Studies on radioprotective and antiviral activities of some bischalcone derivatives

This work reports the cyclic voltammetric,modulatory effect on oxidative stress markers againstradiation induced oxidative stress in E. coli bacteriaand antiviral activities of two bischalcone derivatives(2E,5E)-2,5-bis(3-methoxy-4-hydroxy-benzylidene)-cyclo-pentanone (B1) and (2E,5E)-2,5-bis(4-fluorobenzylidene)-cyclopentanone (B2). The reducing ability of B1 and B2was determined by cyclic voltammetry. The anodic peakcurrent ipa and anodic peak potential Epa of B1 and B2were -154.7, -99 lA, and -0.15 V, 0.0125 V, respec-tively. The low anodic current and low anodic peakpotential imply the good reducing ability of the molecules.The radioprotective effect of bischalcones was studied bygamma radiation induced oxidative stress in E. coli K12 at0.2 and 0.4 Gy. The bacteria samples treated with B1 andirradiated showed diminished level of TBARS, an oxida-tive stress marker. The levels of SOD and CAT antioxidantenzymes were brought to near basal level for B1 treatedand irradiated bacteria with respect to the control. Theprotective effect of the bischalcone derivatives againstradiation was further supported by determining colonyforming units (CFU) of bacteria in pre- and post-irradiatedsamples. Further, B2 showed 73.69% of inhibition ofbuffalopox virus and camelpox viru

In vitro biological activities of new heterocyclic chalconederivatives

This work reports the synthesis and character-ization of new heterocyclic chalcone derivatives 3(a–j) andin vitro biological evaluation for antiproliferative, antiox-idant, antibacterial, antifungal, and antiviral properties. The antiproliferative efficacy and LC50 of the compoundsagainst HepG2 cell lines were determined. The LC50 for 3dwas found to be 8 lg/mL. All the compounds exhibitedmoderate DPPH scavenging activity and moderate to goodantimicrobial activity against tested bacterial and fungalstrains. Further, the compounds at their respective maxi-mum non-toxic concentrations did not inhibit DNA viruseslike buffalopox, camelpox, and goatpox

In vitro and in silico biological studies of novel thiazolo[3,2-a]pyrimidine-6-carboxylate derivatives

In the present study, we report the synthesis,characterization of new series of thiazolo[3,2-a]pyrimi-dine-6-carboxylate derivatives 3a–f and 4a–f. The newlysynthesized compounds were screened for in vitro antimi-crobial and antiviral activities. The probable mode ofaction of these active compounds was determined throughin silico docking study by docking the receptor methionyl-tRNA synthetase and human inosine-50-monophosphatedehydrogenase (IMPDH) for antibacterial and antiviralactivities, respectively. Among the compounds, 4c exhib-ited excellent in vitro antimicrobial activity against alltested strains with binding and docking energies -35.6 and-12.4 kcal/mol, respectively. The antiviral studies werecarried out for the selected compounds in which 4aexhibited 73.69 and 54.42 % of inhibition of buffalopoxand camelpox viruses, respectively. Furthermore, com-pound 4a showed minimum docking and binding energyalong with the maximum hydrogen/hydrophobic interac-tion with IMPDH. The study contributes towards identifi-cation and screening of potential antimicrobial andantiviral agent’s against the pathogen