Design,synthesis and antifungal evaluation of novel benzimidazole tertiary amine type of fluconazole analogues

A novel series of compounds containing tertiary amine moiety, substituted benzimidazole and triazole ring, initial design by molecular docking study of this scaffold at the active site of the fungal enzymes lanosterol 14α-demethylase (homology modeled of C. albicans) was synthesized by microwave irradiation and characterized by Proton Nuclear Magnetic Resonance (¹H NMR), Infra Red (IR), and Mass Spectroscopy (MS), and by elemental analysis. The screening of compound for in vitro (turbidimetric method) and in vivo (kidney burden test) antifungal activity against C. albicans revealed activity in many of the compounds as comparable to that of fluconazole.     

Determination of guaifenesin from spiked human plasma using RP-HPLC with UV detection

A rapid, simple, selective and specific high performance liquid chromatography (HPLC) method with UV detection (230 nm) was developed and validated for estimation of guaifenesin from spiked human plasma. The analyte and internal standard (eplerenone) were extracted with dichloromethane. The chromatographic separation was performed on HiQSil C 18HS column (250 × 4.6 mm, 5 μm) with a mobile phase of methanol: water (60: 40%, v/v) at a flow rate of 1 mL/min. Guaifenesin was well resolved from plasma constituents and internal standard. The calibration curve was linear in the range of 100–3200 ng/mL. The heteroscedasticity was minimized by using weighted least square regression with weighing factor of 1/x. The intra- and inter-day % RSD was less than 15. Results of recovery studies prove the extraction efficiency. Stability data indicated that guaifenesin was stable in plasma after three freeze thaw cycles and upon storage at ?20°C for 30 days.