Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists.

Fragment-based Binding Efficiency Indices in Bioactive Molecular Design: A Computational Approach to BACE-1 Inhibitors

One of the most important targets in Alzheimer disease is Beta site amyloid precursor protein cleaving enzyme-1 (BACE-1). It is a membrane associated protein and is one of the main enzymes responsible for amyloid β (Aβ) production. Up to now, a considerable number of peptidic and non-peptidic inhibitors of BACE-1 have been developed. Recently, small molecule BACE-1 inhibitors have attracted the...

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Fragment-based Binding Efficiency Indices in Bioactive Molecular Design: A Computational Approach to BACE-1 Inhibitors

One of the most important targets in Alzheimer disease is Beta site amyloid precursor protein cleaving enzyme-1 (BACE-1). It is a membrane associated protein and is one of the main enzymes responsible for amyloid β (Aβ) production. Up to now, a considerable number of peptidic and non-peptidic inhibitors of BACE-1 have been developed. Recently, small molecule BACE-1 inhibitors have attracted the...

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Pharmacokinetics Applications of Traditional Chinese Medicines

Traditional Chinese medicine (TCM) has been widely used in many oriental countries for thousands of years and played an indispensable role in the prevention and treatment of diseases, especially the complicated and chronic ones. It is a very complex mixture containing hundreds or thousands of different components. Pharmacokinetic study on active constituents in TCM preparations is a good way fo...

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Synthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity

In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...

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Synthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity

In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...

متن کامل

Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists.

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Fragment-based Binding Efficiency Indices in Bioactive Molecular Design: A Computational Approach to BACE-1 Inhibitors

Fragment-based Binding Efficiency Indices in Bioactive Molecular Design: A Computational Approach to BACE-1 Inhibitors

Pharmacokinetics Applications of Traditional Chinese Medicines

Synthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity

Synthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity

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