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摘要:The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition for predefined particle size of sodium fluoride. The sodium fluoride is mainly used in dental preparation for delivering the fluoride ion to the tooth enamel for that nano-particle size is required. Nowadays the milling process is used to reduce the particle size. But that process has some limitations due to crystalline nature of sodium fluoride;for overcoming those limitations, lyophilization method is used. A 43 level full factorial design was used to study the significant influence of process and product variables i.e. 1) Concentration of sodium fluoride, 2) Concentration of PVP, 3) Sample volume, 4) Drying surface, on particle size of sodium fluoride. The experimental design result shows that independent product variables significantly modify the structure and improve particle size reduction of sodium fluoride.
摘要:Objective Sulfanilamide,sulfadiazine,and dapsone were the first sulfonamides to be used to treat malaria by disrupting the folate biosynthesis process,which is essential for parasite ***,we aimed to synthesize novel N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives through a rational drug design *** All compounds were synthesized by the conventional method,and the products were characterized by spectral analysis(1 H NMR and mass spectrometry).The progression of the reaction was monitored using thin-layer chromatography(TLC).All the derivatives were analyzed for their effective binding mode in the allosteric site of the plasmodium cysteine protease *** and antifungal activities were determined using the broth dilution *** S6(N-(2-thiazol-4 yl)-acetyl-aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S9(N-(1 H-benzo[d]imidazol-2-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed five hydrogen bonds;S8(N-(2-1 H-imidazol-2 yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S10(N-(1 H-benzo[d]imidazol-5-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed four hydrogen bonds with the allosteric site of the *** the docking scores and formation of hydrogen bonds with the target enzyme,the novel derivatives were processed for wet lab *** the newly synthesized derivatives were subjected to in vitro antimalarial,antifungal,and antibacterial *** the derivatives exhibited sufficient sensitivity to the Plasmodium falciparum strain compared to the ***,compounds S9 and S10 showed the most potent dual antimicrobial and antimalarial *** also exhibited powerful molecular interactions in molecular docking *** Based on the above results,it was concluded that N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives have excellent biological potential to act as antimalarial,antifungal,
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