Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors
عرض / فتح
التاريخ
2016المؤلف
Hammuda, ArwaShalaby, Raed
Rovida, Stefano
Edmondson, Dale E.
Binda, Claudi
Khalil, Ashraf
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البيانات الوصفية
عرض كامل للتسجيلةالملخص
A novel series of substituted chalcones were designed and synthesized to be evaluated as selective human MAO-B inhibitors. A combination of either methylsulfonyl or trifluoromethyl substituents on the aromatic ketone moiety with a benzodioxol ring on the other end of the chalcone scaffold was investigated. The compounds were tested for their inhibitory activities on both human MAO-A and B. All compounds appeared to be selective MAO-B inhibitors with Ki values in the micromolar to submicromolar range. Molecular modeling studies have been performed to get insight into the binding mode of the synthesized compounds to human MAO-B active site. 2016 Elsevier Masson SAS. All rights reserved.
المجموعات
- أبحاث الصيدلة [1234 items ]
وثائق ذات صلة
عرض الوثائق المتصلة بواسطة: العنوان، المؤلف، المنشئ والموضوع.
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