A series of twenty new chloropyrazine conjugated benzothiazepines (22–41) have been synthesized with 58%–95% yields. The compounds were characterized by using different spectroscopic techniques including FT-IR, 1H NMR, 13C NMR spectroscopy and mass spectrometry. their precursor chalcones (2–21) evaluated for antitubercular cytotoxic activities. Additionally, 22–41 also tested antimicrobial acti...

A series of novel 3, 4-methylenedioxybenzene scaffold incorporated 1,3,5-trisubstituted-2-pyrazoline derivatives was synthesised as potent antitubercular agents via chalcone intermediates by reaction with hydrazines. The structures of the compounds were confirmed by IR, 1HNMR, 13CNMR and mass spectral data. The novel pyrazolines were screened for in vitro antitubercular activity by almar blue d...

A series of heteronemin-related antitubercular scalaranes, both from natural products and from chemical derivatization, were subjected to structure–activity investigations. Based on the activity profile, three main regions; i.e., the substituted groups hovering over C-19/C-18 and furan moiety, the functionalities in the vicinity of C-16 and the right-hand side of ring D, and the substituted gro...

Hemophagocytic lymphohistiocytosis (HLH) is a disease of abnormal activation the immune system, either due to familial cause or sporadic cause, in relation various triggering agents. Secondary HLH complication diseases, such as infections, malignancies, and autoimmune disorders. In our case series, we present three cases secondary with varied etiologies. Case 1 involved an 18-year-old male hist...

Fragment based Quantitative structure activity relationship (QSAR) analysis on reported 25 2-(2-(4-aryloxybenzylidene) hydrazinyl) benzothiazole dataset as antitubercular agents were carried out. Molecules in the current dataset were fragmented into six fragments (R1, R2, R3, R4, R5, R6).Group based QSAR Models were derived using Multiple linear regression (MLR) analysis and selected on the bas...

Compounds originally designed as putative tubulin inhibitors were tested as antitubercular agents for inhibition of the Mycobacterium tuberculosis analogue of tubulin, FtsZ. Initial screening of 200 2-alkoxycarbonylpyridines found several that inhibited M. tuberculosis growth. Two compounds, SRI-3072 and SRI-7614, inhibited FtsZ polymerization and were equipotent against susceptible and single-...

Insertion profiles of antitubercular drugs isoniazid (INH), rifampicin (RFM) and ethambutol (ETH) into dipalmitoylphosphatidylcholine (DPPC) membrane models were evaluated by Langmuir monolayer technique. Maximum drug insertion into DPPC monolayer was observed with rifampicin with a surface pressure increase (Deltapi(max)) in the range of 21-33 mN/m depending upon rifampicin concentration. Ison...