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A series of 4‐(1H‐pyrazol‐4‐yl)‐polyhydroquinolines were synthesized through one‐pot four‐component Hantzsch condensation of 1,3‐diphenyl‐1H‐pyrazole‐4‐carbaldehydes, ammonium acetate, dimedone, and alkyl acetoacetate in glycerol as a green reaction medium. The structures of the compounds are verified by spectroscopic methods and screened for their antimicrobial activity against Mycobacterium tuberculosis H37RV strain. Almost all the synthesized derivatives reveal excellent antitubercular activity based on minimum inhibitory concentration. Especially the compounds 5h and 5k exhibit outstanding antitubercular activity with minimum inhibitory concentration 1.6 μg/mL. In addition, molecular docking study of synthesized scaffolds against enoyl‐acyl carrier protein reductase from M. tuberculosis was performed to propose the binding modes.

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A clean and ecofriendly approach for the catalyst‐free synthesis of pyrido[2,3‐d]pyrimidine derivatives by one‐pot three‐component condensation of aromatic aldehyde, malononitrile and 6‐aminouracil or 6‐amino‐1,3‐dimethyluracil using glycerol–water (3:1) as green reaction media has been developed. Catalyst‐free synthesis with high to excellent yields and use of glycerol–water system as an environmentally benign reaction condition are the prominent features of this strategy. Moreover, excellent outcomes from the calculations of green chemistry metrics reveal the greenness of the protocol.