A wide array of dihydro[1,5]azo[1,2-a]pyrimidine 2-esters have been synthesised at room temperature in moderate to good yields through one-pot reaction between nitrostyrene derived MBH acetates and aminoazole derivatives with γ-α cyclisation. The reaction involves a cascade S_N2 reaction followed by intramolecular Michael addition–cyclisation with the generation of two new carbon–nitrogen bonds. The structure was further confirmed by single X-ray crystal analysis. Docking and in vitro studies of dihydrobenzimidazo pyrimidine derivatives against acetylcholinesterase (AChE) have been performed and the compounds 3d and 3e exhibit potent inhibitory activities with an IC₅₀ of 46.8 nM and 42.5 nM respectively.

A series of substituted 2-amino-1,3-thiazines were synthesized as amides (9a–9i), carbamates (9j–9m), sulfonamides (9n–9o) and urea derivatives (9p–9q) by treating the compound 7 with acid chlorides (8a–8i), chloroformates (8j–8m), sulfonyl chlorides (8n–8o) and isocyanates (8p–8q) respectively. The synthesized compounds (9a–9q) were screened for antituberculosis activity against Mycobacterium tuberculosis H₃₇Rv ATCC 27294 and the results show that some of these derivatives possess good activity against Mycobacterium tuberculosis H₃₇Rv ATCC 27294. A few also display promising cytotoxic activity against human breast cancer MCF-7 and human esophageal cancer EC-9706 cell lines. Regarding both biological profiles 9b, 9m and 9h are the most active for anti-cancer, anti-TB activity.