Selective CB2 receptor agonists. Part 3: The optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model was written by Bartolozzi, Alessandra;Cirillo, Pier Francesco;Berry, Angela K.;Hickey, Eugene R.;Thomson, David S.;Wu, Lifen;Zindell, Renee;Albrecht, Claudia;Ceci, Angelo;Gemkow, Mark J.;Nagaraja, Nelamangala V.;Romig, Helmut;Sauer, Achim;Riether, Doris. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.Category: isoxazole This article mentions the following:
A novel class of potent cannabinoid receptor 2 (CB2) agonists based on a (S)-piperidine scaffold was identified using ligand-based pharmacophore models. Optimization of solubility and metabolic stability led to the identification of several potent CB2 agonists, e.g. I, that displayed selectivity over cannabinoid receptor 1 (CB1) and acceptable drug like properties. In rats, compound 30 demonstrated a favorable pharmacokinetic profile and efficacy in a Streptozotocin-induced diabetic neuropathy model, with full reversal of mech. hyperalgesia. In the experiment, the researchers used many compounds, for example, 3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9Category: isoxazole).
3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9) belongs to isoxazole derivatives. Isoxazole rings are found in some natural products, such as ibotenic acid and muscimol. The most common methods for N–O bond cleavage in isoxazoles are hydrogenation with palladium or platinum catalysts or with Raney Ni. Recent developments have shown that Mo(CO)6 efficiently cleaves the N–O bond in isoxazoles.Category: isoxazole
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem