- Preparation of tricyclic analog as CDE ring model of renieramycin marine natural product by novel photo-induced transformation of 6-methoxy-1,2,3,4-tetrahydroisoquinoline-5,8-dione
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2-Acetyl-6-[(benzyloxy)methyl]-9-methoxy-8-methyl-11,11adihydro-2H-pyrazino[1,2-b]isoquinoline-1,4,7,10(3H,6H)-tetraone (11a) was prepared as the CDE ring model of renieramycins, and its novel photo-induced transformation was demonstrated to construct a 1,3-dioxol ring.
- Yokoya, Masashi,Takahashi, Shohei,Saito, Naoki
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p. 1276 - 1303
(2019/07/31)
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- Btk INHIBITORS WITH IMPROVED DUAL SELECTIVITY
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Disclosed herein is a tri-substituted phenyl Btk inhibitors with improved dual selectivity, a method and a composition for inhibiting Btk and treating disease associated with undesirable Btk activity (Btk-related diseases).
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Paragraph 0134-0136
(2019/03/05)
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- MODIFIED NUCLEOTIDE REAGENTS
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Labeled nucleotide analogs comprising at least one avidin protein, at least one dye-labeled compound, and at least one nucleotide compound are provided. The analogs are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The analogs are detectable with high sensitivity at desirable wavelengths. They contain structural components that modulate the interactions of the analogs with DNA polymerase, thus decreasing photodamage and improving the kinetic and other properties of the analogs in sequencing reactions. Also provided are nucleotide and dye-labeled compounds of the subject analogs, as well as intermediates useful in the preparation of the compounds and analogs. Compositions comprising the compounds, methods of synthesis of the intermediates, compounds, and analogs, and mutant DNA polymerases are also provided.
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Paragraph 0238
(2017/11/29)
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- Effect of methyl substitution on the antioxidative property and genotoxicity of resveratrol
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Resveratrol (trans-3,4′,5-trihydroxystilbene) is a natural phytoalexin with various biological activities including inhibition of lipid peroxidation and free radical scavenging properties. In addition to its beneficial effects, resveratrol also has significant genotoxicity that leads to a high frequency of chromosome aberration together with micronucleus and sister chromatid exchanges. To enhance the radical scavenging activities and to reduce the genotoxicity of resveratrol, we designed 4′-methyl resveratrol analogues where a methyl group was introduced at the ortho position relative to the 4′-hydroxy group, which is responsible for both antioxidative activities and genotoxicity of resveratrol. These synthesized methyl analogues of resveratrol showed increased antioxidative activities against galvinoxyl radical as an oxyl radical species. Furthermore, the methyl analogues also surprisingly showed reduced in vitro genotoxicities, suggesting that methyl substitution may improve resveratrol efficacy.
- Fukuhara, Kiyoshi,Nakanishi, Ikuo,Matsuoka, Atsuko,Matsumura, Tomohiro,Honda, Sachiko,Hayashi, Mikiko,Ozawa, Toshihiko,Miyata, Naoki,Saito, Shinichi,Ikota, Nobuo,Okuda, Haruhiro
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p. 282 - 287
(2008/12/22)
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- New oxybenzamide derivatives useful for inhibiting factor Xa or VIIa
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The present invention relates to compounds comprising the following formula: R0—Q—X—Q′—W—U—V—G—M??(I) These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.
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- Approaches to the fully functionalized DEF ring system of ristocetin A via highly selective ruthenium-promoted SNAr reaction
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Ruthenium-promoted intramolecular SNAr reaction has allowed the construction of the fully functionalized 16-membered DEF macrocycle 4 of ristocetin A that incorporates the required arylglycine and arylserine residues as the F and E ring, respectively.
- Pearson, Anthony J.,Heo, Jung-Nyoung
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p. 2987 - 2990
(2007/10/03)
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- Porphyrin receptors for amines, amino acids, and oligopeptides in water
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A series of water-soluble porphyrin receptors having a hydrophobic binding pocket, a Lewis acidic site (Zn), and an electrostatic recognition site (COO- groups) were prepared. All the porphyrin receptors have a [meso- tetrakis(p-carboxyphenyl)porphyrinato]zinc (Zn·TCPP) as a common structural unit, and eight ω-carboxyalkyloxy groups (alkyloxy = methoxy (1), butoxy (2), decyloxy (3)) at the ortho positions of the phenyl groups. These receptors bind amines, α-amino acid esters, and oligopeptides in water with significant selectivity. For binding of hydrophilic guests, 1, 2, and 3 bind histamine in pH 8 buffer at 25 °C with binding constants of 157000, 31000, and 18200 M-1, respectively, where the coordination (Imd-Zn) and the salt bridge (NH3+--OOC) stabilized the complex. The large dependence of the binding constants on the ionic strength indicated that the electrostatic interaction between the ammonium group of histamine and the carboxylate groups of receptor contributes significantly to tight binding in water. Receptors 1-3 also bind a cationic guest, Arg-OMe, with a binding constant of 440-11000 M-1. The effective charge of the receptors for electrostatic recognition of Arg-OMe in pH 9 Borax (1 = 0.1 M) at 25 °C was evaluated by the Debye-Huckel limiting law as 4.2, 4.3, and 3.0 for 1, 2, and 3, respectively. These observations indicate that a salt bridge, which is exposed to water and involves hydrogen bonding, as seen in the 1-histamine and 1-Arg-OMe complexes, can be used as a significant recognition force. Binding of Arg-OMe by 2 and 3 was entropically driven, and binding of Arg-OMe by 1 was enthalpically driven. Therefore, the driving force of binding is desolvation from the ionic groups in the former case and the electrostatic attraction in the latter case. For binding of hydrophobic guests, 3 binds Trp-OMe or pyridine in water with binding constants of 7000-8000 M-1, while 1 and Zn·TCPP bind these guests less tightly with binding constants of 20- 500 M-1, indicating the importance of the long alkyl chains to provide a hydrophobic binding pocket above the porphyrin plane.
- Mizutani, Tadashi,Wada, Kenji,Kitagawa, Susumu
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p. 11425 - 11431
(2007/10/03)
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- Synthesis of 2-Formyl-3,5-dihydroxy-4-methylbenzoic Acid, a Root Growth Stimulating Fungal Metabolite
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A total synthesis of 2-formyl-3,5-dihydroxy-4-methylbenzoic acid (XII), a root growth promoting metabolite is described.
- Murthy, A. R. K.,Rao, G. S. R. Subba
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p. 569 - 571
(2007/10/02)
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