5409-39-2Relevant academic research and scientific papers
Convenient and practical synthesis of 6-chloro-2-(chloromethyl)- thiazolo[5,4-b]pyridine
Ding, Zi-Chun,Ma, Xiang,Zhou, Weicheng
, p. 2791 - 2796 (2012)
(Chemical Equation Presented) A high-yielding and practical synthesis of 6-chloro-2-(chloromethyl)- thiazolo[5,4-b]pyridine starting from 2-amino-5-chloropyridine has been accomplished in a sequence of five steps. Copyright Taylor & Francis Group, LLC.
Design, synthesis and characterization of indole based anion sensing receptors
Manivannan, Ramalingam,Satheshkumar, Angupillai,El-Mossalamy, El-Sayed H.,Al-Harbi, Laila M.,Kosa, Samia A.,Elango, Kuppanagounder P.
, p. 3936 - 3947 (2015/05/20)
The design and synthesis of six new receptors (R1-R6) and their anion sensing properties through multiple channels are reported. These receptors are constructed in such a way that they possess indole groups as the binding sites and different acceptors units of varying electron acceptor strengths. Receptors R1, R3 and R5 could recognize fluoride ions visually and spectroscopically with high selectivity over other anions in DMF, which was demonstrated by a visual detection experiment and UV-Vis, fluorescence and 1H NMR spectral studies. The remaining three receptors (R2, R4 and R6) exhibited colour changes with both fluoride and cyanide ions. The binding constants for fluoride binding by these receptors were determined to be in the order of 104 to 106 M-1 and found to depend on the electron accepting property of the acceptor unit in the intra molecular charge transfer (ICT) transition existing with the indole donor units. 1H NMR titration experiments not only provide evidence for the existence of H-bonding interactions between the indolic N-H groups of these receptors and F-, but also offer key insight into the strengths of the receptor-anion complexes of stoichiometry 1:2. The higher fluoride binding ability of the receptor containing the naphthoquinone signalling unit has been interpreted in terms of the greater electron deficiency of the acceptor unit (quinone) and enhanced H-bond donating character of the indole N-H group. The results of the electrochemical and DFT computation studies corroborate well with the spectroscopic studies.
SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
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Page/Page column 100, (2015/01/07)
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
OLEFIN SUBSTITUTED OXINDOLES HAVING AMPK ACTIVITY
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Page/Page column 96, (2015/01/07)
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
OXIME COMPOUNDS AND THE USE THEREOF
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Page/Page column 369, (2008/06/13)
The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CRsu
Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: Synthesis and biological testing
Hussenether, Thomas,Huebner, Harald,Gmeiner, Peter,Troschuetz, Reinhard
, p. 2625 - 2637 (2007/10/03)
Novel 4-arylpiperazin-1-yl-substituted 2,3-dihydro-1H-1,4- and 1H-1,5-benzodiazepines and their aza-analogues were synthesized as debenzoclozapine derivatives for evaluation as potential D4-ligands. While Ki values of some of the title compounds came within the range of clozapine, they showed an impressively greater selectivity over other dopamine receptor subtypes, especially D2. For the most promising compounds, intrinsic activity and binding properties to serotonin 5-HT1A and 5-HT2 were also determined.
Synthesis and SAR of 5-, 6-, 7- and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2(1H)-one as NMDA/glycine site antagonists
Zhou, Zhang-Lin,Navratil, James M.,Cai, Sui Xiong,Whittemore, Edward R.,Espitia, Stephen A.,Hawkinson, Jon E.,Tran, Minhtam,Woodward, Richard M.,Weber, Eckard,Keana, John F.W.
, p. 2061 - 2071 (2007/10/03)
A series of 5-, 6-, 7- and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2(1H)-one was synthesized and assayed as NMDA/glycine receptor antagonists. The in vitro potency of these antagonists was determined by displacement of the glycine site radioligand [3H]5,7-dicholorokynurenic acid ([3H]DCKA) in rat brain cortical membranes. Selected compounds were also tested for functional antagonism using electrophysiological assays in Xenopus oocytes expressing cloned NMDA receptor (NR) 1A/2C subunits. Among the 5-, 6-, 7-, and 8-aza-3-aryl-4-hydroxyquinoline-2(1H)-ones investigated, 5-aza-7-chloro-4-hydroxy-3-(3-phenoxyphenyl)quinolin-2-(1H)-one (13i) is the most potent antagonist, having an IC50 value of 110 nM in [3H]DCKA binding and a Kb of 11 nM in the electrophysiology assay. Compound 13i is also an active anticonvulsant when administered systemically in the mouse maximum electroshock-induced seizure test (ED50 = 2.3 mg/kg, IP).
8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/NMDA receptor
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, (2008/06/13)
Disclosed is a method of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma or hypoglycemia. The method comprises administering to an animal a compound of the formula: STR1 or a pharmaceutically acceptable salt thereof; wherein n is zero or 1; R 4, R 5, R 6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and R c and R d are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor.
Heterocyclic compounds having anti-diabetic activity and their use
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, (2008/06/13)
Compounds of formula (I): STR1 [wherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrimidinyl group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxothiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethyl group; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group; and m is an integer of from 1 to 5] have hypoglycemic and anti-diabetic activities.
