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Novel pyridine derivatives 1d and 7, pyrido[2,3‐d]pyrimidine derivatives 2a, 2b, 2c, 2d, 3a, 3b, 3c, 3d, 4a, 4b, 4c, 4d, 5a, 5b, 5c, 5d, 6a, 6b, 6c, 6d, 8a,8b, and 9a,9b were synthesized and screened for their anti‐microbial and cytotoxic activities. Compounds 2b, 2c, 3b, 3c, 5b, 5c, 6b, 6c, and 7 showed excellent anti‐microbial activities against all the tested bacteria and fungi compared to the reference drugs. Furthermore, they exhibited high safety profile in cytotoxicity test except 2c and 3c. The structures of the newly synthesized compounds were confirmed by spectral data and elemental analysis.

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