77959-68-3Relevant academic research and scientific papers
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease
Cao, Zhongcheng,Deng, Yong,Li, Yan,Luo, Li,Qiang, Xiaoming,Song, Qing,Tan, Zhenghuai
, (2020/03/13)
A series of phthalide alkyl tertiary amine derivatives were designed, synthesized and evaluated as potential multi-target agents against Alzheimer's disease (AD). The results indicated that almost all the compounds displayed significant AChE inhibitory and selective activities. Besides, most of the derivatives exhibited increased self-induced Aβ1-42 aggregation inhibitory activity compared to the lead compound DL-NBP, and some compounds also exerted good antioxidant activity. Specifically, compound I-8 showed the highest inhibitory potency toward AChE (IC50 = 2.66 nM), which was significantly better than Donepezil (IC50 = 26.4 nM). Moreover, molecular docking studies revealed that compound I-8 could bind to both the catalytic active site and peripheral anionic site of AChE. Furthermore, compound I-8 displayed excellent BBB permeability in vitro. Importantly, the step-down passive avoidance test indicated that I-8 significantly reversed scopolamine-induced memory deficit in mice. Collectively, these results suggested that I-8 might be a potent and selective AChE inhibitor for further anti-AD drug development.
3-amine alkyl phthalide compound as well as preparation method and application thereof
-
Paragraph 0007; 0020, (2020/02/14)
The invention discloses a type of novel 3-amino alkyl phthalein compound (I) as well as a pharmaceutical acceptable salt, a preparation method, a medicine composition and application thereof in preparing medicines for treating and/or preventing diseases a
4-(aminoalkyl)phthalazine-1-one compound, preparation method and use thereof
-
Paragraph 0020-0021, (2020/02/14)
The invention discloses a novel 4-(aminoalkyl)phthalazine-1-one compound (I) and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition and use in the preparation of drugs for treating and/or preventing neurological
New ligands at the?melatonin binding site MT3
Boussard, Marie-Fran?oise,Truche, Sandrine,Rousseau-Rojas, Anne,Briss, Sylvie,Descamps, Sophie,Droual, Monique,Wierzbicki, Michel,Ferry, Gilles,Audinot, Valérie,Delagrange, Philippe,Boutin, Jean A.
, p. 306 - 320 (2007/10/03)
The third melatonin binding site, MT3 is a non-classical one since it is not a seven transmembrane domains receptor, but an enzyme, quinone reductase 2. A major concern for the study of the physiological role of this site is the lack of specific ligands, permitting to more accurately dissect the pathways linked to the activation of MT3. Indeed, in the course of finding new ligands, we identified a new series of compounds with affinity to the binding site in the nM range, particularly 2,3-dimethoxy 7-hydroxy 10-methyl 5H 10H indeno(1,2-b)indol-10-one (DMHMIO), with a Ki of 190 pM. Based on slightly different and novel synthons compared to most of the compounds used in melatonin pharmacology studies, these compounds offer new perspective for the description of the melatonin pathways, so much more by not having any affinity towards the MT1 and MT2 'classical' melatonin receptors.
2,3,6,7,10,11-Hexamethoxytribenzotriquinacene: Synthesis, solid-state structure, and functionalization of a rigid analogue of cyclotriveratrylene
Harig, Marco,Neumann, Beate,Stammler, Hans-Georg,Kuck, Dietmar
, p. 2381 - 2397 (2007/10/03)
The syntheses of several tribenzotriquinacenes bearing six methoxy groups at the outer peripheral positions of the aromatic rings are reported. The centro-methyl derivative is accessible in surprisingly good yield through two-fold cyclodehydration in the
New indenoindolone compounds
-
, (2008/06/13)
Compound of formula (I): wherein R represents hydrogen, optionally substituted alkyl or alkenyl, R1 to R8, which may be identical or different, each represents hydrogen, optionally substituted alkyl, hydroxy, acyloxy, optionally subs
Indenoindolone compounds
-
, (2008/06/13)
Compound of formula (I): wherein: R represents hydrogen or a group selected from alkenyl and optionally substituted alkyl, each of R1 to R8, which may be identical or different, represents hydrogen or a group selected from alkyl, alkenyl, hydroxy, alkoxy, alkenyloxy, arylalkyl, arylalkoxy, carboxy, acyloxy and arylcarbonyloxy, or one of R1 to R8 forms with an adjacent one R1 to R8 an alkylenedioxy group, its optical isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid or base, with the proviso that: when R does not represent hydrogen, then at least one of R1 to R8 represents hydroxy or acyloxy, and the compounds of formula (I) are other than indeno[1,2-b]indol-10(5H)-one. Medicinal products containing the same which are useful for treatment of disorders of the melatoninergic system.
Isoindoloindolone compounds
-
, (2008/06/13)
Compound of formula (I): STR1wherein:R 1, R 2, R 3, R 4, R 5, R 6 and R 8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy,R 7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group,or one of R 1 to R 8, together with another of R 1 to R 8 adjacent to it, forms an alkylenedioxy,its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
Phthalazine derivatives as phosphodiesterase 4 inhibitors
-
Page column 14, (2010/11/30)
The present invention provides a compound selected from the group including: N-3-acetyl-1-(3,5-dichloropyridin-4-ylmethyl)-5-cyclopentyloxy-6-methoxy-4H-phthalazine; 6,7-dimethoxy-1-pyridin-4-ylmethyl-4-thiazol-2-yl-phthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)ethanone; 2-methanesulphonyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 2-formyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)-1-imidazol-1-ylmethanone; 1-(3,5-dichloro-pyridin-4-ylmethyl)-3-methansulphonyl-6-difluoromethoxy-5-(tetrahydro-furan-2-yloxy)-4H-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition, which contains a therapeutically effective amount of the above compound in admixture with a pharmaceutically acceptable carrier.
