Evaluation of anti-inflammatory and antibacterial potential of newly synthesized 4-(2-Keto-1-benzimidazollinyl) derivatives of piperidine.

Benzimidazole and its derivatives found variety of biological activities, for the searching of its potent anti-inflammatory analogues, we synthesized four novel 4-(2-keto-1-benzimidazollinyl) piperidine derivatives (Q1 to Q4) by refluxing piperidine with substituted imidazole and subjected to in-vitro anti-inflammatory (ROS, NO) and antibacterial activities, structures were elucidated using spectroscopic techniques. Results revealed that compound Q1 showed most effective anti-inflammatory activity with IC 50 7.6±1.3 µg/ml compared with standard Ibuprofen having IC50 11.2±1.9µg/mL. Compound Q3 showed good activity for Nitrite accumulation by stimulating macrophages test similar to standard NG Methyl L-arginine acetate with IC50 value 24.2±0.8µg/mL. The antibacterial activity of these compounds were evaluated against selected Gram+ve E. faecalis, C. diphtheriae, S. aureus and Gram -ve organism E. coli, Enterobacter aerogenes and P. aeruginosa. Synthesized compounds showed low to moderate level of antibacterial activity Q1 showed the highest antibacterial activity against Enterococcus faecalis and Escherichia coli with zone of inhibition 18mm and Q3 showed highest activity against Corynebacterium diptheriae (ZOI:18mm). Structure-activity relationship (SAR) study revealed that among all the synthesized compounds unsubstituted naphthalene (Q1) and phenyl (Q3) ring containing derivatives were most potent.

Anti-Oxidant and digestive enzymes inhibitory based anti diabetic activity of crude and fractions of Carum carvi L. extracts.

In the present study crude ethanolic extract and its various fractions (ethyl acetate, hexane and aqueous) of medicinal plant Carum carvi L. were examined for α-amylase and α-glucosidase inhibition using an-in vitro model. Both digestive enzymes were extracted from bovine and green gram. The crude extract and its fractions were also studied for their antioxidant potential by DPPH and Nitric oxide activity. The quantitative assessment of phenol and flavonoid contents was also estimated. The crude extract and its fractions exhibited high in-vitro enzyme inhibitory activity against α-amylase and α-glucosidase at different concentrations with IC50 ranging from 421.4±7.8 to 810±5.71and 72±8.81 to 307.0±11.42µg/mL of each extract respectively. The plant showed highest total phenolic contents ranging from 29.5±0.49 to 112.5±0.36mg/g Gallic acid of extract, while the total flavonoid contents were estimated from3.08±0.02-85.4± 0.12mg/g Quercetin. The antioxidant activities of the all extracts, measured in terms of IC50 values were in the range of 53.05±1.98 to 211.5±31.06µg/mL. Nitric oxide scavenging ability exhibited their IC50 values from 26.3±5.51 to 121.3±5.32µg/mL. Ethanolic crude extract showed excellent result among all these fractions. GCMS analysis of ethanolic extract of Carum carvi L indicated the presence of several phytochemicals such as monoterpenes, unsaturated fatty acids, furan derivatives, phenolic and flavonoid contents.