| Abstract: |
SUMMARY OF THE ORIGINAL WORK SYNTHESIS AND PHARAMACOLOGICAL STUDIES OF SOME INDOLE DERIVATIVESIndoles are know to possess extensive and varied biological activity, therefore the aim of the present investigation is to synthesize some new indole derivatives to test their toxicity, affect on smooth muscles, effect on arterial blood pressure and respiration and analgesic activity.Thus 2, 3-diphyenly-5-methoxy indole (XIX) was formulated according to VII smeier-Haack to yield the 6-formyl derivative (XX). The latter reacted with malononitrile to form -cyano-B (2, 3-diphenyl-5-methoxy-6-indolyl) acrylonitrile (XXI) which when treated with ketones, i.e. acetophenone, p-hydroxyacetophenone and p-aminoacetophenone, in the presence of ammonium acetate gave the corresponding 2-amino-3-cyano-4, 6-disubstituted pyridines (XXII a-C) (Cf scheme). When 2, 3-diphenyl-6-formyl-5-methoxyindole (XX) was treated with ethyl cyanoacetate, ethyl -cyano-B- (2, 3-diphenyl-5-methoxy-6-indolyl) cinnamate (XXIII) was obtained which upon reaction with urea in presence of potassium carbonate afforded 5-cyano-6-(2, 3-diphenyl-5-methoxy-6-indolyl) -2, 4-dioxo-1, 2, 3, 4-tetrahyDROPyrimidine (XXIV). On the other hand ethyl -cyano-B-substituted cinnamate (XXIII) yielded with thiourea 5-cyano-6-(2, 3-diphenyl-5-methoxy-6-indolyl)-4-oxo-2-thioxo-1, 2, 3, 4-tetrahyDROPyrimidine (XXXX) (Cf scheme).
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