15540-90-6Relevant academic research and scientific papers
Further Studies on Triazinoindoles as Potential Novel Multitarget-Directed Anti-Alzheimer's Agents
Patel, Dushyant V.,Patel, Nirav R.,Kanhed, Ashish M.,Teli, Divya M.,Patel, Kishan B.,Gandhi, Pallav M.,Patel, Sagar P.,Chaudhary, Bharat N.,Shah, Dharti B.,Prajapati, Navnit K.,Patel, Kirti V.,Yadav, Mange Ram
, p. 3557 - 3574 (2020/11/18)
The inadequate clinical efficacy of the present anti-Alzheimer's disease (AD) drugs and their low impact on the progression of Alzheimer's disease in patients have revised the research focus from single targets to multitarget-directed ligands. A novel series of substituted triazinoindole derivatives were obtained by introducing various substituents on the indole ring for the development of multitarget-directed ligands as anti-AD agents. The experimental data indicated that some of these compounds exhibited significant anti-AD properties. Among them, 8-(piperidin-1-yl)-N-(6-(pyrrolidin-1-yl)hexyl)-5H-[1,2,4]triazino[5,6-b]indol-3-amine (60), the most potent cholinesterase inhibitor (AChE, IC50 value of 0.32 μM; BuChE, IC50 value of 0.21 μM), was also found to possess significant self-mediated Aβ1-42 aggregation inhibitory activity (54% at 25 μM concentration). Additionally, compound 60 showed strong antioxidant activity. In the PAMPA assay, compound 60 exhibited blood-brain barrier penetrating ability. An acute toxicity study in rats demonstrated no sign of toxicity at doses up to 2000 mg/kg. Furthermore, compound 60 significantly restored the cognitive deficits in the scopolamine-induced mice model and Aβ1-42-induced rat model. In the in silico ADMET prediction studies, the compound satisfied all the parameters of CNS acting drugs. These results highlighted the potential of compound 60 to be a promising multitarget-directed ligand for the development of potential anti-AD drugs.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING CFTR
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, (2017/08/01)
The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.
Reductive Coupling of Acrylates with Ketones and Ketimines by a Nickel-Catalyzed Transfer-Hydrogenative Strategy
Buxton, Craig S.,Blakemore, David C.,Bower, John F.
supporting information, p. 13824 - 13828 (2017/10/24)
Nickel-catalyzed coupling of benzyl acrylates with activated ketones and imines provides γ-butyrolactones and lactams, respectively. The benzyl alcohol byproduct released during the lactonization/lactamization event is relayed to the next cycle where it serves as the reductant for C?C bond formation. This strategy represents a conceptually unique approach to transfer-hydrogenative C?C bond formation, thus providing examples of reductive heterocyclizations where hydrogen embedded within an alcohol leaving group facilitates turnover.
TETRAZOLINONE COMPOUNDS AND ITS USE AS PESTICIDES
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, (2013/11/18)
The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, or a C3-C12 cycloalkyl group, etc., which each optionally be substituted; R2, R3, R4 and R5 represent independently of each other a hydrogen atom, a halogen atom or an C1-C3 alkyl group, etc.; R6 represents an C1-C6 alkyl group, a C3-C6 cycloalkyl group, a halogen atom, a C1-C6 haloalkyl group, an C2-C6 alkenyl group, an C1-C6 alkoxy group, or a C1-C6 haloalkoxy group, etc.; R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, or an C1-C4 alkyl group, etc.; X represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.
Synthesis of novel 3-acyloxy-1,3-dihydro-2H-indol-2-ones and isomeric 4- acyl-1,4-dihydro-3,1-benzoxazin-2-ones: Double rearrangement of 3- hydroxyquinoline-2,4(1H,3H)-diones
Klásek, Antonín,Ko?istek, Kamil,Polis, Ji?í,Ko?mrlj, Janez
, p. 1551 - 1560 (2007/10/03)
Substituted 3-hydroxyquinoline-2,4(1H,3H)-diones 3 were transformed into 3-acyloxy-1,3-dihydro-2H-indol-2-ones 4 and isomeric 4-acyl-1,4-dihydro-3,1- benzoxazin-2-ones 5. The influence of the substituents and the reaction conditions on the course of the r
Dicyclooctabiphenylene. Synthesis and Properties
Wilcox, Charles F.,Farley, Erik N.
, p. 7195 - 7200 (2007/10/02)
The synthesis and properties of the "antiaromatic" hydrocarbon dicyclooctabiphenylene (1) are described.The observed electronic and 1H NMR spectra of 1 agree well with previous predictions.The series of polycycles consisting o
Conformational Behaviour of Medium-sized Rings. Part 10. Dithiosalicylides and Trithiosalicylides
Guise, G. Bruce,Ollis, W. David,Peacock, Judith A.,Stephanatou, Julia Stephanidou,Stoddart, J. Fraser
, p. 1637 - 1648 (2007/10/02)
The trithiosalicylide derivatives (8)-(11) have been synthesised and shown by temperature-dependent 1H n.m.r. spectroscopy to exist in solution as ring inverting (35a)(35b) enantiomeric helical conformations with trans-thioester linkages.The free energies of activation for these conformational changes are ca. 10 kcal mol-1 higher than those for the similar process in the corresponding trisalicylides.In contrast with the trisalicylides, the trithiosalicylides can only ring invert between enantiomeric helical conformations via intermediates containing a cis-thioester linkage.The dithiosalicylide derivatives (3)-(7) have been synthesised; the temperature dependence of the 1H n.m.r. spectrum of di-o-thiothymotide (7) has been interpreted in terms of ring inversion (40a)(40b) between enantiomeric boat conformations.Comparison of the ΔG value of 24.6 kcal mol-1 for this conformational change with that of 17.7 kcal mol-1 previously obtained for di-o-thymotide (41) suggests that cis-thioester linkages are subject to more resonance stabilisation than are cis-ester linkages.
