32752-54-8Relevant articles and documents
Photoaffinity labeling of rat steroid 5α-reductase (isozyme-1) by a benzophenone derivative of a 4-methyl-4-azasteroid
Taylor, Matthew F.,Bhattacharyya, Anjan K.,Rajagopalan, Krishnan,Hiipakka, Richard,Liao, Shutsung,Collins, Delwood C.
, p. 323 - 331 (1996)
[1,2-3H]N-4(Benzylbenzoyl)-3-oxo-4-aza-4-methyl-5α-androstane-17β- carboxamide ([3H]-4MABP) has been synthesized as a photoaffinity probe of the steroid 5α-reductase isozyme-1 (5αR-1). Reversible binding of the probe to 5αR-1 in microsomal preparations yielded a reversible dissociation constant (K(d)) of ~3 nM, whereas inhibition experiments indicated that the probe had a 50% inhibition concentration of 4.4 nM and was a competitive inhibitor of the enzyme (K(i) ? 3 nM) with respect to testosterone. SDS- PAGE analysis of microsomal, detergent-solubilized, and (6.5%) polyethylene glycol-precipitated fractions of 5αR-1 photolyzed with [3H]4MABP in the presence of NADPH showed that the radioactivity was incorporated into a single protein band with a mass of 26 kDa (apparent molecular weight of 5αR- 1). UV photolysis was accompanied by an irreversible loss in enzyme activity, consistent with its covalent modification. Increasing the time of UV irradiation and concentration of [3H]4MABP indicated that the half-life and apparent K(d) for its photo insertion were ~3 min and 7.5 nM, respectively. Photolysis in the presence of a 20-fold excess of N,N-diethyl-4-aza-4- methyl-3-oxo-5α-androstune-17β-carboxamide or the 3-carboxysteroid SKF- 105111 resulted in partial protection of 5αR-1 from the probe, whereas minimal incorporation of radioactivity was observed in the absence of NADPH or in the presence of NADP+. The results indicated that [3H]4MABP is an effective probe of the steroid (D-ring) binding domain of 5αR-1.
Development of a photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor
Davie, Briana J.,Sexton, Patrick M.,Capuano, Ben,Christopoulos, Arthur,Scammells, Peter J.
, p. 902 - 907 (2014)
The field of G protein-coupled receptor drug discovery has benefited greatly from the structural and functional insights afforded by photoactivatable ligands. One G protein-coupled receptor subfamily for which photoactivatable ligands have been developed is the muscarinic acetylcholine receptor family, though, to date, all such ligands have been designed to target the orthosteric (endogenous ligand) binding site of these receptors. Herein we report the synthesis and pharmacological investigation of a novel photoaffinity label, MIPS1455 (4), designed to bind irreversibly to an allosteric site of the M1 muscarinic acetylcholine receptor; a target of therapeutic interest for the treatment of cognitive deficits. MIPS1455 may be a valuable molecular tool for further investigating allosteric interactions at this receptor.
Surfaces and coating compositions having antifouling, antithrombotic, and antibacterial properties and methods of making
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Paragraph 0215-0216, (2020/11/23)
Coating compositions, coated articles including the coating compositions, and methods of making the coating compositions and coated articles are provided. In some aspects, the coating compositions areapplied to a substrate having nitric oxide-releasing properties. The coating compositions can include copolymers having crosslinking agents that can be activated with mild UV light (about 345 nm to 365 nm) to avoid damaging the substrate while creating strong covalent bonds to the substrate. The copolymers can include hydrophilic repeat units, and in particular zwitterionic repeat units such as repeat units containing phosphorylcholine groups. In some aspects, the coating compositions are applied to a surface of a polymer substrate, wherein the polymer substrate had nitric oxide releasing properties. The coating compositions and the coated articles can have antifouling, antithrombotic, and/or antibacterial properties.
Visible Light-Catalyzed Benzylic C-H Bond Chlorination by a Combination of Organic Dye (Acr+-Mes) and N-Chlorosuccinimide
Xiang, Ming,Zhou, Chao,Yang, Xiu-Long,Chen, Bin,Tung, Chen-Ho,Wu, Li-Zhu
, p. 9080 - 9087 (2020/08/14)
By combining "N-chlorosuccinimide (NCS)"as the safe chlorine source with "Acr+-Mes"as the photocatalyst, we successfully achieved benzylic C-H bond chlorination under visible light irradiation. Furthermore, benzylic chlorides could be converted to benzylic ethers smoothly in a one-pot manner by adding sodium methoxide. This mild and scalable chlorination method worked effectively for diverse toluene derivatives, especially for electron-deficient substrates. Careful mechanistic studies supported that NCS provided a hydrogen abstractor "N-centered succinimidyl radical,"which was responsible for the cleavage of the benzylic C-H bond, relying on the reducing ability of Acr?-Mes.
Novel high-activity diphenyl ketone photoinitiator and preparation method thereof
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Paragraph 0031; 0034; 0037; 0040, (2019/02/19)
The invention belongs to the field of photosensitive high polymer materials, and provides a novel high-activity diphenyl ketone photoinitiator. Two diphenyl ketone derivatives are synthesized into a novel diphenyl ketone photoinitiator through synthesis reaction, so that ultraviolet absorption wavelength and absorption peak area of the photoinitiator are increased, a utilization rate on ultraviolet light is increased, the photoinitiating activity is greatly improved, and range of application is increased. The invention provides a preparation method for the novel diphenyl ketone photoinitiator,and the preparation method is simple in reaction process, is gentle in reaction condition, is simple in post-treatment, and is easy to purify.