کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1224442 967922 2006 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Rationalization of physicochemical characters of 1,5-diarylpyrazole analogs as dual (COX-2/LOX-5) inhibitors: A QSAR approach
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
Rationalization of physicochemical characters of 1,5-diarylpyrazole analogs as dual (COX-2/LOX-5) inhibitors: A QSAR approach
چکیده انگلیسی

Arachidonic acid metabolizing enzymes cyclooxygenases and lipoxygenases lead to the formation of various eicosanoids involved in variety of human diseases, like inflammation, fever, pain, rheumatic and osteoarthritis, etc. Non-steroidal anti-inflammatory drugs are useful tools in the treatment of prostaglandin mediated complications. The development of dual inhibitors may prevent a drift of arachidonic acid metabolism towards the other pathway, leading to potential side effects. Hence emphasis was focused on quantification of structure–activity relationship, with a view to delineating the influence of key COX-2/LOX-5 activity, to explore structural insights to aid the designing of safer dual inhibitors. The quantification of the structural features of 1,5-diarylpyrazole analogs with various biological activities gave some important structural insights, i.e. Hy (hydrophilic factor) and Mor17v (3D molecular representation of structure based on electron diffraction code). These two physicochemical properties may be helpful in development of more selective dual COX-2/LOX-5 inhibitors.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 42, Issue 2, 18 September 2006, Pages 283–289
نویسندگان
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