Lange, Jos H. M. published the artcileNovel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity, Recommanded Product: N-Methyl-N-isopropylsulfamoyl amide, the publication is Bioorganic & Medicinal Chemistry Letters (2005), 15(21), 4794-4798, database is CAplus and MEDLINE.
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 372136-76-0. 372136-76-0 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Amine,Aliphatic hydrocarbon chain, name is N-Methyl-N-isopropylsulfamoyl amide, and the molecular formula is C4H12N2O2S, Recommanded Product: N-Methyl-N-isopropylsulfamoyl amide.
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