122849-72-3Relevant academic research and scientific papers
CONJUGATED CHEMICAL INDUCERS OF DEGRADATION AND METHODS OF USE
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, (2020/05/28)
The subject matter described herein is directed to antibody-CIDE conjugates (Ab-CIDEs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
Salidroside derivative, reparation method and application thereof in whitening cosmetics
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Paragraph 0040-0041; 0045-0047, (2020/04/17)
The invention discloses a salidroside derivative, a preparation method and application thereof in whitening cosmetics. The whitening activity of salidroside is enhanced; the protection effect of a salidroside sugar cycle is fully utilized; salidroside-plu
Discovery of KLS-13019, a Cannabidiol-Derived Neuroprotective Agent, with Improved Potency, Safety, and Permeability
Kinney, William A.,McDonnell, Mark E.,Zhong, Hua Marlon,Liu, Chaomin,Yang, Lanyi,Ling, Wei,Qian, Tao,Chen, Yu,Cai, Zhijie,Petkanas, Dean,Brenneman, Douglas E.
supporting information, p. 424 - 428 (2016/05/19)
Cannabidiol is the nonpsychoactive natural component of C. sativa that has been shown to be neuroprotective in multiple animal models. Our interest is to advance a therapeutic candidate for the orphan indication hepatic encephalopathy (HE). HE is a serious neurological disorder that occurs in patients with cirrhosis or liver failure. Although cannabidiol is effective in models of HE, it has limitations in terms of safety and oral bioavailability. Herein, we describe a series of side chain modified resorcinols that were designed for greater hydrophilicity and "drug likeness", while varying hydrogen bond donors, acceptors, architecture, basicity, neutrality, acidity, and polar surface area within the pendent group. Our primary screen evaluated the ability of the test agents to prevent damage to hippocampal neurons induced by ammonium acetate and ethanol at clinically relevant concentrations. Notably, KLS-13019 was 50-fold more potent and >400-fold safer than cannabidiol and exhibited an in vitro profile consistent with improved oral bioavailability.
Synthetic approaches to anti-inflammatory macrolactones of the oxacyclododecindione type
Tauber, Johannes,Rudolph, Kristina,Rohr, Markus,Erkel, Gerhard,Opatz, Till
, p. 3587 - 3608 (2015/06/08)
Abstract Various synthetic approaches to the oxacyclododecindione-type macrolactones, known for their potent anti-inflammatory activity, are presented. These include an attempted carbonylative ring closure, a hydroacylation route, and an approach by ring-
Total synthesis of (S)-(-)-curvularin: A ring-closing-metathesis-based construction of the macrocyclic framework
Mohapatra, Debendra K.,Rahaman, Hasibur,Pal, Rita,Gurjar, Mukund K.
scheme or table, p. 1801 - 1804 (2009/04/08)
A convergent, flexible, and efficient approach to the synthesis of curvularin is described. Key step is the high-yielding macrocyclic ring formation by ring-closing metathesis (RCM) using the Grubbs second-generation catalyst. Georg Thieme Verlag Stuttgar
Radical-mediated cyclisation of ω-aryl-β-dicarbonyl compounds to tetrahydrobenzocyclohepten-6-ones, hexahydrobenzocycloocten-6-ones and naphthalen-2(1H)-ones
Jamie, Joanne F.,Rickards, Rodney W.
, p. 3613 - 3621 (2007/10/03)
Manganese(III) acetate in acetic acid promotes efficient radical-mediated oxidative cyclisation of ε-aryl-β-dicarbonyl and Z-γ,δ-unsaturated δ-aryl-β-dicarbonyl compounds carrying electron-releasing groups in the aromatic ring, forming 6,7,8,9-tetrahydro-5H-benzocyclohepten-6-ones and naphthalen-2(1H)-ones, respectively. The process is accompanied by secondary acetoxylation at the activated benzylic position of the initial cyclisation products, and is exemplified by the conversions of the ε- and δ-aryl-β-dicarbonyl compounds 6 and 11 into the benzocycloheptenone 18 and the naphthalenone 21, respectively. Application of the oxidation to the formation of 8-membered hexahydro- and tetrahydro-benzocycloocten-6-ones 19 and 22 from ζ-aryl-β-dicarbonyl and Z-γ,δ-unsaturated ζ-aryl-β-dicarbonyl compounds is limited by low reactivity, and in the latter case, by radical rearrangement followed by cyclisation to a tetralin.
Depsidone synthesis. Part 24. The synthesis of epiphorellic acid 2. A pseudo-depsidone and x-ray crystal structure of a grisadienedione epoxide
Comber, Mark F.,Sargent, Melvyn V.,Skelton, Brian W.,White, Allan H.
, p. 441 - 448 (2007/10/02)
The synthesis of the unusual pseudo-depsidone epiphorellic acid 2 (2) {6-hydroxy-3-[5-hydroxy-2-methoxycarbonyl-3-(3-oxopentylphenoxy] -4-methoxy-2-pentylbenzoic acid} by a route involving grisadienedione-depsidone rearrangement and subsequent steps is de
