Convenient Synthesis and Molecular Docking of Novel Pyrido [2,3- d ]pyrimidines as Potent Antimicrobial Candidates.

Sarhan, Alaadin; Soliman, Hanaa M.; Saleh, Abdulrahman M.; Nofal, Zinab M.

doi:10.21608/ejchem.2021.87454.4223

Convenient Synthesis and Molecular Docking of Novel Pyrido [2,3- d ]pyrimidines as Potent Antimicrobial Candidates.

Document Type : Original Article

Authors

¹ Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Center, 33 El Behouth St, Dokki-Giza, 12622-Egypt.

² 2Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Cairo, Egypt, 12622.

³ 3 Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys) Al-Azhar University , Cairo-Egypt

⁴ Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Center, 33 El Behouth St, Dokki-Giza, 12622-Egypt

10.21608/ejchem.2021.87454.4223

Abstract

New 3-(3,4-dimethoxyphenyl)-1-(thiophene-2-yl)prop-2-en-1-one has been designed as a starting compound to synthesis a novel series of substituted pyrido[2,3-d]pyrimidine system incorporated to different Schiff's bases and enamine derivatives as potent antimicrobial compounds. Novel synthesized compounds were evaluated for their in-vitro antimicrobial potency against different gram-positive and gram-negative bacteria, where they reveal high effectuality at low concentration compared to Trimethoprim. Docking studies and structure-activity relationship declared that new pyrido [2,3-d] pyrimidines completely occupied the active pocket of Biotin Carboxylase of both bacterial types and fungal strains acting as selective Fatty Acid Synthesase type II inhibitors.

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