Synthesis of some new pyrazole and pyrazolopyrimidine derivatives of expected analgesic and antiinflammatory activity /
Reham Sayed Ibrahim
Synthesis of some new pyrazole and pyrazolopyrimidine derivatives of expected analgesic and antiinflammatory activity / تشييد بعض مركبات البيرازول ومشتقات البيرازولوبيرمدين الجديده ذات تاثير مسكن متوقع و مضاد للالتهاب Reham Sayed Ibrahim ; Supervised Afaf Kamal Eldin Elansary , Ehab Mohamed Gedawy , Elham Azz Elarab - Cairo : Reham Sayed Ibrahim , 2018 - 138 P. : charts , facsimiles ; 25cm
Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry
Novel pyrazole and pyrazolo[3,4-d]pyrimidine derivatives were prepared and evaluated for their analgesic activity. The most potent compounds V,Vb, IX, XIId, XIIIc,d, XIVa, XV were further evaluated for their antiinflammatoryactivity. Compounds VIb, IX, XIIIc,d were further evaluated for their ulcerogenic activity. Compounds VIb, IX, XIIId undergo in-vitro COX-II inhibitory activity assay. All Final prepared compounds were studied by molecular docking studies. Compound VIb showed both high analgesic, antiinflammatory, no ulcerogenic effect in addition to its higher selectivity index for COX-II enzyme with SI = 5.1 when comparing to celecoxib with SI = 6.2 exhibiting moderate binding energy -24.12 score Kcal/mol
Antiinflammatory activity Pyrazole Pyrazolopyrimidine
Synthesis of some new pyrazole and pyrazolopyrimidine derivatives of expected analgesic and antiinflammatory activity / تشييد بعض مركبات البيرازول ومشتقات البيرازولوبيرمدين الجديده ذات تاثير مسكن متوقع و مضاد للالتهاب Reham Sayed Ibrahim ; Supervised Afaf Kamal Eldin Elansary , Ehab Mohamed Gedawy , Elham Azz Elarab - Cairo : Reham Sayed Ibrahim , 2018 - 138 P. : charts , facsimiles ; 25cm
Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry
Novel pyrazole and pyrazolo[3,4-d]pyrimidine derivatives were prepared and evaluated for their analgesic activity. The most potent compounds V,Vb, IX, XIId, XIIIc,d, XIVa, XV were further evaluated for their antiinflammatoryactivity. Compounds VIb, IX, XIIIc,d were further evaluated for their ulcerogenic activity. Compounds VIb, IX, XIIId undergo in-vitro COX-II inhibitory activity assay. All Final prepared compounds were studied by molecular docking studies. Compound VIb showed both high analgesic, antiinflammatory, no ulcerogenic effect in addition to its higher selectivity index for COX-II enzyme with SI = 5.1 when comparing to celecoxib with SI = 6.2 exhibiting moderate binding energy -24.12 score Kcal/mol
Antiinflammatory activity Pyrazole Pyrazolopyrimidine