الفهرس 
Title : Synthesis and biological evaluation of some new heterocycles incorporating pyridine
AbstractOnly 14 pages are availabe for public view
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Abstract
In 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