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Unbound Medicine.
(monocyclic)
2,025 results
  • Direct, Competitive Comparison of Linear, Monocyclic, and Bicyclic Libraries Using mRNA Display. [Journal Article]
    ACS Comb Sci. 2020 May 17 [Online ahead of print]Hacker DE, Abrigo NA, … Hartman MCT
  • Peptide macrocyclization is typically associated with the development of higher affinity and more protease stable protein ligands, and, as such, is an important tool in peptide drug discovery. Yet, within the context of a diverse library, does cyclization give inherent advantages over linear peptides? Here, we used mRNA display to create a peptide library of diverse ring sizes and topologies (mon…
  • Chemical Equivalent of Arene Monooxygenases: Dearomative Synthesis of Arene Oxides and Oxepines. [Journal Article]
    J Am Chem Soc. 2020 May 08 [Online ahead of print]Siddiqi Z, Wertjes WC, Sarlah D
  • Direct epoxidation of aromatic nuclei by cytochrome P450 monooxygenases is one of the major metabolic pathways of arenes in eukaryotes. The resulting arene oxides serve as versatile precursors to phenols, oxepines, or trans-dihydrodiol-based metabolites. Although such compounds have an important biological and chemical relevance, the lack of methods for their production has hampered access to the…
  • Cyclic Aliphatic Hydrocarbons as Linkers in Metal-Organic Frameworks: New Frontiers for Ligand Design. [Review]
    Chempluschem. 2020 May; 85(5):845-854.Slyusarchuk VD, Kruger PE, Hawes CS
  • In this Minireview we outline the development of cyclic aliphatic moieties as ligands in metal-organic frameworks (MOFs), with a focus on the relationship between ligand design and synthesis and the properties of the subsequent materials. Aliphatic ligands have received considerably less attention than aromatic analogues in MOF chemistry but offer advantages in their unique combinations of geomet…
  • Palladium-Catalyzed Asymmetric [8+2] Dipolar Cycloadditions of Vinyl Carbamates and Photogenerated Ketenes. [Journal Article]
    Angew Chem Int Ed Engl. 2020 May 05 [Online ahead of print]Lu LQ, Zhang QL, … Xiao WJ
  • Higher-order cycloadditions, particularly [8+2] cycloadditions, are a straightforward and efficient strategy for constructing significant medium-sized architectures. Typically, configuration-restrained conjugated systems are utilized as 8π-components for higher-order concerted cycloadditions. However, for this reason, 10-membered monocyclic skeletons have never been constructed via the catalytic …
  • Treatment of Systemic JIA: When do we need a biologic? Real world data of a single center. [Journal Article]
    Mod Rheumatol. 2020 Apr 28 [Online ahead of print]Adiguzel Dundar H, Acari C, … Unsal E
  • Objectives: This paper aimed to present real-world data of treatment results of a single center in patients with systemic Juvenile Idiopathic arthritis (SJIA), in which methotrexate (MTX) along with glucocorticoids was preferred as the first-line treatment option.Methods: The medical records of 50 patients (58 episodes) with SJIA were evaluated. All patients with SJIA were hospitalized and were…
  • Novel o-Toluidine Metabolite in Rat Urine Associated with Urinary Bladder Carcinogenesis. [Journal Article]
    Chem Res Toxicol. 2020 May 12 [Online ahead of print]Tajima Y, Toyoda T, … Miyoshi N
  • o-Toluidine (o-Tol), a monocyclic aromatic amine, causes bladder cancer in humans and experimental animals and is therefore classified as a Group 1 carcinogen (IARC) in which the carcinogenicity of o-Tol is involved in metabolic activation, DNA damage, and DNA adduct formation. In the DNA adduct formation mechanism, o-Tol is metabolized by N-hydroxylation, N-acetoxylation, and then deacetoxylatio…
  • Red-mud based porous nanocatalysts for valorisation of municipal solid waste. [Journal Article]
    J Hazard Mater. 2020 Apr 23; 396:122711.Ahmed MHM, Batalha N, … Konarova M
  • Red mud samples were used to catalyse in-situ co-pyrolysis of pinewood and low-density polyethylene for the production of high-quality bio-oil. The sodium cation in the crude red-mud was exchanged with barium and calcium cations and further tested to explore their role in oil upgrading. The relationship between red-mud catalytic activity and its constituents was explored using synthetic sodalite.…
  • Synergistic and Antagonistic Effects of Aromatics on the Agglomeration of Gas Hydrates. [Journal Article]
    Sci Rep. 2020 Mar 26; 10(1):5496.Bui T, Monteiro D, … Striolo A
  • Surfactants are often used to stabilize aqueous dispersions. For example, surfactants can be used to prevent hydrate particles from forming large plugs that can clog, and sometimes rupture pipelines. Changes in oil composition, however dramatically affect the performance of said surfactants. In this work we demonstrate that aromatic compounds, dissolved in the hydrocarbon phase, can have both syn…
  • Terpenoids in Marine Heterobranch Molluscs. [Review]
    Mar Drugs. 2020 Mar 14; 18(3)Avila C
  • Heterobranch molluscs are rich in natural products. As other marine organisms, these gastropods are still quite unexplored, but they provide a stunning arsenal of compounds with interesting activities. Among their natural products, terpenoids are particularly abundant and diverse, including monoterpenoids, sesquiterpenoids, diterpenoids, sesterterpenoids, triterpenoids, tetraterpenoids, and stero…
  • BIM-46174 fragments as potential ligands of G proteins. [Journal Article]
    Medchemcomm. 2019 Oct 01; 10(10):1838-1843.Küppers J, Benkel T, … Gütschow M
  • The 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine derivative BIM-46174 has received attention as Gαq inhibitor. We conducted structural reductions to monocyclic and bicyclic substructures to explore the chemical space of BIM fragments and to gain insights into the pharmacophore of BIM-type Gαq inhibitors. Two piperazin-2-one-containing fragments and a small library of bicyclic lactams featuring fused …
  • Oxygen detoxification by dienoyl-CoA oxidase involving flavin/disulfide cofactors. [Journal Article]
    Mol Microbiol. 2020 Feb 21 [Online ahead of print]Schmid G, Scheffen M, … Boll M
  • Class I benzoyl-CoA reductases (BCRs) are oxygen-sensitive key enzymes in the degradation of monocyclic aromatic compounds in anaerobic prokaryotes. They catalyze the ATP-dependent reductive dearomatization of their substrate to cyclohexa-1,5-diene-1-carboxyl-CoA (1,5-dienoyl-CoA). An aromatizing 1,5-dienoyl-CoA oxidase (DCO) activity has been proposed to protect BCRs from oxidative damage, howev…
  • Observation of Möbius Aromatic Planar Metallaborocycles. [Journal Article]
    J Am Chem Soc. 2020 Feb 19; 142(7):3356-3360.Cheung LF, Kocheril GS, … Wang LS
  • Möbius aromaticity was developed for twisted annulenes with electron counting rules opposite to those of Hückel aromaticity. The introduction of transition metals makes it possible for planar cyclic systems to exhibit Möbius aromaticity. Here we report the first planar monocyclic metallaboron systems with Möbius aromaticity. The structures and bonding of two rhenium-boride clusters are studied by…
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