71025-26-8Relevant articles and documents
5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2)
Bursavich, Matthew G.,Gilbert, Adam M.,Lombardi, Sabrina,Georgiadis, Katy E.,Reifenberg, Erica,Flannery, Carl R.,Morris, Elisabeth A.
, p. 5630 - 5633 (2008/03/14)
5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. Selected compounds 23, 33-35 show sub-micromolar ADAMTS-5 potency and strong SAR trends with selectivity over the related metalloproteases ADAMTS-4 (Aggrecanase-1), MMP12, and MMP13. This series of compounds represents progress toward a selective ADAMTS-5 inhibitor as a disease modifying osteoarthritis drug.
Antibacterial 1-normon-2-yl-heterocyclic compounds
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, (2008/06/13)
Compounds of formula (I): STR1 wherein STR2 is a 5-membered heterocyclic group having a 6-?electron system, the five ring atoms being either (a) one carbon atom and four atoms selected from carbon and nitrogen, (b) two carbon atoms, two nitrogen atoms and one atom selected from oxygen and sulphur, or (c) four carbon atoms and one atom selected from oxygen and sulphur and R1 is a substituent on a carbon or nitrogen of STR3 selected from C1-20 alkyl, C2-8 alkenyl aryl, aralkyl and heterocyclyl, each of which may optionally be substituted; hydrogen and C3-7 cycloalkyl, and, where appropriate, R2 is a substituent on a carbon or nitrogen of STR4 and when present is the same or different to R1 and is selected from C1-20 alkyl, C2-8 alkenyl, aryl, aralkyl and heterocyclyl each of which may optionally be substituted; hydrogen and C3-7 cycloalkyl, have antibacterial and antimycoplasmal activity.
