98489-50-0Relevant academic research and scientific papers
Mild and rapid Pd-catalyzed cross-coupling with hydrazine in continuous flow: Application to the synthesis of functionalized heterocycles
Deangelis, Andrew,Wang, Dong-Hui,Buchwald, Stephen L.
supporting information, p. 3434 - 3437 (2013/05/09)
Minimizing risk: The synthesis of arylhydrazines through C?£?N cross-coupling of aryl chlorides with hydrazine is described. Through the use of continuous flow, the hazards associated with the use of hydrazine in the presence of transition metals are decreased. In addition, multistep flow sequences have also been developed for the generation of functionalized heterocycles utilizing the arylhydrazine intermediates.
Rational design, synthesis, and characterization of highly fluorescent optical switches for high-contrast optical lock-in detection (OLID) imaging microscopy in living cells
Petchprayoon, Chutima,Yan, Yuling,Mao, Shu,Marriott, Gerard
experimental part, p. 1030 - 1040 (2011/03/19)
A major challenge in cell biology is to elucidate molecular mechanisms that underlie the spatio-temporal control of cellular processes. These studies require microscope imaging techniques and associated optical probes that provide high-contrast and high-r
THIAZOLYL-DIHYDRO-INDAZOLES
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Page/Page column 40, (2009/10/22)
The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a
Rigidized trimethine cyanine dyes
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Page 12-13, (2008/06/13)
Disclosed are analogues of trimethine cyanine dyes which are useful for imparting fluorescent properties to target materials by covalent and non-covalent association. The compounds have the following general formula: optionally substituted by groups R2-R9 wherein groups R6, R7, R8 and R9 are attached to the rings containing X and Y or, optionally are attached to atoms of the Za and Zb ring structures and groups R1-R9 are chosen to provide desired solubility, reactivity and spectral properties to the fluorescent compounds; A is selected from O, S and NR11 where R11 is the substituted amino radical: where R′ is selected from hydrogen, a C1-4 alkyl and aryl and R″ is selected from C1-18 alkyl, aryl, heteroaryl, an acyl radical having from 2-7 carbon atoms, and a thiocarbamoyl radical; Za and Zb each represent a bond or the atoms necessary to complete one, two fused or three fused aromatic rings each ring having five or six atoms, selected from carbon atoms and, optionally, no more than two oxygen, nitrogen and sulphur atoms.
Synthesis and serotonergic activity of substituted 2,N- benzylcarboxamido-5-(2-ethyl-1-dioxoimidazolidinyl)-N,N-dimethyltryptamine derivatives: Novel antagonists for the vascular 5-HT(1B)-like receptor
Moloney, Gerard P.,Martin, Graeme R.,Mathews, Neil,Milne, Aynsley,Hobbs, Heather,Dodsworth, Susan,Sang, Pang Yih,Knight, Cameron,Williams, Marnie,Maxwell, Miles,Glen, Robert C.
, p. 2504 - 2526 (2007/10/03)
The synthesis and vascular 5-HT(1B)-like receptor activity of a novel series of substituted 2,N-benzylcarboxamido-5-(2-ethyl-1- dioxoimidazolidinyl)-N,N-dimethyltryptamine derivatives are described. Modifications to the 5-ethylene-linked heterocycle and to substituents on the 2-benzylamide side chain have been explored. Several compounds were identified which exhibited affinity at the vascular 5-HT(1B)-like receptor of pK(B) > 7.0, up to 100-fold selectivity over α1-adrenoceptor affinity and 5-HT(2A) receptor affinity, and which exhibited a favorable pharmacokinetic profile. N-Benzyl-3-[2-(dimethylamino)ethyl]-5-[2-(4,4-dimethyl-2,5-dioxo-1- imidazolidinyl)ethyl]-1H-indole-2-carboxamide (23) was identified as a highly potent, silent (as judged by the inability of angiotensin II to unmask 5- HT(1B)-like receptor-mediated agonist activity in the rabbit femoral artery), and competitive vascular 5-HT(1B)-like receptor antagonist with a plasma elimination half-life of ~4 h in dog plasma and with good oral bioavailability. The selectivity of compounds from this series for the vascular 5-HT(1B)-like receptors over other receptor subtypes is discussed as well as a proposed mode of binding to the receptor pharmacophore. It has been proposed that the aromatic ring of the 2,N-benzylcarboxamide group can occupy an aromatic binding site rather than the indole ring. The resulting conformation allows an amine-binding site to be occupied by the ethylamine nitrogen and a hydrogen-bonding site to be occupied by one of the hydantoin carbonyls. The electronic nature of the 2,N-benzylcarboxamide aromatic group as well as the size of substituents on this aromatic group is crucial for producing potent and selective antagonists. The structural requirement on the 3-ethylamine side chain incorporating the protonatable nitrogen is achieved by the bulky 2,N-benzylcarboxamide group and its close proximity to the 3- side chain.
