A series of novel pyrido[2,3-d]pyrimidine derivatives 6 were prepared starting from 2-amino-3-cyano-4-trifluoromethyl-6-phenyl pyridine 3 via Grignard’s reaction, cyclization followed by coupling with aliphatic and cyclic amines. All the compounds 6 were screened for antibacterial, minimum bactericidal concentration (MBC), biofilm inhibition activity as well as antifungal and minimum fungicidal concentration (MFC) activities. Among the screened compounds, the compounds 6e, 6f, and 6m which showed exhibiting promising activity have been identified. The results reveal that the compound pyrido[2,3-d]pyrimidine derivative 6e altered the sterol profile which may exert its antifungal activity through inhibition of ergosterol biosynthesis and could be an ideal candidate for antifungal therapy. The molecular docking results also validated the antifungal results.

从2-氨基-3-氰基-4-三氟甲基-6-苯基吡啶3，经格氏反应，环化，然后与脂族和环状胺偶联，制备了一系列新颖的吡啶并[2,3- d ]嘧啶衍生物6。筛选所有化合物6的抗菌，最小杀菌浓度（MBC），生物膜抑制活性以及抗真菌和最小杀真菌浓度（MFC）活性。在筛选出的化合物中，已经鉴定出显示出有希望的活性的化合物6e，6f和6m。结果表明，化合物吡啶并[2,3- d ]嘧啶衍生物6e改变了甾醇谱，其可能通过抑制麦角固醇的生物合成而发挥其抗真菌活性，并且可能是抗真菌治疗的理想候选者。分子对接结果也验证了抗真菌结果。