Synthesis of Chalcones, Pyrazolines, Amino Pyrimidines and Pyrimidinethiones as Antibacterial Agents.

Abstract

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Behaviour of 4,6-Diaryl-2(1H) pyrimidine-2-thiones Towards Some Electrophiles and Nucleophiles

“…40-60º) to give 12 (Table 1). Results and Discussion 4, 6-Diaryl -1, 2-dihydropyrimidine-2(1H)-thione (1) (11) is used as a key starting compound in the synthesis of fused pyrimidine derivatives. Thus, compounds 1a, 1b reacted with zinc dust in the presence of glacial acetic acid to give the corresponding 4, 6-diaryl-1, 2, 3, 4-tetrahydropyrimidine-2-thiones 2a, 2b.…”

“…Also, some thiazolopyrimidines were tested for their antiinflammatory activity and exerted a moderate effect (4) . In conjunction with our previous work on the synthesis of pyrimidinethione derivatives for biological evaluations (11)(12)(13)(14)(15)(16) , we report herein on the synthesis of a series involving the pyrimidine-2-thione moiety and screening of the antimicrobial activity of some of the new derivatives.…”

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“…Among numerous heterocycles compounds that have been synthesized and evaluated for their pharmacological activities, chalcone, pyrimidinone and pyrimidinethione have played a crucial role in medicinal chemistry. It was demonstrated that the presence of reactive α, β-unsaturated keto function in chalcones was responsible for their antibacterial and antifungal activities [3].…”

Solution Phase Combinatorial Synthesis and Screening of Mini Libraries of Arylchalcones for Antibacterial Activity

“…So far, several chalcone containing biologically active compounds have been synthesized [5][6][7]. However, there are few reports on solution phase combinatorial synthesis and combinatorial antibacterial screening, despite the simplicity, time and material saving involved in the process.…”