82815-86-9Relevant articles and documents
Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment
Chai, Jianqi,Chen, Min,Jin, Fei,Kong, Xiangyi,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
, (2021/08/03)
Developing novel fungicide candidates are intensively promoted by the rapid emergences of resistant fungi that outbreak on agricultural production. Aiming to discovery novel antifungal leads, a series of 1,3,4-oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment were constructed for evaluating their inhibition effects against phytopathogenic fungi in vitro and in vivo. Systematically structural optimizations generated the bioactive molecule I32 that was identified as a promising inhibitor against Rhizoctonia solani with the in vivo preventative effect of 58.63% at 200 μg/mL. The observations that were captured by scanning electron microscopy and transmission electron microscopy demonstrated that the bioactive molecule I32 could induce the sprawling growth of hyphae, the local shrinkage and rupture on hyphal surfaces, the extreme swelling of vacuoles, the striking distortions on cell walls, and the reduction of mitochondria numbers. The above results provided an indispensable complement for the discovery of antifungal lead bearing a quinazolin-4(3H)-one and 1,3,4-oxadiazole fragment.
Development of a Robust Protocol for the Synthesis of 6-Hydroxybenzofuran-3-carboxylic Acid
Aronow, Jonas,Chassagne, Pierre,Cortes-Clerget, Margery,Erb, Bernhard,Gallou, Fabrice,Gallou, Isabelle,Jager, Andreas,Marti, Michael,Nuzzo, Gian-Luca,Seeger, Manuela
supporting information, p. 861 - 866 (2020/07/14)
Benzofuran scaffolds are fundamental moieties found in a variety of biologically active natural products and synthetic drugs. In the course of one of our development programs, we needed to develop a practical and cost-effective manufacturing approach to such a benzofuran scaffold. Here we report a highly robust four-step, one-pot process that provides access to a 6-hydroxybenzofuran-3-carboxylic acid structure. An 1H NMR monitoring study allowed a better understanding of the overall sequence of events and the nature of the detected intermediates. After six steps, including the optimized tandem process, the desired hydroxylated benzofuran was obtained in 40% yield with a purity above 99%.
Design and Synthesis of New 1,3,4-Oxadiazole - Benzothiazole and Hydrazone Derivatives as Promising Chemotherapeutic Agents
Kaya, Betül,Hussin, Weiam,Yurtta?, Leyla,Turan-Zitouni, Gülhan,Gen?er, Hülya Karaca,Baysal, Merve,Karaduman, Abdullah Burak,Kaplanclkll, Zafer Asim
, p. 275 - 282 (2017/06/05)
Looking for new cytotoxic and antimicrobial agents with improved antitumor activity, a series of hydrazide and oxadiazole derivatives were designed and synthesized using 3-methoxyphenol as starting substance. Novel N'-(arylidene)-2-(3-methoxyphenoxy)aceto