Two series of bis(3,5-dimethylpiperidinyl)-1,3,5-triazinyl)-N-(phenyl/benzothiazolyl)-acetamides were synthesized so as to investigate their antimicrobial and antimycobacterial actions. Intermediate 4-(4,6-bis(3,5 dimethylpiperidin-1-yl)-1,3,5-triazin-2-yl)aniline was synthesized by palladium-catalyzed Suzuki cross-coupling reaction to furnish C–C bond formation to s-triazine ring. Pharmacological screening against eight bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, and S. flexneri), four fungi (A. niger, A. fumigatus, A. clavatus, and C. albicans), and Mycobacterium tuberculosis H37Rv was examined and the effects of various substituents on biological profiles (MIC, 1.56–50 lg/mL) of final analogues were investigated. Four (8c, 8i, 9d, 9j) of the final analogues displayed antimycobacterial activity (3.12–6.25 lg/mL) equipotent to standard drugs.