Chemistry Articles

With an aim to identify the structural requirements for selective AT1 angiotensin antagonistic activity, a quantitative structure activity relationship (QSAR) analysis was carried out on a series of 6-substituted benzimidazole derivatives. The QSAR expressions were generated using 28 compounds and the predictive ability of the resulting model was evaluated against a test set of 12 compounds.

3,5-Bis(4-chlorobenzylidene)-1-ethylpiperidin-4-one (1b) was condensed with malononitrile or cyanothioacetamide to yield pyranopyridine 2 and thiopyrido-pyridine 3b, respectively. Treatment of compound 3b with methyl iodide or ethyl chloroacetate in the presence of a base catalyst gave the corresponding compounds 4 and 5.

Four pendenticity based topological descriptors termed as superaugmented pendentic indices have been conceptualized in the present study. An in-house computer program was utilized to compute index values of all the possible structures (with at least one pendent vertex) containing four, five and six vertices.

Parasitic and bacterial infections affecting the gastrointestinal tract represent a significant cause of morbidity and mortality worldwide. Nitroheterocyclic drugs have been available since the early 1960s for the treatment of anaerobic protozoa. The application of these drugs has widened and they are presently used to treat anaerobic pathogenic bacteria and protozoa.

The treatment for chronic anal fissure (CAF) has undergone a transformation in recent years from surgical to medical. Both the approaches share the common goal of reducing the spasm of anal sphincter. Though surgical treatment has a high success rate but it can permanently impair fecal continence in large number of patients.

An improved pegylated liposomal formulation of docetaxel has been developed with the purpose of improving the docetaxel solubility without any need to use tween80 that is responsible for hypersensitivities following administration. Liposomes all had spherical shape with size of 130–160 nm.

In the present work a new indomethacin (IND) self-nanoemulsifying drug delivery formulation (SNEDDF) have been prepared to enhance its dissolution which in turn could provide a better chance for IND oral absorption. IND SNEDDF have been prepared using different concentrations of castor oil as a solvent for IND, Cremophor RH 40 (Cr-40) as surfactant and Capmul MCM-C8 (Ca-8) as co-surfactant.

The present study describes development and in vitro evaluation of budesonide microparticles prepared by spray drying for delivering drug directly to lungs via dry powder inhaler. This paper introduces new formulations for pharmaceutical applications which includes conventional formulations and novel spray dried microparticles viz., pulmosols, microspheres and porous particles.

Pluronic F68 is a surfactant which can inhibit CYP3A4, an enzyme responsible for hepatic metabolism of many drugs including itraconazole. This study investigated the effect of incorporation of Pluronic F68 as a ternary component in solid dispersions of itraconazole with hydroxypropyl-methylcellulose (HPMC) on the dissolution rate of itraconazole.

Eighty-seven methanol extracts of medicinal plants, most of them are currently used in Vietnamese oriental medicine, were screened for NF-κB inhibitory activity. Seven methanol extracts showed strong to moderate inhibitory activity.