DNA base analogs, 2,4,5,6-substituted pyrimidines and 2,6-substituted purines were tested as potential inhibitors of E. coli Fpg protein (formamidopyrimidine -DNA glycosylase). Three of the seventeen compounds tested revealed inhibitory properties. 2-Thioxanthine was the most efficient, inhibiting 50% of 2,6-diamino-4-hydroxy-5N-methyl-formamidopyrimidine (Fapy-7MeG) excision activity at 17.1 m...

In acidic media, the 5,6-double bond of uridine is rapidly hydrated to give a small amount of 6-hydroxy-5,6-dihydrouridine (Urd-H2O), the mechanism of which is known from studies of the acid-catalyzed dehydration of Urd-H2O (Prior, J. J., Maley, J., and Santi, D. V. (1984) J. Biol. Chem. 258, 2422-2428). In addition to dehydration, Urd-H2O also undergoes direct hydrolysis of the N-glycosidic bo...

C1402 is fixed in pyrimidines of nucleic acids by Brucella abortus, strain 6232, during growth on complex artificial media (Newton et al., 1954). The incorporation of C02 into pyrimidines appears to be more obligatory in this strain of B. abortus which requires an increased pCO2 than it is in Escherichia coli (Bolton et al., 1952); a finding which suggested that strains of B. abortus which requ...

4,6-Disubstituted-2-(4-morpholinyl)pyrimidines, an important class of bioactive compounds, have been synthesized from 4,6-dichloro-2-(4-morpholinyl)pyrimidine by selective and sequential palladium-catalyzed cross-coupling reactions using triorganoindium reagents. This methodology, being efficient and versatile, allowed the synthesis of a variety of non-symmetrical pyrimidines functionalized at ...

In this investigation, the synthesis of 2-substituted pyrimidines by the reaction of benzofuranchalcones (3a-d) with urea, thiourea and guanidine hydrochloride was reported. The structuresof title compounds (4a-d), (5a-d) and (6a-d) were established on the basis of analyticaland spectral data. The synthesized compounds were screened for antimicrobial activityand molecular docking studies. Some ...

A highly efficient one-pot approach for the synthesis of carbonyl 2-amino-pyrimidines from 1,3-diynes and guanidine in the presence of Cs2CO3 and DMSO has been described. In these reactions, 1,3-diynes act as a precursor of buta-1,2,3-trienes and guanidine serves as the N-C[double bond, length as m-dash]N source for the construction of pyrimidines. This methodology proves to be a tandem regiose...

Conjugate addition reaction of various nucleophiles across the vinyl group of 2-chloro-4-vinylpyrimidine, 2-chloro-4-(1-phenylvinyl)pyrimidine and 2-chloro-4-vinylquinazoline provides the corresponding 2-chloro-4-(2-substituted ethyl)pyrimidines and 2-chloro-4-(2-substituted ethyl)quinazolines. Treatment of these products, without isolation, with N-methylpiperazine results in nucleophilic displ...