40598-66-1Relevant academic research and scientific papers
Discovery of a Series of Indazole TRPA1 Antagonists
Pryde, David C.,Marron, Brian E.,West, Christopher W.,Reister, Steven,Amato, George,Yoger, Katrina,Antonio, Brett,Padilla, Karen,Cox, Peter J.,Turner, Jamie,Warmus, Joseph S.,Swain, Nigel A.,Omoto, Kiyoyuki,Mahoney, John H.,Gerlach, Aaron C.
, p. 666 - 671 (2017)
A series of TRPA1 antagonists is described which has as its core structure an indazole moiety. The physical properties and in vitro DMPK profiles are discussed. Good in vivo exposure was obtained with several analogs, allowing efficacy to be assessed in rodent models of inflammatory pain. Two compounds showed significant activity in these models when administered either systemically or topically. Protein chimeras were constructed to indicate compounds from the series bound in the S5 region of the channel, and a computational docking model was used to propose a binding mode for example compounds.
Synthesis of N-aryl-3H-indazol-3-imine and N-aryl-1H-indazol-3-amine via Na2WO4/H2O2 mediated by intramolecular N–N coupling
Sajadi, Mahdieh Sadat,Darehkordi, Ali,Hosseini, Seyed Mohammad Sadegh
, (2021/03/01)
A fast and convenient method for synthesis of N-aryl-1H-indazol-3-amine and N-aryl-3H-indazol-3-imine compounds has been described via intramolecular oxidative cyclization of the 2-amino-Nˊ-arylbenzimidamide intermediates by Na2WO4/H2O2 in excellent yields. This procedure has several advantages such as mild reaction conditions, short reaction time, and excellent yields, making this methodology practical.
