التفاصيل البيبلوغرافية
العنوان:
Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2
المؤلفون:
Andrew David Morley , Galith Karoutchi , Stefan Gerhardt , Attilla Ting , Chris De Savi , Nash Ian Alun , Ken Page
المصدر:
Bioorganic & Medicinal Chemistry Letters . 22:271-277
بيانات النشر:
Elsevier BV, 2012.
سنة النشر:
2012
مصطلحات موضوعية:
Models, Molecular , Zinc binding , Matrix metalloproteinase inhibitor , Chemistry, Pharmaceutical , Clinical Biochemistry , Pharmaceutical Science , Matrix Metalloproteinase Inhibitors , Biochemistry , Inhibitory Concentration 50 , Structure-Activity Relationship , Dogs , Matrix Metalloproteinase 13 , Osteoarthritis , Drug Discovery , Animals , Humans , Structure–activity relationship , Potency , Enzyme Inhibitors , Lead (electronics) , Molecular Biology , Chemistry , Organic Chemistry , Dosing regimen , Combinatorial chemistry , Rats , Bioavailability , Zinc , Models, Chemical , Solubility , Drug Design , Molecular Medicine , Selectivity
الوصف:
Directed screening has identified a novel series of non-zinc binding MMP13 inhibitors that possess good levels of activity whilst demonstrating excellent selectivity over related MMPs. A lead optimisation campaign has delivered compounds with enhanced MMP13 potency, good selectivity and acceptable bioavailability profiles leading to a predicted twice-a-day dosing regimen in man.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1edcdff0979b6502875d67bc0caf41a9 https://doi.org/10.1016/j.bmcl.2011.11.034
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....1edcdff0979b6502875d67bc0caf41a9
قاعدة البيانات:
OpenAIRE
