Jagattaran Das

Cu(I)-catalyzed three component coupling protocol for the synthesis of quinoline derivatives

Abstract Synthesis of 2,4-disubstituted quinolines has been achieved in a one-pot reaction from an aryl amine, an aldehyde and a terminal alkyne using CuCl (30 mol%) as a catalyst.

A facile conversion of a 310 helical structure to a cyclic β-turn mimic in dehydrophenylalanine-derived small peptides through ring-closing metathesis

Abstract Dehydrophenylalanine-derived small peptides can be preorganized in a 3 10 helical structure which is transformed into a β-turn mimic during a ring-closing metathesis cyclization.

Three-dimensional quantitative structure–activity relationship (3D-QSAR) studies of tricyclic oxazolidinones as antibacterial agents ☆

Oxazolidinones exemplified by eprezolid and linezolid are a new class of antibacterials that are active against Gram positive and anaerobic bacteria including methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphylococcus epidermidis (MRSE) and vancomycin resistant enterococci (VRE). In an effort to have a better antibacterial agent in the oxazolidinone class, we have performed three-dimensional quantitative structure-activity relationship (3D-QSAR) studies for a series of tricyclic oxazolidinones. 3D-QSAR studies were performed using the Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) procedures. These studies were performed using 42 compounds; the QSAR model was developed using a training set of 33 compounds. The predictive ability of the QSAR model was assessed using a test set of 9 compounds. The predictive 3D-QSAR models have conventional r(2) values of 0.975 and 0.940 for CoMFA and CoMSIA respectively; similarly, cross-validated coefficient q(2) values of 0.523 and 0.557 for CoMFA and CoMSIA, respectively, were obtained. The CoMFA 3D-QSAR model performed better than the CoMSIA model.

A study of adherence to DOTS regimen among pulmonary tuberculosis patients in West Tripura District

BACKGROUND Noncompliance to the DOTS regimen leads to treatment failure, relapse, MDR tuberculosis, XDR tuberculosis etc. requiring more prolonged & expensive therapy. AIM To assess the adherence rate among pulmonary tuberculosis patients in west Tripura district and to study the factors affecting adherence to DOTS regimen among pulmonary tuberculosis patients. MATERIAL AND METHODS This community based cross-sectional study was conducted among 220 pulmonary tuberculosis patients registered for treatment with DOTS therapy; under six randomly selected DMC of West Tripura District. RESULTS The study revealed that the adherence rate among the pulmonary TB patients was 84.50 percent. Male tuberculosis patients had 87.10 percent less chance of being adherent to the DOTS regimen in reference to females, and Cat I patients were 8.96 times (C.I. 2.689-29.857) more adherent to the therapy compared to the retreatment cases. Again, patients whose continuation phase was supervised as per the guidelines of DOTS were 12.07 times more adherent to the therapy. PTB patients who had the knowledge of supervised therapy in DOTS and curability of the disease, were 4.70 times (C.I. 1.39-15.79) and 9.39 times (C.I. 1.03-85.99) more adherent to the therapy, respectively. CONCLUSION The study showed good adherence to the regimen among pulmonary tuberculosis patients in spite of being a difficult area. It may also help in planning and implementation of tuberculosis control measures by addressing and overcoming the barriers regarding treatment completion.

Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid®

SummaryThe aim of this study was to determine the bioavailability of a novel oxazolidinone, DRF-6196, in mice and rats followingintravenous (i.v) and oral dosing and to compare the pharmacokinetics with those obtained following linezolid dosing. Blood samples were drawn at predetermined intervals up to 24 h post-dose after either DRF-6196 or linezolid administration. The concentrations of DRF-6196 and linezolid in various plasma samples were determined by a HPLC method. Following oral administration maximum concentrations of DRF-6196 were achieved within 0.5 h irrespective of the species. While the doses increased in the ratio of 1∶ 3 ∶10, mean Cmax and AUC(0−∞) values in mice for DRF-6196 increased in the ratio of 1∶ 3.87∶8.53 and 1 ∶ 2.51 ∶ 9.24, respectively. Both the Cmax and AUC0−∞ values increased almost proportional to the dose administered in mice. Following i.v administration, the concentration of DRF-6196 declined in a bi-exponential fashion with terminal elimination half-life of 1.5 h irrespective of the species. The systemic clearance and volume of distribution of DRF-6196 in mice were 1.14 L/h/kg and 0.66 L/kg, respectively afteri.v} administration, while the respective values in rats were 0.61 L/h/kg and 0.41L/kg, respectively. Elimination half-life ranged between 0.8–1.5 h. Absolute oral bioavailability of DRF-6196 was found to be 80–96% across the test dose range. Although plasma levels of DRF-6196 were lesser compared to linezolid in the initial hours, it may not have any consequences on the clinical effectiveness of the molecule.