Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies was written by Frett, Brendan;McConnell, Nick;Wang, Yuanxiang;Xu, Zhigang;Ambrose, Andrew;Li, Hong-yu. And the article was included in MedChemComm in 2014.Product Details of 59669-59-9 This article mentions the following:
Trk receptors play a key role in the development and maintenance of neuronal networks. Recent evidence suggests that the Trk family, specifically TrkA, is an important driver for tumor growth, inflammatory and neuropathic pain, and chemoresistance. Through a computational screen, a novel Trk active pharmacophore was identified and a series of pyrazine-based inhibitors were developed, which potently inhibited TrkA. Inhibitors displayed the highest activity on TrkA when screened against a small, tyrosine kinase panel and also exhibited a non-linear SAR. Predicted binding modes of the inhibitors were examined, which identified exploitable regions for future development of more advanced inhibitors. In the experiment, the researchers used many compounds, for example, 3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9Product Details of 59669-59-9).
3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9) belongs to isoxazole derivatives. Isoxazoles present in various natural products and synthetic compounds of biological importance like antibacterial, antagonists, antiinflammatory, analgesics, and also show the applications in functional materials. The electrophilic cyclization of various 2-alkynone O-methyl oximes with a wide range of substrates such as ICl, I2, Br2, PhSeBr, etc. provides a variety of 3,4,5-trisubstituted isoxazoles in good to excellent yields.Product Details of 59669-59-9
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem