By Neera Borkakoti (auth.), Kevin M. K. Bottomley, Dr. David Bradshaw, Dr. John S. Nixon (eds.)
ISBN-10: 3034886667
ISBN-13: 9783034886666
ISBN-10: 3034897243
ISBN-13: 9783034897242
This quantity describes contemporary examine within the box of metalloproteinases (a kin of enzymes that could catalyze tissue degradation), specifically their participation in autoimmune illnesses corresponding to rheumatoid arthritis, reviewing the newest advancements in metalloproteinase inhibitor layout and the present prestige of medical applicants. This quantity is meant not just for these energetic in examine into metalloproteinases but additionally for people with an curiosity in inflammatory ailments. hence it addresses either educational and business researchers.
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Additional resources for Metalloproteinases as Targets for Anti-Inflammatory Drugs
Example text
BAY 129566 is presently undergoing clinical trials for the treatment of cancer. Constraining C-2 and C-3 of the biarylbutyric acids in a five-membered ring also yields highly active MMP inhibitors, though there is no significant enhancement of in vitro activity over the acyclic compounds (80 vs. 83). In a guinea pig partial medial menisectomy model of osteoarthritis a 15 mg/kg/day oral dose of carboxylic acids 79, 80 and 84 inhibited the formation of femoral surface lesions by 46%,53% and 31 %, respectively.
Skotnicki et al. 6 compounds with an ether linkage between the Pl' phenyl rings are somewhat less selective. Within the sulfone-hydroxamic acid class of MMP inhibitor, the linker between the sulfone and hydroxamic acid moieties has been extended to three carbons without significant loss in potency [45]. Monsanto has disclosed sulfone-based MMP inhibitors which are among the first non-peptide inhibitors that utilize a thiol as the zinc chelator rather than a hydroxamic acid or carboxylic acid (Tab.
Thus, AG3340 is much more soluble at low pH, and less protein bound. ) and metabolic stability (human microsomes) are each 5-10-fold better than those of AG3319. Pharmacokinetic data and Lewis lung carcinoma (LLC) studies in rats and mice have been reported for compounds 55 and 59 and four additional congeners. Thiomorpholine 59 (AG3340) was the most active of these compounds in a mouse LLC model [30]. 29 Jerauld S. Skotnicki et al. 7 101 A series of achiral hexahydro-pyrimidines have been shown to be potent inhibitors of MMP-3 and MMP-9 (Tab.
Metalloproteinases as Targets for Anti-Inflammatory Drugs by Neera Borkakoti (auth.), Kevin M. K. Bottomley, Dr. David Bradshaw, Dr. John S. Nixon (eds.)
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