Abstract

In the present study, a new class of triazino-caffeine derivatives with good antimicrobial activities is reported. Eight new triazino-caffeine derivatives were synthesized via Mitsunobu reaction, followed by intramolecular cyclization. Their chemical structures were established on the basis of elemental analysis, IR, 1H NMR, mass spectral data as well as through an alternate synthetic route. The compounds were also screened for their antimicrobial activities, among them, compounds 5c and 5d showed good inhibitory potentials, indicating the importance of morpholine moiety in enhancing antimicrobial activity. Therefore, it is concluded that the triazino-caffeine derivatives developed, show encouraging potentials in their medicinal applications.

Keywords: Triazino-caffeine derivatives, Mitsunobu reaction, intramolecular cyclization, antimicrobial activities, morpholine moiety, heterocycles.

Graphical Abstract