الفهرس 
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Abstract
In the present study there is a brief literature review covering the most
important biological activities and the general methods for synthesis of pyridine,
pyrazole, thiazole and dihydrothiazolone derivatives.
Novel pyrazoline derivatives Va-g , VIa-g , IXa-c , Xa-c and XIa-c have been
synthesized starting from new α,β-unsaturated ketones IVa-g and VIIIa-c via
reaction with hydrazine hydrate in ethanol and acetic acid and thiosemicarbazide
(schemes 1,2).N-Thiocarbamoyl pyrazoline derivatives XIa-c used as key
intermediate for the synthesis of some new 2-pyrazolylthiazoles XIIa-l via
cyclization using phenacyl bromide derivatives (scheme 3) .Moreover,new
nicotinamide derivatives containing thiosemicarbazone moiety XIIIa-d were
obtained by refluxing equimolar amounts of N-(4-acetylphenyl)nicotinamide III
and the corresponding thiosemicarbazide derivatives (scheme 4) . Furthermore the
nicotinamide derivative with thiosemicarbazone moiety XIIIa was cyclized to
either thiazolyl nicotinamide derivatives XIVa-d,thiazolyl-4-(5H)-one-2-yl
nicotinamide XV and nicotinamidothiazole carboxylate XVI through their reaction
with phenacyl bromide derivat ives , ethyl bromoacetate or ethyl 2-
chloroacetoacetate, respectively .(Scheme 5).
Furthermore, theoretical discussion and detailed survey for the experimental
results attained with an interpretation of data.
The chemical structure of the newly synthesized compounds was confirmed
by IR, 1HNMR, 13CNMR, mass spectrometry and elemental analysis.The antimicrobial activity evaluation showed that most of the newly
synthesized compounds exhibited promising antibacterial as well as antifungal
activities.
On the other hand, some of the new compounds were screened for
cyclooxygenase I and II (COX-I and COX-II) inhibition assays using Celecoxib
,Diclofenac and Indomethacin as standards,Moreover their anti-inflammatory and
ulcerogenic activities were carried out using Celecoxib and Indomethacin as
reference drugs. The results obtained clearly focus the significance of compounds
XIIa, XIIb, XIIe, XIIj, XIIk, XIIl and XV as selective COX-II inhibitors,
However,their efficacies were associated with lower gastric ulcerogenicity
compared to Indomethacin.
Furthermore, some selected samples of the newly synthesized compounds
were evaluated for their anticancer activity against breast carcinoma (MCF-7) and
colon carcinoma (HCT-116) cell lines, Imatinib was used as positive control. The
anticancer activity showed that compounds Vc and VIc were the most active against
the two cell lines.
Molecular docking studies were performed in order to rationalize the obtained
biological results.