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003 EG-GiCUC
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008 191114s2019 ua d f m 000 0 eng d
040 _aEG-GiCUC
_beng
_cEG-GiCUC
041 0 _aeng
049 _aDeposite
097 _aPh.D
099 _aCai01.12.10.Ph.D.2019.Mo.S
100 0 _aMona Said Mohammed Mahdy
245 1 0 _aSynthesis of some new azoles and their fused derivatives of expected biological activity /
_cMona Said Mohammed Mahdy ; Supervised Eman Ali Ragab
246 1 5 _aتشييد بعض الآزولات و مشتقاتها الملتحمة الجديدة ذات نشاط بيولوجى متوقع
260 _aCairo :
_bMona Said Mohammed Mahdy ,
_c2019
300 _a229 P. :
_bcharts ;
_c25cm
502 _aThesis (Ph.D.) - Cairo University - Faculty of Science - Department of Organic Chemistry
520 _aPyrazoles 4a, b, 7a-d and 10 obtained by reaction of 5-amino-3-cyanomethyl- 1H-pyrazole-4-carbonitrile 1 with each of arylsulfonyl chlorides, chloroacetamide derivatives and ethyl chloroacetate, respectively. The condensation of pyrazoles 4a,b, 7a-d and 10 with various aromatic aldehydes afforded the corresponding arylidene 12a-c, 15a-r and 17a-c, respectively. The antimicrobial activity of some new selected products was also investigated. Compound 1 also reacted with each of acetoacetanilide and chalcone afforded pyrazolo[1,5-a]pyrimidine 30 and 42, respectively. Condensation of 30 and 42 with various aromatic aldehydes afforded the corresponding arylidene 31a-i and 44a-g, respectively. Coupling of compounds 30 and 42 with aryldiazonium chlorides led to formation of 2- arylhydrazono derivatives 40a-d and 47a-d, respectively. The anticancer activity of some new selected products was also investigated, enzyme inhibition, cell cycle and apoptosis. Cyclocondensation of benzoylglycine with aromatic aldehyde give new oxazolone derivative 54a,b and 56. Oxazolone 4a,b heated with different aromatic amines gave imidazole 60a-h, also, compounds 54a,b heated with bis-amines to afford bis-imidazole derivatives 66a,b and 68a,b. The in vivo anti-inflammatory activity studied for some synthesized imidazole, also enzyme inhibition against COX-2 and DHFR enzyme. In silico study for some synthesized compounds were carried out (Molecular docking and lipiniski's rule of five)
530 _aIssued also as CD
653 4 _a5-amino-3-cyanomethyl-1H-pyrazole-4-carbonitrile
653 4 _aChalcone
653 4 _aThe antimicrobial activity
700 0 _aEman Ali Ragab ,
_eSupervisor
856 _uhttp://172.23.153.220/th.pdf
905 _aNazla
_eRevisor
905 _aSamia
_eCataloger
942 _2ddc
_cTH
999 _c75197
_d75197