Abstract:Pyrimidine is a 5-membered heterocyclic ring which is versatile lead compound for designing potent bioactive agents. This interesting group of compound has diverse biological activities such as antimicrobial, CNS depressant, anti-inflammatory, analgesic, anticonvulsant, anticancer, antihelmentic, antioxidant and herbicidal. Available data represents that pyrimidine being heterocyclic planar five membered ring systems has various pharmacological actions and Synthesis of various pyrimidine derivatives and their … Show more
“…Benzimidazole [ 51 , 52 ] and Pyrazole derivatives acting as antimicrobial agents [ 53 , 54 ]. Some recent review articles on novel pyrimidine analogs with various pharmacological activities may help the young researcher for designing and developing new active drugs [ [55] , [56] , [57] , [58] , [59] ]. Fig.…”
Section: Commercially Available Pyrimidine Drugsmentioning
“…Benzimidazole [ 51 , 52 ] and Pyrazole derivatives acting as antimicrobial agents [ 53 , 54 ]. Some recent review articles on novel pyrimidine analogs with various pharmacological activities may help the young researcher for designing and developing new active drugs [ [55] , [56] , [57] , [58] , [59] ]. Fig.…”
Section: Commercially Available Pyrimidine Drugsmentioning
“…Pyrimidinones are a significant component of many marine alkaloids and are important pharmacologically as privileged structures in drug research. Pyrimidinone system possesses inherent properties like calcium channel modulating, adrenergic agonistic, mitotic kinesin inhibiting, antibacterial, fungicidal, etc …”
Section: Solid-phase Synthesis Of
Pyrimidinonesmentioning
This
Review describes the existing synthetic approaches for the
solid-phase synthesis (SPS) of differently substituted and fused pyrimidine
derivatives. These synthetic strategies are classified on the basis
of the different synthetic routes leading to the particular type of
pyrimidine heterocycle formed. The Review discusses the application
of a variety of polystyrene derived supports for the construction
of pyrimidine rings. The effect of microwave heating on the solid-phase
synthesis is also addressed in the review.
“…Furthermore, the pyrimidine structure is closely related to the nucleobases—uracil, thymine, and cytosine—which makes pyrimidine molecules important building blocks in all living cells [ 28 , 29 ]. Pyrimidine-based compounds exhibit a broad spectrum of pharmacological activity, such as antimalarial [ 30 ], antidiabetic [ 31 ], antimicrobial [ 32 , 33 ], and anticancer activities [ 34 , 35 , 36 ].…”
The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b–9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. Molecular docking study was also performed to explore the binding modes of these derivatives at the active site of EGFR-PK. Compounds 3a, 5a and 9b displayed broad spectrum antimicrobial activity with MIC ranges of 4–16 µg/mL and potent cytotoxic activity with IC50 ranges of 1.17–2.79 µM. In addition, they provided suppressing activity against EGFR with IC50 ranges of 7.27–17.29 nM, higher than that of erlotinib, IC50 = 27.01 nM.
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