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A Note on Derivatives of Isoniazid,Rifampicin, and Pyrazinamide Showing Activity Against Resistant Mycobacterium tuberculosis
Authors:Ameeruddin Nusrath Unissa  Luke Elizabeth Hanna  Soumya Swaminathan
Institution:1. Centre for Biomedical Informatics, National Institute for Research in Tuberculosis, Chennai, Tamil Nadu, India;2. Scientist D, Division of Clinical Research, National Institute for Research in Tuberculosis, Chennai, Tamil Nadu, India;3. Director General, Indian Council of Medical Research, Ansari Nagar, New Delhi, India
Abstract:Drug‐resistant tuberculosis (DR‐TB) is a serious problem that impedes the success of the TB control program. Of note, multidrug‐resistant (MDR)‐TB and extensively drug‐resistant (XDR)‐TB have certainly complicated the scenario. One of the possible strategies to overcome drug resistance in an economic and simple manner would involve modification of existing anti‐TB drugs to obtain derivatives that can work on resistant TB bacilli. These may have improved half‐life and increased bioavailability, be more efficacious, and serve as cost‐effective alternatives, as compared to new drugs identified through conventional methods of drug discovery and development. Although extensive literature is available on the activity of various derivatives of first‐line drugs (isoniazid, rifampicin and pyrazinamide) on drug‐susceptible Mycobacterium tuberculosis (MTB), reports on the activity of derivatives on resistant MTB are very limited, to our knowledge. In light of this, the present review aims to provide a concise report on the derivatives of first‐line drugs that have the potential to overcome the resistance to the parental drug and could thus serve as effective alternatives.
Keywords:derivatives  drug resistance     INH        MTB        PZA        RIF   
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