BACKGROUND The emergence of multi-drug resistant tuberculosis (MDR-TB) has heightened the need for new chemical classes and innovative strategies to tackle TB infections. It is urgent to discover new classes of molecules without cross-resistance with currently used antimycobacterial drugs. RESULTS Eighteen new 8-substituted protoberberine derivatives were synthesized and evaluated for their a...

Under the QSPR/QSAR paradigm, a comparative study is made of the known drug activity of as many as 15 anti-tubercular drugs vis-à-vis the computed quantum mechanical global reactivity descriptors like global hardness, global softness and global electrophilicity index. The comparative study reveals that the experimentally determined activity of drug molecules, including its variation with side s...

Schiff bases are a proven moiety in antitubercular drug discovery and the development. Drug is never-ending process due to evolving resistance by bacteria, as result, there need of developing new drugs. In this continuous discovery, series synthesized using quinoline carbohydrazide upon coupling with different aldehydes ethanolic media through multistep synthesis. These compounds were purified ...

Pseudomembranous colitis (PMC) may develop with long-term antibiotic administration, but is rarely reported to be caused by antitubercular agents. We present a case of PMC that occurred 120 days after starting rifampicin. A 74-year-old man was diagnosed with pulmonary tuberculosis and started on a standard HERZ regimen (isoniazid, ethambutol, rifampicin, pyrazinamide). After 4 months of HERZ, h...

Tuberculosis (TB) is the most common cause of cervical lymphadenopathy in the TB-endemic zone, like India but it can also mimic other diseases. Four cases of cervical lymphadenopathy presented to us as initial treatment failure after completion of six months of antitubercular drugs (ATD), including rifampicin, isoniazid, pyrazinamide, and ethambutol. All were diagnosed as having tuberculosis ei...

PURPOSE We report here the antimycobacterial activity of some already synthesized tetrazole derivatives containing tetrazole against Mycobacterium tuberculosis strain H37Rv. METHODS In vitro evaluation of the antitubercular activity was carried out within the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF) screening program for the discovery of novel drugs for the treat...

OBJECTIVE To report a case of cycloserine-induced acute psychosis in a young female while on second line antitubercular treatment (ATT) for tubercular meningitis. METHOD Case report. RESULTS A 20-year-old female, known case of tubercular meningitis on ATT since 8 months, presented with a 10-days history of headache, vomiting, and photophobia. A provisional diagnosis of drug-resistant tuberc...

Tuberculosis remains one of the major grievous diseases worldwide. The emergence of resistance to antituberculosis drugs emphasize the necessity to discover new therapeutic agents for preferential tuberculosis therapy. In this study, various novel 1-(1H-benzimidazol-2-ylmethyl) piperidin-4-imine derivatives were developed and checked for favorable pharmacokinetic parameters based on drug-likene...

Maintenance of cell-wall integrity in Mycobacterium tuberculosis is essential and is the target of several antitubercular drugs. For example, ethambutol targets arabinogalactan and lipoarabinomannan (LAM) biosynthesis through the inhibition of several arabinofuranosyltransferases. Apart from their role in cell-wall integrity, mycobacterial LAMs also exhibit important immunomodulatory activities...

Tuberculosis is considered to be one of the world's deadliest disease with 2 million deaths each year. The need for new antitubercular drugs is further exacerbated by the emergence of drug-resistance strains. Despite multiple recent efforts, the majority of the hits discovered by traditional target-based screening showed low efficiency in vivo. Therefore, there is heightened demand for whole-ce...