Synthesis and biological activities of some indole derivatives

Abstract

The present investigation comprises a sUrvey coveri:pg the chemistry and the biological activities of compounds containing the indole ring system, with particularreference to 1-phenyl-1H-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 well as ulcerogenicity. The results revealed that compounds IV6, IV11,V,2, IV8 and X2 were the most active. The present investigation involves the synthesis of the following

intermediates: