SYNTHESIS OF SUBSTITUTED TRIAZOLO-PYRROLE FUSED RING ADDUCT WITH BENZYLIDENE PIPERIDYL UREA/THIOUREA BRIDGE AND SCREENING FOR CNS DEPRESSION

The molecular design of two molecules have been derived from the tailoring of the benzodiazepine moiety in which the amide group is in cyclic form as well as bioisosteric (CH2≈NH) and we have incorporated the same amide linkage in open chain by keeping the triazolo-pyrrole ring having Mannich base of urea/thiourea linkage with piperidine nucleus for CNS depression activity. Phenyl substituted 5-pyrazolone has been synthesized by the reaction between phenyl hydrazine and ethyl acetoacetate and substituted trizolo-pyrrole fused ring has been synthesized by condensation of benzoylated phenyl substituted 5-pyrazolone with urea. This on reaction between Mannich base which has been synthesized by the reaction between benzaldehyde with piperidine and urea/thiourea produced amide bridge having variable atom X=O: Urea and X=S: Thiourea. The two components were characterized for their structural confirmation by IR spectra and elemental microanalysis

Author(s): VIKRAMKUMAR VISHNUBHAI PATEL AND PROF DR DHRUBO JYOTI SEN

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