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：目的磺胺、磺胺嘧啶和氨苯砜是第一批通过破坏叶酸生物合成过程来治疗疟疾的磺胺类药物,叶酸生物合成过程是寄生虫存活的关键。因此,我们旨在通过合理的药物设计方法合成新型N-(2-芳基氨基苯基)-2,3-二苯基喹喔啉-6-磺酰胺衍生物。方法按常规方法合成所有化合物,并用光谱分析(1H核磁共振和质谱)对产物进行表征。使用薄层色谱法(TLC)监测反应进程。分析了所有衍生物在疟原虫半胱氨酸蛋白酶falcipain-2变构位点的有效结合模式。采用肉汤稀释法测定抗菌和抗真菌活性。结果S6(N-(2-噻唑-4-基)-乙酰基-氨基苯基)-2,3-二苯基喹喔啉-6-磺酰胺与S9(N-(1H-苯并[d]咪唑-2-基)氨基苯基)-2,3-二苯基喹喔啉-6-磺酰胺形成5个氢键;S8(N-(2-1H-咪唑-2-基)氨基苯基)-2,3-二苯基喹喔啉-6-磺酰胺和S10(N-(1-苯并[d]咪唑-5-基)氨基苯基)-2,3-二苯基喹喔啉-6-磺酰胺与酶的变构位点形成四个氢键。考虑到与目标酶的对接分数和氢键的形成,新的衍生物被加工用于湿实验室合成。所有新合成的衍生物都具有体外抗疟疾、抗真菌和抗菌活性。与标准品相比,所有衍生物对恶性疟原虫株表现出足够的敏感性。此外,化合物S9和S10显示出最有效的双重抗微生物和抗疟疾活性。它们在分子对接研究中也显示出强大的分子相互作用。结论基于以上结果,我们认为N-(2-芳基氨基苯基)-2,3-二苯基喹喔啉-6-磺酰胺衍生物具有作为抗疟药、抗真菌药和抗菌剂的优异生物潜力。