81574-69-8Relevant academic research and scientific papers
Construction of Enantiopure Taxoid and Natural Product-like Scaffolds Using a C-C Bond Cleavage/Arylation Reaction
Weber, Manuel,Owens, Kyle,Masarwa, Ahmad,Sarpong, Richmond
, p. 5432 - 5435 (2015)
An approach to construct enantiopure complex natural product-like frameworks, including the first reported synthesis of a C17 oxygenated taxoid scaffold, is presented. A palladium-catalyzed C-C activation/cross-coupling is utilized to access these structu
Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors: Optimization of Whole-Cell Anticryptococcal Activity and Insights into the Structural Origins of Cryptococcal Selectivity
Marcyk, Paul T.,Leblanc, Emmanuelle V.,Kuntz, Douglas A.,Xue, Alice,Ortiz, Francisco,Trilles, Richard,Bengtson, Stephen,Kenney, Tristan M. G.,Huang, David S.,Robbins, Nicole,Williams, Noelle S.,Krysan, Damian J.,Privé, Gilbert G.,Whitesell, Luke,Cowen, Leah E.,Brown, Lauren E.
, p. 1139 - 1169 (2021/02/01)
The essential eukaryotic chaperone Hsp90 regulates the form and function of diverse client proteins, many of which govern thermotolerance, virulence, and drug resistance in fungal species. However, use of Hsp90 inhibitors as antifungal therapeutics has be
Reinvestigating the acyl cyclization to the precursor of diptoindonesin G
Li, Nan-Sheng,Greene, Geoffrey L.
supporting information, (2021/03/29)
We reinvestigated the synthesis of the precursor of diptoindonesin G (2) by the intramolecular acyl cyclization of compound 1 or compound 3 in the presence of trifluoroacetic anhydride (TFAA) [1,2]. Although the reaction of 3 with TFAA generated 2 smoothl
Method for preparing apabetalone, intermediates and preparation method of intermediates
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Paragraph 0061-0066, (2020/05/30)
The invention provides a preparation method of apabetalone. The preparation method comprises the step of reacting a first intermediate, namely 2-bromo-4,6-dimethoxybenzoic acid with a second intermediate, namely 4-(2-hydroxyethoxy)-3,5-dimethylbenzamidine hydrochloride in an alkali-containing organic solvent under the action of a catalyst so as to obtain apabetalone. According to the invention, total yield is 33.4% or above, raw materials are easy to obtain, process is simple, reaction conditions are mild, post-treatment method is simple, the yield of each step and the total yield are high, and cost can be reduced. Apabetalone is a medicine for treating cardiovascular diseases such as atherosclerosis and the like, and has good application prospects. The invention also provides the intermediate 4-(2-hydroxyethoxy)-3,5-dimethylbenzamidine hydrochloride for synthesizing apabetalone and a preparation method thereof, and a preparation method of the compound 2-bromo-4,6-dimethoxybenzoic acid.
AROMATIC DERIVATIVES, PREPARATION METHODS, AND MEDICAL USES THEREOF
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Paragraph 0192, (2020/09/19)
The present disclosure relates generally to aromatic derivatives that are inhibitors of FGFR4 and are useful in treating FGFR4-associated diseases or conditions. Compositions containing the compounds of the present disclosure are also provided.
Synthesis and pharmacological evaluation of childinin E and several derivatives as anti-hyphal formation inhibitors against Candida albicans
Hirata, Momoka,Kamauchi, Hitoshi,Sugita, Yoshiaki,Takao, Koichi
supporting information, (2020/11/12)
The natural highly substituted benzophenone childinin E (1) was previously isolated from the fungus Daldinia childiae. Here we describe the total synthesis of childinin E and several derivatives using a linear seven-step sequence. The antifungal propertie
HSP90 INHIBITORS AND USES THEREOF
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Paragraph 00476-00478, (2020/11/23)
Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related deseases.
Design and Synthesis of Metabolically Stable tRNA Synthetase Inhibitors Derived from Cladosporin
Rusch, Marion,Thevenon, Arnaud,Hoepfner, Dominic,Aust, Thomas,Studer, Christian,Patoor, Maude,Rollin, Patrick,Livendahl, Madeleine,Ranieri, Beatrice,Schmitt, Esther,Spanka, Carsten,Gademann, Karl,Bouchez, Laure C.
, p. 644 - 649 (2019/02/13)
Selective and specific inhibitors of Plasmodium falciparum lysyl-tRNA synthetase represent promising therapeutic antimalarial avenues. Cladosporin was identified as a potent P. falciparum lysyl-tRNA synthetase inhibitor, with an activity against parasite
Convergent synthesis of diptoindonesin G
Singh, Dileep Kumar,Kim, Ikyon
supporting information, p. 300 - 301 (2019/01/04)
A convergent and scalable synthetic route to a tetracyclic oligostilbenoid natural product, diptoindonesin G, is described where Suzuki-Miyaura cross-coupling and intramolecular Friedel-Crafts acylation were employed to construct the central C ring of dip
Drug compound for treating hepatopathy and application thereof
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Paragraph 0307-0309, (2019/10/15)
The invention discloses a drug compound for treating hepatopathy and application thereof. The drug compound specifically serves as a compound shown in general formula (I) or an optical isomer or a pharmaceutically-acceptable salt of the compound. The compound or the optical isomer or the pharmaceutically-acceptable salt of the compound has a good curative effect and low toxicity on hepatopathy, especially fatty liver. Experiments show that the compound has an obvious protective effect on zebrafish nonalcoholic fatty liver, so that the drug compound has a good application prospect in medicinesfor treatment or prevention of hepatopathy, especially fatty liver or liver fibrosis or liver cirrhosis.
