Sui, Yan-Fei; Ansari, Mohammad Fawad; Zhou, Cheng-He published the artcile< Pyrimidinetrione-imidazoles as a Unique Structural Type of Potential Agents towards Candida Albicans: Design, Synthesis and Biological Evaluation>, Quality Control of 611-19-8, the main research area is imidazolylmethylene pyrimidinetrione preparation antifungal antibacterial cytotoxicity mol docking SAR; Antifungal; DNA; Imidazole; Membrane; Pyrimidinetrione.
A series of pyrimidinetrione-imidazole conjugates I [R1 = H, Et, 2-chlorobenzl, etc.] as potentially antifungal agents were developed. Bioassays manifested that I [R1 = 4-fluorobenzl] exerted favorable inhibition towards C. albicans (MIC=0.002 mM), being 6.5 folds more active than clin. antifungal drug fluconazole (MIC=0.013 mM). Preliminary mechanism research indicated that compound I [R1 = 4-fluorobenzl] could not only depolarize membrane potential but also permeabilize the membrane of C. albicans. Mol. docking was operated to simulate the interaction mode between mol. I [R1 = 4-fluorobenzl] and CYP51. In addition, hybrid I [R1 = 4-fluorobenzl] might form I [R1 = 4-fluorobenzl]-DNA supramol. complex via intercalating into DNA. The interference of membrane and DNA might contributed to its fungicidal capacity with no obvious tendency to induce the resistance against C. albicans. Conjugate I [R1 = 4-fluorobenzl] endowed good blood compatibility as well as low cytotoxicity towards HeLa and HEK-293T cells.
Chemistry – An Asian Journal published new progress about Antibacterial agents. 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Quality Control of 611-19-8.
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