82072-23-9Relevant articles and documents
Synthesis and evaluation of novel α-aminoamides containing benzoheterocyclic moiety for the treatment of pain
Cheng, Jingchao,He, Junlin,Ren, Fengxia,Ren, Fengzhi,Shi, Weiguo,Tong, Kun,Yu, Zixing,Zhang, Ruotian,Zhang, Tao,Zhang, Yatong
, (2021/06/15)
Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a, 6e, and 6f containing the benzofuran group displayed more potent in vivo analgesic activity than ralfinamide in both the formalin test and the writhing assay. Interestingly, they also exhibited potent in vitro anti-Nav 1.7 and anti-Nav 1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds 6a, 6e, and 6f, which have inhibitory potency for two pain-related Nav targets, could serve as new leads for the development of analgesic medicines.
Amide derivative containing benzoheterocycle structure, and composition and application thereof
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, (2020/06/17)
The invention belongs to the technical field of medicines, and discloses an amide derivative containing a benzoheterocycle structure, and a composition and an application thereof. The amide derivativecontaining the benzoheterocycle structure is a compound represented by structural formula I and a nontoxic pharmaceutically acceptable salt thereof, or the amide derivative containing the benzoheterocycle structure is a compound represented by structural formula II or a nontoxic pharmaceutically acceptable salt thereof. The amide derivative containing the benzoheterocycle structure has good analgesic activity and good inhibition effect on a target sodium ion channel Nav1.7.
Design, Synthesis, and Biological Evaluation of Novel Acylhydrazone Derivatives as Potent Neuraminidase Inhibitors
Li, Meng,Cheng, Li Ping,Pang, Wan,Zhong, Zhi Jian,Guo, Ling Ling
, p. 1745 - 1750 (2020/10/19)
Neuraminidase (NA) is an important target for current research on anti-influenza drugs. The acylhydrazone derivatives containing the -CONHN═CH- framework have been shown to have good NA inhibitory activity. In this paper, a series of novel acylhydrazone NA inhibitors (9a-9n) were designed and synthesized, and the inhibitory activities against NA were evaluated in vitro. The NA inhibition results showed that compound 9j has the most potent inhibitory activity (IC50 = 0.6 μM) against NA, which is significantly lower than that of the positive control oseltamivir carboxylic acid (OSC) (IC50 = 17.00 μM). Molecular docking analysis indicates that the acylhydrazone group plays an important role in compound 9j, which can bind well to the residues Arg371 and Arg292 in the S1 subsite of NA. The good potency of 9j may be also ascribed to the extending of morpholinyl ring into the 430-cavity. The results of this work may contribute to the development of more potent NA inhibitors to against mutant influenza viruses.