cas 629-09-4, 1,6-DIIODOHEXANE | Articles data

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Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands
Herein, we report the development of bitopic ligands aimed at targeting the orthosteric binding site (OBS) and a metastable binding site (MBS) within the same receptor unit. Previous molecular dynamics studies on ligand binding to the β2-adrenergic receptor (β2AR) suggested that ligands pause at transient, less-conserved MBSs. We envisioned that MBSs can be regarded as allosteric binding sites and targeted by homobivalent bitopic ligands linking two identical pharmacophores. Such ligands were designed based on docking of the antagonist (S)-alprenolol into the OBS and an MBS and synthesized. Pharmacological characterization revealed ligands with similar potency and affinity, slightly increased β2/β1AR-selectivity, and/or substantially slower β2AR off-rates compared to (S)-alprenolol. Truncated bitopic ligands suggested the major contribution of the metastable pharmacophore to be a hydrophobic interaction with the β2AR, while the linkers alone decreased the potency of the orthosteric fragment. Altogether, the study underlines the potential of targeting MBSs for improving the pharmacological profiles of ligands.
Gaiser, Birgit I.,Danielsen, Mia,Marcher-R?rsted, Emil,R?pke J?rgensen, Kira,Wróbel, Tomasz M.,Frykman, Mikael,Johansson, Henrik,Br?uner-Osborne, Hans,Gloriam, David E.,Mathiesen, Jesper Mosolff,Sejer Pedersen, Daniel
p. 7806 - 7839
(2019/09/07)

A Far-Red Fluorescent DNA Binder for Interaction Studies of Live Multidrug-Resistant Pathogens and Host Cells
Transgene expression of green fluorescent protein (GFP) has facilitated the spatiotemporal investigation of host–pathogen interactions; however, introduction of the GFP gene remains challenging in drug-resistant bacteria. Herein, we report a novel far-red fluorescent nucleic acid stain, 6-TramTO-3, which efficiently labels bacteria through a DNA binding mode without affecting growth and viability. Exemplarily, we stained Klebsiella pneumoniae, a major threat to hospitalized patients, and deciphered divergent interaction strategies of antibiotic-resistant and antibiotic-sensitive Klebsiella strains with immune cells. 6-TramTO-3 constitutes an off-the-shelf reagent for real-time analysis of bacterial infection, including strains for which the use of genetically encoded reporters is not feasible. Eventually, our approach may aid the development of strategies to combat a major worldwide health threat: multidrug-resistant bacteria.
Schulte, Leon N.,Heinrich, Benedikt,Janga, Harshavardhan,Schmeck, Bernd T.,Vázquez, Olalla
supporting information
p. 11564 - 11568
(2018/09/10)

Applications of surfactant-modified clays to synthetic organic chemistry
Two triphase catalysts (SLL) have been developed for organic phase-aqueous phase reactions catalyzed by suitable modified clay (solid phase). These triphase catalysts have been applied to nucleophilic displacement on activated (benzylic) as well as unactivated organic halides and provide a convenient and effective method of preparation of the corresponding products. Other useful transformations to, which these triphase catalysts have been successfully applied are the synthesis of 9,9-dichloro bicyclo[6.1.0]nonane, O-alkylation and C-alkylation of β-naphthol.
Ghiaci,Sedaghat,Kalbasi,Abbaspur
p. 5529 - 5534
(2007/10/03)

Local anesthetic compounds and uses
Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+channel to modulate the biological processes/functions thereof.
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(2008/06/13)

Pharmaceutically active compounds
Compounds of the formula pharmaceutically acceptable acid addition, basic addition salts or quaternary amine salts thereof, wherein Z is phenyl, substituted phenyl, wherein the substituents are independently one or more of halogen, lower alkylthio, loweralkylsulfonyl, lower alkoxy, oxazol-2-yl; imidazo-1-yl; lower alkyl substituted imidazo-1-yl; or tert-butyl; X is a bond, STR1 Q is lower alkane-diyl or 5, 6, or 7 carbon atoms optionally substituted by --OH; loweralkylnediyl of 6-8 carbon atoms; methylcyclohexylmethyl; tetrahydrofurandiyl; or (C1 -C2) lower alkane-diyl tetrahydrofurandiyl-C1 -C2 loweralkanediyl; wherein the tetrahydrofuran ring is substituted by 0-2 hydroxy groups; Y is a bond; and W is benzimidazol-1-yl or benzimidazol-2-yl are described. These compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
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(2008/06/13)

Pharmaceutically active compounds
The disclosed invention is compounds represented by the formula and pharmaceutically acceptable acid addition salts and quarternary amine salts thereof, wherein Z is phenyl, naphthyl or adamantyl; substituted phenyl wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, methylsulfonyl, isoxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, loweralkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 5 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen and one carbon in the ring, wherein the substituents are one or more of carboxyl, hydroxymethyl, loweralkyl, loweralkylcarbonyl or aryl lower alkyl; or tertiary butyl; X and Y are each independently a bond, -O-, STR1 Q is a divalent substituted or unsubstituted straight or branched chain lower alkanediyl, -lower alkanedinyl- cycloalkanediyl- lower alkanediyl-, lower alkendiyl, lower alkynediyl, phenylene, tetrahydrofurandiyl or tetrahydropyrandiyl; W is a monovalent substituted or unsubstituted aromatic heterocyclic single or fused ring containing from 5 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom, wherein the substituents are hydroxy, amino, carbamoyl, carboxyl, nitrile, nitro, oxo, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxylowralkyl; and W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
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(2008/06/13)

A CONVENIENT METHOD FOR THE SYNTHESIS OF DIIODO COMPOUNDS. FACILE CLEAVAGE OF CYCLIC ETHERS BY PHENYL DICHLOROPHOSPHATE AND SODIUM IODIDE
Cyclic ethers were found to react readily with phenyl dichlorophosphate and sodium iodide to give diiodo compounds under mild reaction conditions.
Liu, Hsing-Jang,Shewchuk, Lisa M.,Llinas-Brunet, Montse
p. 3043 - 3046
(2007/10/02)

LONG-ACTING CONTRACEPTIVE AGENTS: ESTERS OF NORETHISTERONE WITH ALKOXY- AND HALOGENO-SUBSTITUTED CARBOXYLIC ACIDS
The chemical synthesis and physical data of several new esters of norethisterone (17α-ethynyl-17β-hydroxyestr-4-en-3-one) are reported, which contain either a chloro- or an alkoxy-group as a substituent in the acid side-chain.
Shafiee, A.,Vossoghi, M.,Francisco, C. G.,Freire, R.,Hernandez, R.,et al.
p. 285 - 290
(2007/10/02)

The Synthesis of Linked Acridines as Intercalating and Antitumor Agents
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Acheson, R. Morrin,Constable, Edwin C.,Wright, R. Gordon McR.,Taylor, Grahame M.
p. 101 - 132
(2007/10/02)