Enzyme inhibitory, antifungal, antibacterial and hemolytic potential of various fractions of Colebrookia oppositifolia

The purpose of the present investigation was to assess the enzyme inhibition, antifungal, antibacterial and hemolytic activities of various fractions of Colebrookia oppositifolia Smith. The MeOH extract of plant was dissolved in dist. water and partitioned with n-hexane, CHCl[3], EtOAc and n-BuOH sequentially. Enzyme inhibition studies were done against four enzymes i.e. alpha-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Ethyl acetate fraction possessed very good activity against alpha-glucosidase [IC[50] 57.38 +/- 1.23 micro g/mL]. CHCl3 fraction displayed good activity against alpha-glucosidase and lipoxygenase while moderate activity against butyryl cholinesterase. EtOAc fraction displayed good activity against lipoxygenase. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Aqueous fraction displayed good activity against G. lucidum and A. flavus. Antibacterial activity was checked against Staphylococcus aureus, Bacillus subtilis, Pasturella multocida and Escherichia coli by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform, ethyl acetate and aqueous fraction showed good activity against E. coli. Chloroform fraction showed good activity against B. subtilis. Ethyl acetate fraction showed good activity against the P. multocida. All the studied fractions showed very less toxicity i.e. < 7%

Synthesis, characterization and biological screening of 5-substituted-1,3,4-oxadiazole-2yl-N-[2-methoxy-5-chlorophenyl]-2-sulfanyl acetamide

In the current study, a series of 5-substituted-1,3,4-oxadiazole-2yl-N-[2-methoxy-5-chlorophenyl]-2-sulfanyl acetamide was synthesized by converting variously substituted/unsubstituted aromatic organic acids successively into the corresponding esters, hydrazides and then 5-substituted-1,3,4-oxadiazole-2-thiols. Finally the target compounds were obtained by stirring 5-substituted-1,3,4-oxadiazole-2-thiols with N-[2-methoxy-5-chlorophenyl]-2-bromoacetamide in the presence of N,N-dimethyl formamide [DMF] and sodium hydride [NaH]. The structures of the synthesized compounds were confirmed based on [1]H-NMR, IR and mass spectral data. The synthesized compounds were screened against acetylcholinesterase [AChE], butyrylcholinesterase [BChE] and lipoxygenase enzymes [LOX] and were found to be relatively more active against acetyl cholinesterase