Asian Journal of Research in Chemistry

A. Rajasekaran ¹, S. Santhosh ¹, K. S. G. Arulkumaran ¹, M. Periyasamy ¹

Affiliations
1 KMCH College of Pharmacy, Coimbatore, Tamilnadu, IN

Abstract

Evaluating acetyl-CoA carboxylase (ACC) as the target enzyme for the treatment of hyperlipidemia can lead to the detection of new inhibitors that can potentially be optimized as lipid lowering agents and could also form a novel method of screening a large number of plant constituents. Inhibition of ACC2 may prevent lipid-induced insulin resistance and type 2 diabetes, making the enzyme an attractive pharmaceutical target. The crystal structures of the biotin carboxylase (BC) domain of human ACC2 (PDB ID: 3GLK) and carboxyl transferase (CT) domain of human ACC2 (PDB ID: 3FF6) have been selected for molecular targets for Insilico studies of some potent phytochemicals like hydroxycitric acid, terrestrosin, forskolin and EGC. The interactions between the compounds and crystal structures of the enzymes have been performed using Accelrys Discovery Studio 2.1 Ligandfit protocol. Findings from the docking procedure indicate different binding modes of the compounds , further more the studies reveal that EGC was found to be a ideal inhibitor for both ACC2 Domains, thus can be suggested as a better inhibitor for lipid lowering .

Keywords

Phytochemicals, Inhibitory Profiles, ACC Domains.

Full Text

     

I. Ponnilavarasan ¹, A. Rajasekaran ¹, K. K. Sivakumar ¹, C. Sundaramoorthi ¹, Swastika Ganguly ², R. Sivasakthi ³

Affiliations
1 Department of Pharmaceutical Chemistry, College of Pharmacy, Kovai Medical Center Research and Educational Trust, Coimbatore-641048, IN
2 Birla Institute of Technology, Mesra, Ranchi, IN
3 Cherrann’s College of Pharmacy, Coimbatore, Tamilnadu, IN

Abstract

A number of organic compounds obtained by chemical synthesis as model compounds have useful antimicrobial activities. Quinazoline ring is an aromatic benzopyrimidine system;many of its derivatives possess interesting biological activities, such as analgesic, anti-inflammatory, anti-microbial, and anti-tumor. In our study, the biological activity of synthesized quinazoline semicarbazone derivatives were characterized by antimicrobial screening against several gram-positive, gram negative bacteria, and fungus. The purity of the synthesized compounds was characterized by physicochemical properties, such as solubility, melting point, and thin layer chromatography (TLC). Elemental analysis for carbon, nitrogen, hydrogen, and oxygen was performed according to standard procedures. The presence of functional groups was analyzed using FT-IR spectra. Molecular structural information for the compounds was analyzed by 1H-NMR spectroscopy. The wavelengths of maximum absorbance for all the synthesized compounds were measured by UV-Visible spectroscopy. Thereby the chemical structures of the synthesized quinazoline derivatives were confirmed. Antimicrobial screening for all the compounds exhibits characteristic microbial inhibition. A detailed study is in progress to modify the synthetic route, structural activity, and toxicological barriers for the enhanced pharmacological efficiency of synthetic antibiotics.

Keywords

Antimicrobial Activity, Quinazoline Semicarbazone, Biological, Synthetic Antibiotics.

Full Text