61325-02-8Relevant articles and documents
Microwave-assisted synthesis of 2-aminothiophene derivatives via improved gewald reactions
Ruan, Bankang,Zhang, Zhiyan,Huang, Lei,Xu, Chao,Li, Luolan
, p. 2007 - 2018 (2021/09/29)
In this paper, a new and efficient method was developed to prepare 2-aminothiophene derivatives through improved Gewald reaction. Thirty-one final products were synthesized under microwave radiation for 30 min with 57%-95% isolated yields. All the product
Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease
Mugnaini, Claudia,Rabbito, Alessandro,Brizzi, Antonella,Palombi, Nastasja,Petrosino, Stefania,Verde, Roberta,Di Marzo, Vincenzo,Ligresti, Alessia,Corelli, Federico
, p. 239 - 251 (2018/10/24)
A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist 8g, showing the best balance between receptor affinity and selectivity, was tested in vitro in an experimental model of allergic contact dermatitis and proved to be able to block the release of MCP-2 in HaCaT cells at 10 μM concentration.
Photooxygenation of an amino-thienopyridone yields a more potent PTP4A3 inhibitor
Salamoun, Joseph M.,McQueeney, Kelley E.,Patil, Kalyani,Geib, Steven J.,Sharlow, Elizabeth R.,Lazo, John S.,Wipf, Peter
supporting information, p. 6398 - 6402 (2016/07/16)
The phosphatase PTP4A3 is an attractive anticancer target, but knowledge of its exact role in cells remains incomplete. A potent, structurally novel inhibitor of the PTP4A family was obtained by photooxygenation of a less active, electron-rich thienopyrid