14108-81-7Relevant articles and documents
Discovery and evolution of 12N-substituted aloperine derivatives as anti-SARS-CoV-2 agents through targeting late entry stage
Wang, Kun,Wu, Jia-Jing,Xin–Zhang,Zeng, Qing-Xuan,Zhang, Na,Huang, Wei-Jin,Tang, Sheng,Wang, Yan-Xiang,Kong, Wei-Jia,Wang, You-Chun,Li, Ying-Hong,Song, Dan-Qing
, (2021/08/03)
So far, there is still no specific drug against COVID-19. Taking compound 1 with anti-EBOV activity as the lead, fifty-four 12N-substituted aloperine derivatives were synthesized and evaluated for the anti-SARS-CoV-2 activities using pseudotyped virus model. Among them, 8a exhibited the most potential effects against both pseudotyped and authentic SARS-CoV-2, as well as SARS-CoV and MERS-CoV, indicating a broad-spectrum anti-coronavirus profile. The mechanism study disclosed that 8a might block a late stage of viral entry, mainly via inhibiting host cathepsin B activity rather than directly targeting cathepsin B protein. Also, 8a could significantly reduce the release of multiple inflammatory cytokines in a time- and dose-dependent manner, such as IL-6, IL-1β, IL-8 and MCP-1, the major contributors to cytokine storm. Therefore, 8a is a promising agent with the advantages of broad-spectrum anti-coronavirus and anti-cytokine effects, thus worthy of further investigation.
Novel acetamide derivatives containing 3,4-dichlorophenyl group or pharmaceutically acceptable salts thereof, preparation method therof and pharmaceutical composition for use in preventing or treating Urotensin-Ⅱ receptor activity related diseases contain
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Paragraph 0181; 0182; 0183; 0184, (2017/01/02)
The present invention relates to an acetamide derivative including a 3,4-dichlrophenyl group, or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient for
Development of potent and selective small-molecule human Urotensin-II antagonists
McAtee, John J.,Dodson, Jason W.,Dowdell, Sarah E.,Girard, Gerald R.,Goodman, Krista B.,Hilfiker, Mark A.,Sehon, Clark A.,Sha, Deyou,Wang, Gren Z.,Wang, Ning,Viet, Andrew Q.,Zhang, Daohua,Aiyar, Nambi V.,Behm, David J.,Carballo, Luz H.,Evans, Christopher A.,Fries, Harvey E.,Nagilla, Rakesh,Roethke, Theresa J.,Xu, Xiaoping,Yuan, Catherine C.K.,Douglas, Stephen A.,Neeb, Michael J.
scheme or table, p. 3500 - 3503 (2009/04/16)
This work describes the development of potent and selective human Urotensin-II receptor antagonists starting from lead compound 1, (3,4-dichlorophenyl)methyl{2-oxo-2-[3-phenyl-2-(1-pyrrolidinylmethyl)-1-piperidinyl]ethyl}amine. Several problems relating to oral bioavailability, cytochrome P450 inhibition, and off-target activity at the kappa opioid receptor and cardiac sodium channel were addressed during lead development. hUT binding affinity relative to compound 1 was improved by more than 40-fold in some analogs, and a structural modification was identified which significantly attenuated both off-target activities.