الفهرس Only 14 pages are availabe for public view
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Abstract
The present investigation comprises a survey covering the chemistry and the biological activities of compounds containing the indole ring system, with particular reference to 1-phenyl-lH-indole derivatives.
in this work, one known and seven novel intermediate compounds were prepared, in. addition to twenty two novel final compounds. A detailed discussion of the experimental results attained is presented with an adequate interpretation. Moreover, the new compounds were subjected to a molecular modeling simulation study using Catalyst software (Accelrys Inc.) to predict its anti-inflammatory activity and selectivity towards COX-2 enzyme.
Finally, the molecules with high fit values (and some of the molecules with low fit values) were subjected to in vivo evaluation of analgesic and anti-inflammaotory activity as wety as ulcerogenicity. The results revealed that compounds IV6, IVn, V2, IV8 and X2 were the most active.
The present investigation involves the synthesis of the following intermediates:
1. l-(2,6-Dichloropbenyl>lH-indol-2-ol.
2. l-(2,6-Dichlorophenyl)-2-(ethoxycarbonylmethoxy)-lH-indole.
3. l-(2,6-Dichlorophenyl)-2-(hydrazinocarbonylmethoxy)-lH-indole.
4. ]-(2,6-Dichlorophenyl)-2-(phenylarninothiocarbonylhydrazino-carbonylmethoxy)-! H-indole.
5. l-(2,6-Dichlorophenyl)-2-(2,4-dichlorophenyiaminothiocarbonyl-hydrazinocarbonylmethoxy)-lH-indole.
6. l-(2,6-Dichlorophenyl)-2-(4-fluorophenylaminothiocarbonyl-hydrazinocarbonylmethoxy)-lH-indble.
7. i-(2,6-Dichlorophenyl)-2-(4-iodophenylaminothiocarbonyl-hydrazinocarbonylmethoxy)-lH-indole.