Synthesis and characterization of novel benzimidazole embedded 1,3,5-trisubstituted pyrazolines as antimicrobial agents

Efficient syntheses of some new substituted pyrazoline derivatives linked to substituted benzimidazole scaffold were performed by multistep reaction sequences. All the synthesized compounds were characterized using elemental analysis and spectral studies (IR, 1D/2D NMR techniques and mass spectrometry). The synthesized compounds were screened for their antimicrobial activity against selected Gram-positive and Gram-negative bacteria, and fungi strain. The compounds with halo substituted phenyl group at C5 of the 1-phenyl pyrazoline ring (15, 16 and 17) showed significant antibacterial activity. Among the screened compounds, 17 showed most potent inhibitory activity (MIC = 64 μg mL-1) against a bacterial strain. The tested compounds were found to be almost inactive against the fungal strain C. albicans, apart from pyrazoline-1-carbothiomide 21, which was moderately active

Development and Validation of RP-HPLC Method for the Estimation of Voriconazole in Bulk and Pharmaceutical Dosage Form

Abstract: A simple, accurate and precise reverse phase HPLC method was developed for the estimation of Voriconazole in bulk and pharmaceutical dosage form. The drug was resolved on an enable C18G column (250 mm x 4.6 mm i.d, 5 µm particle size) used with photodiode array UVVisible detector using the mobile phase consisting of Acetonitrile and water in the ratio of 60:40V/V. The flow rate was 1 mL/min and the effluent was monitored at 256 nm. The retention time of the drug was 5.360 min. The linearity of the drug was found to be the concentration range 10-50 µg/mL. The method was found to be reproducible with relative standard deviation of <2%. The percentage recovery was 99.89-100.86%. The results of method have been validated according to ICH guidelines requirements. This method can be successfully employed for the quantitative analysis of Voriconazole in bulk and pharmaceutical dosage form

One-pot multicomponent diastereoselective synthesis of novel dihydro-1<i>H</i>-furo[2,3-<i>c</i>]pyrazoles

<p>An efficient method was developed for the diastereoselective synthesis of novel fused dihydro-1<i>H</i>-furo[2,3-<i>c</i>]pyrazole by a one-pot, four-component reaction of β-keto ester, hydrazine, aromatic aldehyde, and pyridinium ylide in the presence of triethylamine under microwave irradiation in solvent-free conditions in good yields. The merits of this cascade Knoevenagel condensation/Michael addition/cyclization sequence include its high atom economy, good yields, and efficiency of producing three new bonds (two C–C and one C–O) and two stereocenters in a single operation.</p

Dual Catalysis with an IrIII–AuI Heterodimetallic Complex: Reduction of Nitroarenes by Transfer Hydrogenation using Primary Alcohols

A triazolyl-di-ylidene ligand has been used for the preparation of a homodimetallic complex of gold, and a heterodimetallic compound of gold and iridium. Both complexes have been fully characterized and their molecular structures have been determined by means of X-ray diffraction. The catalytic properties of these two complexes have been evaluated in the reduction of nitroarenes by transfer hydrogenation using primary alcohols. The two complexes afford different reaction products; whereas the AuI–AuI catalyst yields a hydroxylamine, the IrIII–AuI complex facilitates the formation of an imine