Synthesis, characterization and study biological activity of some new 1, 3, 4-thiadiazole and pyrazolone derivatives containing indole ring

Abstract EN

This work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring.

The new 2-amino-1, 3, 4- thiadiazole derivatives[IV] and [V]a, b were synthesized by cyclization reaction of 2-methyl- 1H-indole-carbothiosemicarbazide[III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively.

Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2- amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter.

The new pyrazolone derivatives [XI] a, b were synthesized from heating under reflux equimolar from a mixture of acid hydrazides [X] a or [X] b and ethylacetoacetate in absolute ethanol.

Acetyl pyrazolone compounds [XII] a, b were synthesized by the reaction of pyrazolone derivatives [X] a or [X] b with acetyl chloride in 1,4-Dioxane in present of calcium hydroxide to give 4-acetyl pyrazolone derivatives [XI] a, b The new aryl hydrazone derivatives of pyrazoline [XIII] and [XIV] were synthesized by the reaction of one mole of compounds [XII] a or [XII] b with one mole of phenyl hydrazine or substituted phenyl hydrazine in ethanol.

All the synthesized compounds have been characterized by melting points, FTIR, 1HNMR and Mass spectroscopy (of some of theme).