Inhibitors of HIV-1 attachment. Part 7: Indole-7-carboxamides as potent and orally bioavailable antiviral agents was written by Yeung, Kap-Sun;Qiu, Zhilei;Xue, Quifen;Fang, Haiquan;Yang, Zheng;Zadjura, Lisa;D’Arienzo, Celia J.;Eggers, Betsy J.;Riccardi, Keith;Shi, Pei-Yong;Gong, Yi-Fei;Browning, Marc R.;Gao, Qi;Hansel, Steven;Santone, Kenneth;Lin, Ping-Fang;Meanwell, Nicholas A.;Kadow, John F.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2013.Name: 1-Ethyl-1H-pyrazol-5-amine This article mentions the following:
A series of substituted carboxamides at the indole C7 position of the previously described 4-fluoro-substituted indole HIV-1 attachment inhibitor I was synthesized and the SAR delineated. Heteroaryl carboxamide inhibitors that exhibited pM potency in the primary cell-based assay against a pseudotype virus expressing a JRFL envelope were identified. The simple Me amide analog II displayed a promising in vitro profile, with its favorable HLM stability and membrane permeability translating into favorable pharmacokinetic properties in preclin. species. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Name: 1-Ethyl-1H-pyrazol-5-amine).
1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities.Name: 1-Ethyl-1H-pyrazol-5-amine
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics