Acta Pharm. 56 (2006) 441-450

full paper

Original research paper

 

Synthesis and antimicrobial evaluation of some new thienopyrimidine derivatives

 

MD. MOSHAREF HOSSAIN BHUIYAN*, KHANDKER MD. MIZANUR RAHMAN, MD. KAMRUL HOSSAIN, ABDUR RAHIM, ISMAIL HOSSAIN and MOHAMMAD ABU NASER

mosharef65@yahoo.com

Department of Chemistry, University of Chittagong, Chittagong-4331, Bangladesh

Accepted September 13, 2006

 

Reaction of heteroaromatic o-aminonitrile with ethyl N-[bis(methylthio)methylene]amino acetate resulted in annelation of a thieno[3,2-e]imidazo[1,2-c]pyrimidine moiety in a one step process. [1,2,4]Triazolo[4,3-c]thieno[3,2-e]pyrimidine derivatives were prepared by initial treatment of o-aminonitrile with carbon disulfide, followed by methylation with methyl iodide and subsequent reaction with benzhydrazide and thiosemicarbazide, respectively. Hydrazinothieno[2,3-d]pyrimidine was prepared by cyclization of heteroaromatic o-aminoester with formamide, followed by chlorination and subsequent displacement with hydrazine. Treatment of the hydrazine derivative with acetylacetone, benzaldehyde and acetic anhydride afforded pyrazolylpyrimidine, benzylidenehydrazonopyrimidine and trizolopyrimidine derivatives, respectively. Some of these derivatives exhibited pronounced antimicrobial activity.

 

Keywords: imidazopyrimidine, triazolopyrimidine, antimicrobial activity