ABSTRACT
Eight new diaryltriazine derivatives containing 4-allylamino and 4-azido substitutes guided by molecular docking have been designed and synthesized based on our previous work.The evaluation of HIV inhibitory activity demonstrated that all compounds were potent against HIV-1 replication.The most active compound 7c exhibited activity against HIV-1 (IC50=0.034 μmol·L-1,SI=6475)and the double mutant strain (IC50=9.39 μmol·L-1)in the micromolar range, which was more potent than nevirapine.
ABSTRACT
Purpose The aim is to develop a synthesis method of the silver carboxymethyl chitosan and to study its bacteriostasis to Staphlococcus aureus(S.aureus),Pseudomonas aeruginusa(P.aeruginusa),Escherichia Coli(E.coli),Klebsiella pneumoniae(K.pneumoniae) and Proteus vulgaris(P.vulgaris).Methods Chitosan was modified by way of chemistry.The structure analysis of its derivate was analysed by infra-red absorption spectroscopy,using methods of dilution and concavering to study the bacteriostasis to some ordinary bacteria which cause infection in burn.Results The infra-red spectragram of the derivate showed the chitosan had been modified by chloroacetic acid.When the concentrationl of silver carboxymethyl chitosan was 1.028 mg/ml and the concentration of the five bacteria were 104CFU/ml，the rate of bacteriostasis was 88%、80.2%、75.3% to S.aureus、P.aeruginusa and E.coli respectively.The MIC of silver carboxymethyl chitosan was similar to that of AgNO3 when they act on S.aureus and P.aeruginusa,but the former was lower than later when acting on E.coli.Conclusion Silver carboxymethyl chitosan could inhibit some bacteria which caused infection in burn.It was a novel pharmaceutical in preventing and curing burn infection.