الفهرس 
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Abstract
A general survey about the inflammation, anti-inflammatory drugs and
their mechanism of action, as well as a survey about the methods of
synthesis of N-aryl pyrazoles. Finally, a small introduction about different
approaches of computer aided drug design.
A series of 3,4-bis-chalcone-N-arylpyrazoles IIIa-k was prepared from
diacetyl pyrazoles IIa-e. The reaction of IId,e with hydrazine hydrate gave
pyrazolo[3,4-d]pyridazine derivatives IVa,b. Furthermore, the reaction of
IIa-e with thiosemicarbazide afforded pyrazolo[3,4-d]pyridazine thiocyanate
salts Va-e. The synthesized compounds were subjected to in vivo antiinflammatory
and ulcerogenic activities in addition to their in vitro Cox
selectivity to give a full profile about their anti-inflammatory activity.
Compounds IIIc, IIIf, IIIi and IIIe showed a significant anti-inflammatory
activity among the synthesized compounds. Moreover, docking studies were
performed to give an explanation for their anti-inflammatory activity
through COX selectivity.
The present investigation involves the synthesis of the following new
intermediates:
1) 3,4-Diacetyl-1(4-fluorophenyl)5-methylpyrazole.
2) 3,4-Diacetyl-1(4-bromophenyl)5-methylpyrazole.
The present study also comprises the synthesis of the following new
compounds:
1) 1-(4-Phenyl)-3,4-bis(2,4dichlorocinnamoyl)-5-methylpyrazole.
2) 1-(4-Methylphenyl)-3,4-bis(2,4-dichlorocinnamoyl)-5-
methylpyrazole.
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3) 1-(4-Chlorophenyl)-3,4-bis(4-methoxycinnamoyl)-5-methylpyrazole.
4) 1-(4-Chlorophenyl)-3,4-bis(2,4-dichlorocinnamoyl)-5-
methylpyrazole.
5) 1-(4-Chlorophenyl)-3,4-bis(3-(furan-2-yl)acryloyl)-5-methylpyrazole.
6) 1-(4-Fluorophenyl)-3,4-bis(4-methoxycinnamoyl)-5-methylpyrazole.
7) 1-(4-Fluorophenyl)-3,4-bis(2,4-dichlorocinnamoyl)-5-methylpyrazole.
8) 1-(4-Fluorophenyl)-3,4-bis(3-(furan-2-yl)acryloyl)-5-methylpyrazole.
9) 1-(4-Bromophenyl)-3,4-bis(4-methoxycinnamoyl)-5-methylpyrazole.
10) 1-(4-Bromophenyl)-3,4-bis(2,4-dichlorocinnamoyl)-5-
methylpyrazole.
11) 1-(4-Bromophenyl)-3,4-bis(3-(furan-2-yl)acryloyl)-5-
methylpyrazole.
12) 2-(4-Fluorophenyl)-3,4,7-trimethyl-2H-pyrazolo[3,4-d]pyridazine.
13) 2-(4-Bromophenyl)-3,4,7-trimethyl-2H-pyrazolo[3,4-d]pyridazine.
14) 3,4,7-Trimethyl-2-phenyl-2H-pyrazolo[3,4-d]pyridazin-5-ium
isothiocyanate.
15) 3,4,7-Trimethyl-2-(p-tolyl)-2H-pyrazolo[3,4-d]pyridazin-5-ium
isothiocyanate.
16) 2-(4-Chlorophenyl)-3,4,7-trimethyl-2H-pyrazolo[3,4-d]pyridazin-5-
ium isothiocyanate.
17) 2-(4-Fluorophenyl)-3,4,7-trimethyl-2H-pyrazolo[3,4-d]pyridazin-5-
ium isothiocyanate.
18) 2-(4-Bromophenyl)-3,4,7-trimethyl-2H-pyrazolo[3,4-d]pyridazin-5-
ium isothiocyanate.