Synthesis of 2-[2'-Carbomyl-5'-(Heteroarylinomethylene)-1',3'4'-Thiadiazol-2' -Yl/Oxadiazol-2'-Yl)]-4,5-Dihydroimidazolines as Hypotensive Agents  

Mirdula Tyagi and Ashok Kumar*

Medicinal Chemistry Division Department of Pharmacology, L.L.R.M. Medical College, Meerut- 250 004 (India)

Ethylheteroarylinoacetates (1a-1b) were prepared by the reaction of ethylchloroacetate in the presence of anhydrous K2CO3. 1-(heteroarylinoa cetyl) thiosemicarbazides/semicarbazides (2a-2b) were synthesized by refluxing compounds (1a-1b) with thiosemicarbazide/semicarbazide. Compounds (2a-2d) reacts with conc. H2SO4 and then neutralized with liquid ammonia to yield compounds (3a-3d). Compounds (3a-3d) were then reacts with chloroacetylchloride to give compounds (4a-4d). Imidazoline derivatives i.e. compounds (5a-5d) were prepared by the reaction of compounds (4a-4d) with ethylenediamine and sulphur. All the newly synthesized compounds (i.e. 3a-3d - 5a-5d) were evaluated for their hypotensive activity. Almost all the compounds have shown promising hypotensive activity. Compound 5d was the most potent compound of this series. The most potent compound was evaluated for its hypotensive potency and acute toxicity.

Ethylheteroarylino acetates; hypotensive activity; acute toxicity