277312-95-5Relevant academic research and scientific papers
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases
Hecker, Scott J.,Reddy, K. Raja,Lomovskaya, Olga,Griffith, David C.,Rubio-Aparicio, Debora,Nelson, Kirk,Tsivkovski, Ruslan,Sun, Dongxu,Sabet, Mojgan,Tarazi, Ziad,Parkinson, Jonathan,Totrov, Maxim,Boyer, Serge H.,Glinka, Tomasz W.,Pemberton, Orville A.,Chen, Yu,Dudley, Michael N.
supporting information, p. 7491 - 7507 (2020/08/21)
Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory to inhibition by agents recently introduced. Most important among these are the class B (metallo) enzyme NDM-1 of Enterobacteriaceae and the class D (OXA) enzymes
Synthesis and Evaluation of Ginkgolic Acid Derivatives as SUMOylation Inhibitors
Brackett, Christopher M.,García-Casas, Ana,Castillo-Lluva, Sonia,Blagg, Brian S. J.
supporting information, p. 2221 - 2226 (2020/12/17)
SUMOylation has emerged as an important post-translational modification that has been shown to modulate protein activity associated with various signaling pathways, and consequently, it has emerged as an important therapeutic target. While several natural products have been shown to inhibit enzymes involved in the SUMOylation process, there has been little progress toward the development of more selective and potent SUMOylation inhibitors. Ginkgolic acid was one of the first natural products discovered to inhibit the SUMO E1 enzyme. Despite its use to mechanistically investigate the SUMOylation process, ginkgolic acid also modulates other pathways as well. In this Letter, preliminary structure-activity relationships for ginkgolic acid as a SUMOylation inhibitor are presented.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0241, (2016/02/28)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0155; 0156, (2014/07/22)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
ARYL AND HETEROARYL FUSED LACTAMS
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Paragraph 0943; 0944, (2014/07/08)
This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
CHROMENE DERIVATIVES AND USE THEREOF AS HIF HYDROXYLASE ACTIVITY INHIBITORS
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Page/Page column 72, (2009/10/09)
The present invention relates to novel compounds of formula (I), methods, and compositions capable of decreasing HIF hydroxylase activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
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Page/Page column 27, (2010/02/11)
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
Dual inhibitors of adipocyte fatty acid binding protein and keratinocyte fatty acid binding protein
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Page 39, (2010/02/06)
Compounds that are dual aP2/k-FABP inhibitors are provided having the formula wherein A, B, X, Y, R1, R2 and R3 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing dual aP2/k-FABP inhibitors alone or in combination with at least one other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
