Wu, Yuan-Yuan; Shao, Wu-Bin; Zhu, Jian-Jun; Long, Zhou-Qing; Liu, Li-Wei; Wang, Pei-Yi; Li, Zhong; Yang, Song published the article 《Novel 1,3,4-Oxadiazole-2-carbohydrazides as Prospective Agricultural Antifungal Agents Potentially Targeting Succinate Dehydrogenase》. Keywords: oxadiazolecarbohydrazide agricultural antifungal targeting succinate dehydrogenase; 1,3,4-oxadiazole; bioactivity; carbohydrazide; succinate dehydrogenase inhibitor.They researched the compound: 2-Furoic hydrazide( cas:3326-71-4 ).Recommanded Product: 3326-71-4. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:3326-71-4) here.
A novel simple 1,3,4-oxadiazole-2-carbohydrazides was reported to discover low-cost and versatile antifungal agents. Bioassay results suggested that a majority of the designed compounds were extremely bioactive against four types of fungi and two kinds of oomycetes. This extreme bioactivity was highlighted by the applausive inhibitory effects of compounds 4b, 4h, 5c, 5g, 5h, 5i, 5m, 5p, 5t, and 5v against Gibberella zeae, affording EC50 values ranging from 0.486μg/mL to 0.799μg/mL, which were superior to that of fluopyram (2.96μg/mL) and comparable to those of carbendazim (0.947μg/mL) and prochloraz (0.570μg/mL). Meanwhile, compounds 4g, 5f, 5i, and 5t showed significant actions against Fusarium oxysporum with EC50 values of 0.652, 0.706, 0.813, and 0.925μg/mL, resp. Pharmacophore exploration suggested that the N’-phenyl-1,3,4-oxadiazole-2-carbohydrazide pattern is necessary for the bioactivity. Mol. docking of 5h with succinate dehydrogenase (SDH) indicated that it can completely locate the inside of the binding pocket via hydrogen-bonding and hydrophobic interactions, revealing that this novel framework might target SDH. This result was further verified by the significant inhibitory effect on SDH activity. In addition, SEM patterns were performed to elucidate the anti-G. zeae mechanism. Given these features, this type of frameworks is a suitable template for future exploration of alternative SDH inhibitors against plant microbial infections.
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Reference:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics