Medicinal Chemistry

A simple and sensitive spectrophotometric method has been described for the assay of quinolones in bulk drug and in pharmaceutical formulations. The developed method is based on the formation of colored charge transfer complexes of quinolones with chloranilic acid in acetonitrile solvent. The formed complexes absorbed at 417, 436, 419 and 436 nm for sparfloxacin, enoxacin, norfloxacin and levofloxacin respectively. Beer’s law is obeyed in the concentration range of 0.5-7, 1-10, 1-10 and 1-5 μg mL -1 with LLOD values 0.036, 0.0041, 0.0344 and 0.0063 ng mL -1 respectively. The data are discussed in terms of molar absorptivity, association constant and Gibb’s free energy. Spectral characteristics including oscillator’s strength, dipole moment, ionizationpotential, energy of complexes and resonance energy have been determined. Benesi-Hildebrand plots for each complex have been constructed. Structural characteristics of synthesized charge transfer complexes were determined by IR spectroscopy. The applicability of the method was demonstrated by determination of studied drugs in commercial tablets with satisfactory results. No interference from excipients was observed in the formulation

Background:

Angiopoietin-like protein 4 (Angptl4) is a new circulating protein of the Angiopoietin-like family, predominantly expressed in adipose tissue and liver. A link between Angptl4 and the levels of free fatty acids in human blood plasma remains unclear. Therefore, we hypothesized that any alteration in the concentration of plasma Angptl4 may be mediated by changes in plasma free fatty acid levels in healthy individuals.

Methods: To examine the effect of plasma free fatty acid levels on Angptl4 concentrations in humans, ELISA method was developed and used for the quantitative determination of human Angptl4 in plasma samples with known free fatty acid concentrations.

Results: It was clearly observed that there were significant (P. value<0.01) positive correlation between plasma Angptl4 concentrations and plasma levels of free fatty acid (0.905 ≤ r ≤ 1.00) and the standard curve using the human recombinant Angptl4 fragments yielded a consistent r 2 value>0.993. Raising plasma fatty acids resulted in an increase in the levels of Angptl4. While, lowering plasma fatty acids resulted in a decrease in the levels of Angptl4.

Conclusion: The results of this study indicate that changes in plasma free fatty acid levels are associated with alterations in the concentrations of Angptl4.

Diospyros lotus roots are traditionally used in various diseases including its use in microbialinfections. We designed a study to identify chemical constituents of oil from D. lotus and its antimicrobial activities. Gas chromatography coupled to mass spectrometer(GC-MS) was used for chemical analyses. Results showed that oil contained saturated as well as unsaturated compounds. Oil was investigated for its antimicrobial properties. Oil showed moderate antibacterial activity against two gram positive and two gram negative bacterial strains however oil showed low activity against four fungal strains. Interestingly no cytotoxicity was observed in Brine shrimp model; these encouraging results indicate further yet extensive studies to explore therapeuticpotential in microbial infections.

CAPE, one of the most active compounds in propolis, is the perfect illustration of a natural compound exhibiting diverse biological activities. However, rapid decomposition by esterase leads to its low bioavailability in vivo. The aim of the present study is to synthesis and investigates the antioxidant and protective activities of novel derivative of caffeic acid, CAMBA against STZ-induced diabetic complications in diabetic rats. Since amide is more resistant to esterase enzyme. CAMBA was synthesized by reacting the amino group of methyl anthranilate with caffeic acid in the presence of PCl 3 . Diabetic rats was induced by injection of STZ (55 mg/kg, i.p.) and diabetes was confirmed 48 h after induction, and then allowed for 7 days to stabilize blood glucose level. CAMBA (25 and 50 mg/kg b.w daily for 28 days) treated diabetic rats significantly reduced elevated blood glucose, TC, TG, atherogenic index, LDL-c, vLDL-c, hepatic, renal and cardiac TBARs and HP. The treatment also resulted in improved the insulin and insulin resistance and significantly increased serumHDL-c and GSH, SOD, CAT and GPx in the liver, kidney and heart of diabetic rats. The results clearly suggest that CAMBA treated group may effectively normalize the impaired antioxidant status in streptozotocin induced diabetes than the glibenclamide-treated groups. CAMBA exerted rapid protective effects against lipid peroxidation by scavenging of free radicals by reducing the risk of diabetic complications. Taken together, CAMBA has potential as an antioxidant agent for diabetes and deserves clinical trial in the near future as an adjuvant therapy in diabetic patients

Among a series of ten, 2-(4-chlorophrnyl)-5-aryl-1,3,4-oxadiazole analogs, 4c showed maximum activity on various cancer cell lines, with average growth percent of 95.37%. The molecular docking studies for the compounds 4a & 4c showed that the residue Cys797 is present near to the para substitution of phenyl group while the five member oxadiazole ring of ligandswas lying near to Leu792 and Met 793 of EGFR tyrosine kinase active