131216-47-2Relevant academic research and scientific papers
Synthesis of AD-Dihydrodipyrrins Equipped with Latent Substituents of Native Chlorophylls and Bacteriochlorophylls
Wang, Pengzhi,Lindsey, Jonathan S.
, p. 11794 - 11811 (2021/08/24)
Native chlorophylls and bacteriochlorophylls share a common trans-substituted pyrroline ring D (17-propionic acid, 18-methyl), whereas diversity occurs in ring A particularly at the 3-position. Two dihydrodipyrrins equipped with native-like D-ring substit
NOVEL IMIDAZO-PYRAZINE DERIVATIVES
-
, (2021/12/31)
The invention provides novel imidazo-pyrazine derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, m, n, and R1to R3 are as described herein: formula (I). Further provided are pharmace
Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids
Rivière, Solenne,Vielmuth, Christin,Ennenbach, Christiane,Abdelrahman, Aliaa,Lemke, Carina,Gütschow, Michael,Müller, Christa E.,Menche, Dirk
, p. 1348 - 1363 (2020/06/17)
The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives. We also reveal important structure-activity relationship data as well as insights into the pharmacophore of these complex polyketides.
Iridium-Catalyzed Aerobic α,β-Dehydrogenation of γ,δ-Unsaturated Amides and Acids: Activation of Both α- And β-C-H bonds through an Allyl-Iridium Intermediate
Wang, Zhen,He, Zhiqi,Zhang, Linrui,Huang, Yong
, p. 735 - 740 (2018/01/26)
Direct aerobic α,β-dehydrogenation of γ, δ-unsaturated amides and acids using a simple iridium/copper relay catalysis system is described. We developed a new strategy that overcomes the challenging issue associated with the low α-acidity of amides and acids. Instead of α-C-H metalation, this reaction proceeds by β-C-H activation, which results in enhanced α-acidity. Conjugated dienamides and dienoic acids were synthesized in excellent yield with this reaction, which uses a simple reaction protocol. Mechanistic experiments suggest a catalyst resting state mechanism in which both α-C-H and β-C-H cleavage is accelerated.
MODULATORS OF LIVER RECEPTOR HOMOLOGUE 1 (LRH-1) AND USES
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, (2018/10/19)
This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure r
Development of Hybrid Phospholipid Mimics as Effective Agonists for Liver Receptor Homologue-1
Flynn, Autumn R.,Mays, Suzanne G.,Ortlund, Eric A.,Jui, Nathan T.
, p. 1051 - 1056 (2018/09/21)
The orphan nuclear receptor Liver Receptor Homologue-1 (LRH-1) is an emerging drug target for metabolic disorders. The most effective known LRH-1 modulators are phospholipids or synthetic hexahydropentalene compounds. While both classes have micromolar ef
Diastereoselective Synthesis of Highly Substituted Tetrahydrofurans by Pd-Catalyzed Tandem Oxidative Cyclization-Redox Relay Reactions Controlled by Intramolecular Hydrogen Bonding
Brooks, Joshua L.,Xu, Liping,Wiest, Olaf,Tan, Derek S.
supporting information, p. 57 - 75 (2017/04/26)
Palladium-catalyzed oxidative cyclization of alkenols provides a convenient entry into cyclic ethers but typically proceeds with little or no diastereoselectivity for cyclization of trisubstituted olefins to form tetrahydrofurans due to the similar energi
Lewis acid-promoted addition of 1,3-bis(silyl)propenes to aldehydes: A route to 1,3-dienes
Borg, Tessie,Tuzina, Pavel,Somfai, Peter
, p. 8070 - 8075 (2011/11/28)
The Lewis acid-promoted addition of 1,3-bis(silyl)-propenes to aldehydes to provide the corresponding (E)-1,3-dienes in excellent stereoselectivity and good to excellent yields is reported. The procedure is mild, base-free, and operationally straightforward.
Synthesis of undecachlorosulfolipid A: Re-evaluation of the nominal structure
Nilewski, Christian,Deprez, Nicholas R.,Fessard, Thomas C.,Li, Dong Bo,Geisser, Roger W.,Carreira, Erick M.
, p. 7940 - 7943 (2011/10/08)
Halo-giant: The title compound at the left in the scheme was constructed by the synthesis and coupling of two stereochemically challenging fragments. A comparison of the NMR data of the synthetic material and the natural product indicates that the configuration had been misassigned in the latter. PT=5-(1-phenyltetrazolyl).
Synthesis and evaluation of dual site inhibitors of 3-deoxy-d-arabino- heptulosonate 7-phosphate synthase
Walker, Scott R.,Jiao, Wanting,Parker, Emily J.
, p. 5092 - 5097 (2011/10/09)
3-Deoxy-d-arabino-heptulosonate 7-phosphate (DAH7P) synthase catalyses the first step of the shikimate pathway for the biosynthesis of aromatic compounds. Enzymes of this pathway have been identified as potential targets for drug design. The reaction catalysed by DAH7P synthase is an aldol condensation between phosphoenolpyruvate (PEP) and d-erythrose 4-phosphate (E4P). In this study inhibitors of DAH7P synthase were prepared which were designed to fit into the binding sites of both PEP and E4P substrates simultaneously. Inhibitors, known to target the PEP binding site, were extended using a C4 linker to include an appropriately placed phosphate group in order to access the phosphate-binding site of E4P. A small increase in inhibition was observed with this modification, and the inhibition results have been rationalised by induced-fit docking.
