This review discusses the biological and medicinal significance of one of the most important and interesting heterocyclic ring systems, the pyrimidine and its condensed derivatives. Herein, various physiologically important molecules, as well as, therapeutically used drugs having a pyrimidine or condensed pyrimidine system in their chemical structures, have been covered. The chemistry and synthesis of pyrimidines have also been briefly discussed.
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2-Cyanopyrimidine-Containing Molecules for N-Terminal Selective Cyclization of Phage-Displayed Peptides.
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Texas A&M Drug Discovery Center, Department of Chemistry, Texas A&M University, College Station, Texas 77843, United States.
Current methods for the macrocyclization of phage-displayed peptides often rely on small molecule linkers that nonspecifically react with targeted amino acid residues. To expand tool kits for more regioselective macrocyclization of phage-displayed peptides, this study explores the unique condensation reaction between an N-terminal cysteine and nitrile along with the reactivity of an internal cysteine. Five 2-cyanopyrimidine derivatives were synthesized for this purpose and evaluated for their selective macrocyclization of a protein-fused model peptide.
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Pharmaceuticals (Basel)
December 2024
Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Saudi Arabia.
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Objective: The synthesis of new heterocyclic compounds including 5-quinoline-pyrido[2,3-] pyrimidinone (-, , -), 6-quinoline-pyrido[2,3-]thiazolo[3,2-]pyrimidinone (, , -), 1,2,4-triazole-6-quinoline-pyrido[2,3-]thiazolo[3,2-]pyrimidinone (-), and pyrido[2,3-]thiazolo[3,2-]pyrimidine-ethyl-(pyridine)-9-thiaazabenzo[]azulenone () derivatives was performed with high yields while evaluating antimicrobial activities.
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Chemistry Department, Faculty of Science, Tanta University, Tanta, 31527, Egypt.
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Chemistry Department, Faculty of Science, Alexandria University, P.O. Box 426, Alexandria, 21321, Egypt.
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Bioorganic Laboratory, Department of Chemistry, University of Delhi Delhi-110007 India
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