- Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors
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FTO catalyzes the Fe(II) and 2-oxoglutarate (2OG)-dependent modification of nucleic acids, including the demethylation of N6-methyladenosine (m6A) in mRNA. FTO is a proposed target for anti-cancer therapy. Using information from crystal structures of FTO
- Aik, Wei Shen,Brown, Tom,Clunie-O'Connor, Caitlin,Demetriades, Marina,El-Sagheer, Afaf H.,Leissing, Thomas M.,Leung, Ivanhoe K. H.,Maheswaran, Pratheesh,McDonough, Michael A.,Ng, Yi Min,Salah, Eidarus,Schofield, Christopher J.,Shishodia, Shifali,Tam, Nok Yin,Tumber, Anthony,Zhang, Dong
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p. 16609 - 16625
(2021/11/24)
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- Design and synthesis of florylpicoxamid, a fungicide derived from renewable raw materials
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The design and synthesis of the broad-spectrum fungicide, florylpicoxamid, embodies multiple Green Chemistry principles. The active ingredient was strategically designed to deliver maximum biological activity and rapidly degrade after application to minimize its enviromental impact. Unlike many chiral crop protection chemicals, florylpicoxamid was purposely developed as a single stereoisomer to minimize the dose rate of this product in field applications and avoid any potential environmental burdens of its less active stereoisomers. Fortunately, the most efficacious stereoisomer of the natural product-inspired active ingredient can be derived from the natural antipodes of lactic acid and alanine. The principles of Green Chemistry were also used to improve the synthetic route originally developed for structure-activity relationship studies, resulting in a convergent stereoselective synthesis that is more sustainable and cost-effective. The streamlined 2ndgeneration route decreases the use of protecting groups and utilizes safer reaction solvents. Development of a novel synthetic sequence to the 2,3,4-trisubstituted pyridine motif from furfural further increased the renewable carbon content of the active ingredient to nearly 50%. Throughout process development, improved reaction conditions and industrially-preferred alternatives were identified to replace hazardous reagents for key transformations. In all, the holistic use of Green Chemistry principles in the design and synthesis of florylpicoxamid will provide farmers with a highly sustainable product for crop disease management.
- Babij, Nicholas R.,Choy, Nakyen,Cismesia, Megan A.,Couling, David J.,Hough, Nicole M.,Johnson, Peter L.,Klosin, Jerzy,Li, Xiaoyong,Lu, Yu,McCusker, Elizabeth O.,Meyer, Kevin G.,Renga, James M.,Rogers, Richard B.,Stockman, Kenneth E.,Webb, Nicola J.,Whiteker, Gregory T.,Zhu, Yuanming
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supporting information
p. 6047 - 6054
(2020/10/18)
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- HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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The invention relates to a novel heterocyclic compound inhibiting a cyclin-dependent kinase (CDK) and a pharmaceutical composition comprising the same as an effective ingredient. The heterocyclic compound according to the present invention or pharmaceutically acceptable salt thereof can be effectively used in treating or preventing cancers, degenerative brain diseases, etc.
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Paragraph 0141; 0142
(2018/01/11)
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- PYRAZOLE DERIVATIVE
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Provided are a compound expressed by formula (I) or a pharmacologically permissible salt thereof, as well as a drug or drug composition that contains this compound as an active ingredient, having a xanthine oxidase inhibiting effect that is very useful fo
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Paragraph 0168
(2016/03/05)
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- TANK-BINDING KINASE INHIBITOR COMPOUNDS
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Compounds having the following formula (I) and methods of their use and preparation are disclosed:
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Page/Page column 64
(2015/12/24)
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- CONDENSED TRICLYCLIC COMPOUNDS AS INHIBITORS OF HIV REPLICATION
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Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted -(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inbitor of HIV replication.
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Page/Page column 44
(2013/07/05)
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- FUSED FURAN COMPOUND
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The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and , R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
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Page/Page column 143
(2008/06/13)
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