445378-38-1Relevant academic research and scientific papers
Synthesis of pyranonaphthoquinone antibiotics involving the phthalide annulation strategy
Claessens, Sven,Naidoo, Dashnie,Mulholland, Dulcie,Verschaeve, Luc,Van Staden, Johannes,De Kimpe, Norbert
, p. 621 - 623 (2006)
The synthesis of the pyranonaphthoquinone antibiotic pentalongin was performed using the phthalide annulation strategy. Annulation of the cyanophthalide onto 6H-pyran-3-one resulted in a hongconin analogue, which upon further elaboration was converted into the natural product. Georg Thieme Verlag Stuttgart.
Discovery of a Cyclic Choline Analog That Inhibits Anaerobic Choline Metabolism by Human Gut Bacteria
Bollenbach, Maud,Ortega, Manuel,Orman, Marina,Drennan, Catherine L.,Balskus, Emily P.
, p. 1980 - 1985 (2020)
The anaerobic conversion of choline to trimethylamine (TMA) by the human gut microbiota has been linked to multiple human diseases. The potential impact of this microbial metabolic activity on host health has inspired multiple efforts to identify small molecule inhibitors. Here, we use information about the structure and mechanism of the bacterial enzyme choline TMA-lyase (CutC) to develop a cyclic choline analog that inhibits the conversion of choline to TMA in bacterial whole cells and in a complex gut microbial community. In vitro biochemical assays and a crystal structure suggest that this analog is a competitive, mechanism-based inhibitor. This work demonstrates the utility of structure-based design to access inhibitors of radical enzymes from the human gut microbiota.
Highly enantioselective Cu-catalyzed conjugate additions of dialkylzinc reagents to unsaturated furanones and pyranones: Preparation of air-stable and catalytically active Cu-peptide complexes
Brown, M. Kevin,Degrado, Sylvia J.,Hoveyda, Amir H.
, p. 5306 - 5310 (2005)
(Chemical Equation Presented) The first generally effective method for catalytic asymmetric conjugate addition (ACA) of dialkylzinc reagents to unsaturated furanones and pyranones (see scheme) with different steric and electronic properties is reported. S
An air-stable, reusable, bimetallic version of Grubbs' catalyst for alkene metathesis
Maishal, Tarun K.,Sarkar, Amitabha
, p. 1925 - 1927 (2002)
RCM, cross-metathesis and ring-opening cross-metathesis are efficiently catalyzed by a new, air-stable, bimetallic analog of Grubbs' Ru-based metathesis catalyst, which can be recovered and recycled.
CYCLIC MOLECULES AS BRUTON'S TYROSINE KINASE INHIBITOR
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Paragraph 0270; 0275-0276, (2021/11/26)
The present invention relates to a novel molecule with protein tyrosine kinase inhibitory activity, and the synthesis and usage thereof. Specifically, the present invention relates to compound by formula A, pharmaceutically acceptable salts, hydrates or solvates thereof, and the synthesis and usage thereof.
TRICYCLIC MODULATORS OF PP2A
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Page/Page column 207-208; 211, (2021/09/04)
Chemical modulators of PP2A, comprising tricyclic sulfonimidamides are disclosed. The compounds are useful in preventing or treating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease and cardiac hypertrophy. The compounds are of formula (I)
CHOLINE METABOLISM INHIBITORS
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Page/Page column 50; 105-106, (2020/07/05)
The present disclosure relates to compounds, compositions and methods for inhibiting choline metabolism, e.g., conversion of choline to trimethylamine. Disclosed herein are compounds, compositions, and methods for inhibiting choline metabolism, e.g., conversion of choline to TMA. Also disclosed herein are compounds, methods and compositions for inhibiting choline metabolism by gut microbiota resulting in reduction in the formation of trimethylamine (TMA) and trimethylamine N-oxide (TMAO).
Guanidine–Copper Complex Catalyzed Allylic Borylation for the Enantioconvergent Synthesis of Tertiary Cyclic Allylboronates
Ge, Yicen,Cui, Xi-Yang,Tan, Siu Min,Jiang, Huan,Ren, Jingyun,Lee, Nicholas,Lee, Richmond,Tan, Choon-Hong
supporting information, p. 2382 - 2386 (2019/02/01)
An enantioconvergent synthesis of chiral cyclic allylboronates from racemic allylic bromides was achieved by using a guanidine–copper catalyst. The allylboronates were obtained with high γ/α regioselectivities (up to 99:1) and enantioselectivities (up to 99 % ee), and could be further transformed into diverse functionalized allylic compounds without erosion of optical purity. Experimental and DFT mechanistic studies support an SN2′ borylation process catalyzed by a monodentate guanidine–copper(I) complex that proceeds through a special direct enantioconvergent transformation mechanism.
THERAPEUTIC COMPOUNDS
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Paragraph 0546, (2014/09/17)
Compounds of formula (I) or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and thera
SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Page/Page column 79, (2012/11/07)
Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
