosis agents

Jun 27, 2015European journal of medicinal chemistry

New developments in coumarin-based drugs as strong treatments for tuberculosis

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Abstract

Tuberculosis (TB) is the second leading infectious cause of mortality today, behind only HIV/AIDS.

Mycobacterium tuberculosis (MTB) is recognized as one of the most deadly human pathogens.
The emergence of multi-drug resistant (MDR) strains has heightened the urgency for new antituberculosis drug development.
Longer therapy durations and the resurgence of TB in immunocompromised patients contribute to the development of MDR strains.
Coumarin derivatives are identified as important compounds with potential anti-TB activities, found in many natural products.
This review compiles information on coumarin derivatives, focusing on their preparation, characterization, and anti-TB applications.
Insights into structure-activity relationships (SAR) of coumarin analogs may assist in designing more effective anti-TB agents.

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Tuberculosis (TB) is still a challenging worldwide health problem and mycobacterium tuberculosis (MTB) remains one of the most deadly human pathogens. TB is the second leading infectious cause of mortality today behind only HIV/AIDS. The impetus for developing new structural classes of antituberculosis drugs comes from the emergence of multi-drug resistant (MDR) strains. The development of MDR strains to commonly used drugs is due to, longer durations of therapy as results of resistance, and the resurgence of the disease in immune compromised patients. Therefore, there is an urgent need to explore new antitubercular (anti-TB) agents. Ironically, the low number of potentially new chemical entities which can act as anti-TB candidates is of great importance at present situation. Considering the severity of the problem, WHO has prepared a strategic plan in Berlin declaration 2007 to stop TB, globally. Among the oxygen heterocycles, coumarin derivatives are important motifs, which can be widely found in many natural products, and many of them displaying diverse biological activities. This spectacular spectrum of applications has intrigued organic and medicinal chemists for decades to explore the natural coumarins or their synthetic analogs for their applicability as anti-TB drugs. To pave the way for the future research, there is a need to collect the latest information in this promising area. In the present review, we collated published reports on coumarin derivatives to shed light on the insights on different types of methods reported for their preparations, characterizations and anti-TB applications, so that its full therapeutic potential class of compounds can be utilized for the treatment of tuberculosis. Therefore, the objective of this review is to focus on important coumarin analogs with anti-TB activities, and structure-activity relationships (SAR) for designing the better anti-TB agents. It is hoped that, this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic coumarin-based anti-TB drugs.

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