A facile method for preparation and evaluation of the antimicrobial efficiency of various heterocycles containing thieno[2,3-d]pyrimidine

Abstract

Heterocyclic compounds play an important role in the field of pharmaceutical chemistry, especially compounds containing hybrid bioactive moieties. So in continuation of our work, We focused mainly here on design, synthesis, and transformations of novel bio-active molecules bearing thieno[2,3-d]pyrimidine moiety which can be used as antibacterial and antifungal drugs after some modifications. The starting compound 2-chloromethyl-3H-7-p-tolylamino-4-oxo-9-phenyl-pyrimido[4',5':4,5]thieno[2,3-d]pyrimidine (1) which was prepared according to literature, was converted into many other derivatives bearing different functional groups to make a comparable study of their antimicrobial activity. The chemical constructions of all obtained compounds were well elucidated by the means of their analytical and spectral analyses (TLC, IR, ¹H NMR, ¹³C NMR, and MS). The title compounds have been chosen and screened for their in vitro antimicrobial efficiency versus some genera of bacteria and fungi, from the practical results we concluded that most of these compounds were powerful antimicrobial agents.

Graphical Abstract

Keywords:

• Antibacterial
• antifungal
• mercaptomethyl
• pyrimidothienopyrimidine
• synthesis
• thiadiazolyl
• thienopyrimidine
• triazolyl

Disclosure statement

No potential conflict of interest was reported by the author(s).