A novel green and efficient one-pot multicomponent reaction of dihydropyridine derivatives was reported as having good to excellent yield. In the presence of the catalyst ceric ammonium nitrate (CAN), different 1,3-diones and same starting materials as 5-bromothiophene-2-carboxaldehyde and ammonium acetate were used at room temperature under solvent-free condition for the Hantzsch pyridine synthesis within a short period of time. All compounds were evaluated for their
in vitro
antibacterial and antifungal activity and, interestingly, we found that
5(b–f)
show excellent activity compared with Ampicillin, whereas only the
5e
compound shows excellent antifungal activity against
Candida albicans
compared with griseofulvin. The cytotoxicity of all compounds has been assessed against breast tumour cell lines (BT-549), but no activity was found. The X-ray structure of one such compound,
5a
, viewed as a colourless block crystal, corresponded accurately to a primitive monoclinic cell.