Using a structure based pharmacophore design, a weak inhibitor of RNase H, identified from a small library of two metal binding HIV-1 integrase inhibitors, was optimized for potency and physicochemical properties. This manuscript describes the SAR and in vivo DMPK for the pyridopyrimidinone class of inhibitors.
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Department of Pharmaceutical and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States. Electronic address:
Article Synopsis
- Researchers have identified calcium-dependent protein kinase 1 (CDPK1) in the protozoan responsible for cryptosporidiosis as a promising target for new therapies.
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Recent Advances and Outlook of Benzopyran Derivatives in the Discovery of Agricultural Chemicals.
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State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Scaffold structures, new mechanisms of action, and targets present enormous challenges in the discovery of novel pesticides. The discovery of new scaffolds is the basis for the continuous development of modern agrochemicals. Identification of a good scaffold such as triazole, carbamate, methoxy acrylate, pyrazolamide, pyrido-pyrimidinone mesoionic, and bisamide often leads to the development of a new series of pesticides.
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State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
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Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni- Suef, 62514, Egypt.
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