Convenient Synthesis and Molecular Docking of Novel Pyrido [2,3- d ]pyrimidines as Potent Antimicrobial Candidates. | ||
| Egyptian Journal of Chemistry | ||
| Article 43, Volume 65, Issue 2, February 2022, Pages 399-411 PDF (986.38 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2021.87454.4223 | ||
| Authors | ||
| Alaadin sarhan* 1; hanaa M. soliman2; Abdulrahman M. Saleh3; Zinab M. Nofal4 | ||
| 1Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Center, 33 El Behouth St, Dokki-Giza, 12622-Egypt. | ||
| 22Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Cairo, Egypt, 12622. | ||
| 33 Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys) Al-Azhar University , Cairo-Egypt | ||
| 4Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Center, 33 El Behouth St, Dokki-Giza, 12622-Egypt | ||
| 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. | ||
| Keywords | ||
| Pyrido [2; 3-d] pyrimidine; Antimicrobial; Biotin Carboxylase; Molecular Docking | ||
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