256373-91-8Relevant articles and documents
Synthesis of deuterium-labelled analogues of NLRP3 inflammasome inhibitor MCC950
Salla, Manohar,Butler, Mark S.,Massey, Nicholas L.,Reid, Janet C.,Cooper, Matthew A.,Robertson, Avril A.B.
, p. 793 - 795 (2018)
This study describes the syntheses of di, tetra and hexa deuterated analogues of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome inhibitor MCC950. In di and tetra deuterated analogues, deuteriums were incorporated into the 1,2,3,5,6,7-hexahydro-s-indacene moiety, whereas in the hexa deuterated MCC950 deuteriums were incorporated into the 2-(furan-3-yl)propan-2-ol moiety. The di deuterated MCC950 analogue was synthesised from 4-amino-3,5,6,7-tetrahydro-s-indacen-1(2H)-one 5. Tetra deuterated analogues were synthesised in 10 chemical steps starting with 5-bromo-2,3-dihydro-1H-inden-1-one 9, whereas the hexa deuterated analogue was synthesised in four chemical steps starting with ethyl-3-furoate 24. All of the compounds exhibited similar activity to MCC950 (IC50 = 8 nM). These deuterated analogues are useful as internal standards in LC-MS analyses of biological samples from in vivo studies.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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Page/Page column 266-267, (2020/06/10)
In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
Sulfonamide compound and medical applications thereof
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Paragraph 0056; 0058; 0060, (2019/02/13)
The invention discloses a compound containing a sulfonamide structure, a preparation method thereof, and medical applications of the compound, and more specifically discloses the compound with a structure represented by formula I, and a pharmaceutically acceptable salt or a prodrug or a solvate thereof. The compound is used for tumor treatment through inhibiting ATP-citrate lyase.