title: A Note on Derivatives of Isoniazid, Rifampicin, and Pyrazinamide Showing Activity Against Resistant Mycobacterium tuberculosis.
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.
authors.affiliation: Centre for Biomedical Informatics, National Institute for Research in Tuberculosis, Chennai, Tamil Nadu, 600 031, India.
authors.forename: Ameeruddin
authors.initials: A
authors.lastname: Nusrath Unissa
authors.affiliation: Scientist D, Division of Clinical Research, National Institute for Research in Tuberculosis, Chennai, Tamil Nadu, 600 031, India.
authors.forename: Luke Elizabeth
authors.initials: LE
authors.lastname: Hanna
authors.affiliation: Director General, Indian Council of Medical Research, Ansari Nagar, New Delhi, 110 029, India.
authors.forename: Soumya
authors.initials: S
authors.lastname: Swaminathan
mesh_terms: D000995:Antitubercular Agents / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000995:Antitubercular Agents
keywords: INH; MTB; PZA; RIF; derivatives; drug resistance