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.