New Advances in Chemical Research in 2021.The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 136630-39-2, Name is 2,7-Dibromo-9H-carbazole, molecular formula is , belongs to benzoxazole compound. In a document, author is Luo, Bo, Safety of 2,7-Dibromo-9H-carbazole.
Based on benzoxazole and benzothiazole scaffold as an important pharmacophore, two series of 2-(aryloxymethyl) benzoxazole and benzothiazole derivatives were synthesized and their antifungal effects against eight phytopathogenic fungi were evaluated. Compounds 5a, 5b, 5h, and 5i exhibited significant antifungal activities against most of the pathogens tested. Especially 5a, 5b, 5h, 5i, 5j, and 6h inhibited the growth of F. solani with IC50 of 4.34-17.61 mu g/mL, which were stronger than that of the positive control, hymexazol (IC50 of 38.92 mu g/mL). 5h was the most potent inhibitor (IC50 of 4.34 mu/mL) against F. Solani, which was about nine times more potent than hymexazol. Most of the test compounds displayed significant antifungal effects against B. cinerea (IC50 of 19.92-77.41 mu g/mL), among them, 5a was the best one (IC50 of 19.92 mu g/mL). The structure-activity relationships (SARs) were compared and analyzed. The result indicates that the electron-drawing ability and position of the substituents have a significant impact on biological activities. Furthermore, docking studies were carried out on the lipid transfer protein sec14p from S. cerevisiae, and preliminarily verified the antifungal activities. Taken together, these results provide 2-(phenoxymethyl)benzo[d]oxazole as an encouraging framework that could lead to the development of potent novel antifungal agents.
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Reference:
Benzoxazole – Wikipedia,
,Benzoxazole | C7H5NO – PubChem