96530-59-5Relevant academic research and scientific papers
FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
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Page/Page column 26; 28-29, (2021/02/12)
The invention relates to compounds of formula I, in which Y, Ar1, Ar2, X, R1 and R2 are defined herein, and to their use in a variety of biological imaging techniques and therapeutic methods. In aspects, the invention relates to conjugates comprising the compounds of formula I and their associated uses and therapeutic uses.
A novel DMSO-assisted regioselective iodination of aniline analogues
Bovonsombat, Pakorn,Lorpaiboon, Wanutcha,Laoboonchai, Sarocha,Sriprachaya-anunt, Prima,Yimkosol, Warangkana,Siriphatcharachaikul, Natthapatch,Siricharoensang, Pornpawit,Kangwannarakul, Terawee,Maeda, Jin,Losuwanakul, Satreerat,Mahesh Abhyankar, Maitraye
, (2020/10/05)
A metal- and oxidant-free electrophilic iodination of aniline analogues was achieved in high to excellent yields at room temperature in MTBE with 0 or 3.5 equivalents of DMSO. Examined substituents include N-alkyl, N,N-dialkyl, N-morpholinyl and N-piperazinyl as well as methyl, Br, CN and CO2CH3 aryl ring substitutions.
Cellular localisation of structurally diverse diphenylacetylene fluorophores
Adams, Candace,Ambler, Carrie A.,Bain, Angus J.,Blacker, Thomas S.,Callaghan, Daniel,Chisholm, David R.,Girkin, John M.,Hughes, Joshua G.,Humann, Rachel,Lembicz, Nicola K.,Pujol, Alba,Whiting, Andrew
, p. 9231 - 9245 (2020/12/03)
Fluorescent probes are increasingly used as reporter molecules in a wide variety of biophysical experiments, but when designing new compounds it can often be difficult to anticipate the effect that changing chemical structure can have on cellular localisa
Pyrazolo[3,4-c]pyridine derivative
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Paragraph 0305; 0306; 0306, (2016/10/08)
The invention relates to a pyrazolo[3,4-c]pyridine derivative. The invention relates to a compound represented by a formula (I), a tautomer thereof, an optical isomer thereof or a pharmaceutically acceptable salt thereof, wherein the formula (I) is shown in the description, and Z, X, RNc, RNd, RNe and RNf are defined according to the claim 1. The invention further relates to the pharmaceutical composition contain the compound. The invention further relates to use of the compound or the pharmaceutical composition in preparing a drug for preventing and/or treating a disease which inhibits positive influence of an Xa factor, particularly use in preparing the drug for preventing and/or treating the disease which inhibits positive influence of the Xa factor under the condition of low hemorrhage risk.
Structural modifications of neuroprotective anti-parkinsonian (-)-N6-(2-(4-(biphenyl-4-yl)piperazin-1-yl)-ethyl)-N6-propyl-4,5,6, 7-tetrahydrobenzo[d]thiazole-2,6-diamine (D-264): An effort toward the improvement of in vivo efficacy of the parent molecule
Modi, Gyan,Antonio, Tamara,Reith, Maarten,Dutta, Aloke
, p. 1557 - 1572 (2014/03/21)
In our overall goal to develop multifunctional dopamine D 2/D3 agonist drugs for the treatment of Parkinson's disease (PD), we previously synthesized potent D3 preferring agonist D-264 (1a), which exhibited neuroprotective properties in two animal models of PD. To enhance the in vivo efficacy of 1a, a structure-activity relationship study was carried out. Competitive binding and [35S]GTPγS functional assays identified compound (-)-9b as one of the lead molecules with preferential D3 agonist activity (EC50(GTPγS); D3 = 0.10 nM; D2/D3 (EC50): 159). Compounds (-)-9b and (-)-8b exhibited high in vivo activity in two PD animal models, reserpinized and 6-hydroxydopamine (OHDA)-induced unilateral lesioned rats. On the other hand, 1a failed to show any in vivo activity in these models unless the compound was dissolved in 5-10% beta-hydroxy propyl cyclodextrin solution. Lead compounds exhibited appreciable radical scavenging activity. In vitro experiments with dopaminergic MN9D cells indicated neuroprotection by both 1a and (-)-9b from toxicity of MPP+.
Multifunctional D2/D3 agonist D-520 with high in vivo efficacy: Modulator of toxicity of alpha-synuclein aggregates
Modi, Gyan,Voshavar, Chandrashekhar,Gogoi, Sanjib,Shah, Mrudang,Antonio, Tamara,Reith, Maarten E. A.,Dutta, Aloke K.
, p. 700 - 717 (2014/11/08)
We have developed a series of dihydroxy compounds and related analogues based on our hybrid D2/D3 agonist molecular template to develop multifunctional drugs for symptomatic and neuroprotective treatment for Parkinson"s disease (PD). The lead compound (-)-24b (D-520) exhibited high agonist potency at D2/D3 receptors and produced efficacious activity in the animal models for PD. The data from thioflavin T (ThT) assay and from transmission electron microscopy (TEM) analysis demonstrate that D-520 is able to modulate aggregation of alpha-synuclein (αSN). Additionally, coincubation of D-520 with αSN is able to reduce toxicity of preformed aggregates of αSN compared to control αSN alone. Finally, in a neuroprotection study with dopaminergic MN9D cells, D-520 clearly demonstrated the effect of neuroprotection from toxicity of 6-hydroxydopamine. Thus, compound D-520 possesses properties characteristic of multifunctionality conducive to symptomatic and neuroprotective treatment of PD.
RADIOLABELED D4 RECEPTOR LIGANDS
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, (2008/06/13)
Herein described are radiolabeled compounds and their precursors useful to image D4 receptors in vivo, of the formula: STR1 wherein R is selected from iodo, tri(loweralkyl)tin and a radioisotopically labeled iodide and R 1 is selected from H and alkoxycar
