000			03657cam a2200337 a 4500
003			EG-GiCUC
005			20250223031822.0
008			171009s2016 ua h f m 000 0 eng d
040			_aEG-GiCUC _beng _cEG-GiCUC
041	0		_aeng
049			_aDeposite
097			_aM.Sc.
099			_aCai01.12.10.M.Sc.2016.Al.S
100	0		_aAly Hassan Abdelrahman Aly
245	1	0	_aSynthesis and biological evaluation of some new heterocycles incorporating pyridine / _cAly Hassan Abdelrahman Aly ; Supervised Fathy Mohamed Abdelrazek , Sobhy Mohamed Gomaa
246	1	5	_aتشييد وتقييم النشاط البيولوجى لبعض الحلقيات الغير متجانسة الجديدة المحتوية على بيريدين
260			_aCairo : _bAly Hassan Abdelrahman Aly , _c2016
300			_a160 P. : _bfacsimiles ; _c25cm
502			_aThesis (M.Sc.) - Cairo University - Faculty of Science - Department of Organic Chemistry
520			_aIn the first part: A novel series of 2-ethylidenehydrazono-5-arylazothiazoles 5a-h and 2-ethylidenehydrazono-5- arylazothiazolones 9a-d were prepared by cyclocondensation of hydrazonyl halides 3a-h and 7a-d with ethylidenethiosemicarbazide 2. In addition, reaction of 2 with N-phenyl carbohydrazonyl chloride (14), afforded 1,3,4-thiadiazole derivative 17 as the end product. Moreover, the thiosemicarbazide derivative 2 was reacted with various bromoacetyl compounds 19a-d and 1,1'-(1,4-phenylene)bis(2-bromoethanone) (21) furnished the respective thiazole derivatives 20a-d and 1,4-phenylene-bis-thiazole derivative 22. The structures of the newly synthesized compounds were established on the basis of spectroscopic evidences and their alternative syntheses. The newly synthesized compounds were evaluated for their anti-tumor activities against hepatocellular carcinoma (HepG2) cell line and the results revealed promising activities of compounds 5h, 5d, 5g, 5f and 5e with IC50 equal 2.23 ± 0.28, 2.48 ± 0.34, 2.49 ± 0.24, 4.03 ± 0.11, and 5.32 ± 0.27 oM, respectively. In the second part: (E)-3-(Dimethylamino)-1-(pyridin-4-yl)prop-2-en-1-one 2 underwent regioselective 1,3-dipolar cycloaddition with nitrilimines 4 to afford the corresponding pyrazoles 6. The reaction of the latter pyrazoles with hydrazine hydrate, afforded the corresponding pyrazolo[3,4-d]pyridazines 7. The enaminone 2 reacts also with 6- aminothiouracil 8 to yielded respective thione 9. The reaction of thione 9 with hydrazonoyl chlorides 3 yielded pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidinone derivatives 13. Furthermore, pyridine analogs substituted in the 4- position with a pyranone 17 or pyridinones 18, pyridinone 20, 22 or naphthofuran 24 were also synthesized. The structures of the newly synthesized compounds were confirmed by spectral data and elemental analyses. The antimicrobial activity of these newly synthesized compounds were assayed against two fungi species and two bacterial species; one Gram positive and one gram negative. Compounds 24 and 18 showed the most inhibitory effect among all tested compound. Molecular docking study predicted the best binding mode between compound 24 and the Enoyl-[acyl-carrier-protein] reductase [NADH] (InhA)f the compounds exhibit considerable activities
530			_aIssued also as CD
653		4	_aHeterocycles incorporating pyridine
653		4	_aIncorporating pyridine
653		4	_aNew heterocycles
700	0		_aFathy Mohamed Abdelrazek , _eSupervisor
700	0		_aSobhy Mohamed Gomaa , _eSupervisor
856			_uhttp://172.23.153.220/th.pdf
905			_aNazla _eRevisor
905			_aShimaa _eCataloger
942			_2ddc _cTH
999			_c62826 _d62826