Lange, Jos H. M.; Van Stuivenberg, Herman H.; Veerman, Willem; Wals, Henri C.; Stork, Bob; Coolen, Hein K. A. C.; McCreary, Andrew C.; Adolfs, Tiny J. P.; Kruse, Chris G. published the artcile< Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity>, Application In Synthesis of 25999-04-6, the main research area is aminosulfonyl isothiocyanate diarylpyrazoline addition; aminosulfonylcarbamoyl diarylpyrazoline preparation chlorination amination; diarylpyrazoline derivative cannabinoid CB1 receptor antagonist.
3,4-Diarylpyrazolines as potent CB1 receptor antagonists with lipophilicity lower than that of SLV319 are described. The key change was the replacement of the arylsulfonyl group in the original series by a dialkylaminosulfonyl moiety. The absolute configuration (4S) of enantiomer I was established by X-ray diffraction anal. and I showed a close mol. fit with rimonabant in a CB1 receptor-based model. II exhibited the highest CB1 receptor affinity (Ki = 24 nM) in this series, as well as very potent CB1 antagonistic activity (pA 2 = 8.8) and a high CB1/CB2 subtype selectivity (∼147-fold).
Bioorganic & Medicinal Chemistry Letters published new progress about Cannabinoid receptor 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Application In Synthesis of 25999-04-6.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics