39232-91-2Relevant articles and documents
Synthetic studies towards paraherquamide F: Synthesis of the 1,7-dihydropyrano[2,3-g]indole ring system
Cox, Rhona J.,Williams, Robert M.
, p. 2149 - 2152 (2002)
A substituted 1,7-dihydropyrano[2,3-g]indole suitable for elaboration to paraherquamide F has been prepared in eight steps and 6% overall yield. The key steps are a Fischer indolization and a Claisen rearrangement.
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains
Bi, Fangchao,Song, Di,Qin, Yinhui,Liu, Xingbang,Teng, Yuetai,Zhang, Na,Zhang, Panpan,Zhang, Nan,Ma, Shutao
, p. 3179 - 3193 (2019/06/17)
The spread of infections caused by multidrug-resistant (MDR) pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA), has created a need for new antibiotics with novel mechanisms of action. The bacterial division protein FtsZ has been identified as a novel drug target that can be exploited clinically. As part of an ongoing effort to develop FtsZ-targeting antibacterial agents, we describe herein the design, synthesis and bioactivity of six series of novel 1,3,4-oxadiazol-2-one-containing, 1,2,4-triazol-3-one-containing and pyrazolin-5-one-containing benzamide derivatives. Among them, compound A14 was found to be the most potent antibacterial agent, much better than clinical drugs such as ciprofloxacin, linezolid and erythromycin against all the tested gram-positive strains, particularly methicillin-resistant, penicillin-resistant and clinical isolated S. aureus. Subsequent studies on biological activities and docking analyses proved that A14 functioned as an effective compound targeting FtsZ. Preliminary SAR indicated a general direction for further optimization of these novel analogues. Taken together, this research provides a promising chemotype for developing newer FtsZ-targeting bactericidal agents.
Synthesis method of substituted phenylhydrazine and salt thereof
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Paragraph 0133; 0136; 0137, (2017/08/29)
The invention relates to a novel synthesis method of substituted phenylhydrazine and salt thereof. A substituted phenyl diazene compound is reduced to generate the substituted phenylhydrazine; a reducing agent B is selected from one or several of a catalytic hydrogenating system, formic acid, formate and formic acid ester compound; the obtained substituted phenylhydrazine can be further acidified to prepare the substituted phenylhydrazine salt which is easily stored and transported. The synthesis method has the advantages that the yield rate is high, the cost is low, the reaction time is short, the technology operation and post-treatment are simple, and the amount of waste water, waste gas and waste residue is fewer; the component of the produced waste water is single, the recycling is convenient, the treatment cost is low, and the green chemical requirement is met; the synthesis method of the substituted phenylhydrazine is more suitable for the large-scale industrialized production.
