29969-23-1Relevant academic research and scientific papers
Design and synthesis of new potent 5-HT7 receptor ligands as a candidate for the treatment of central nervous system diseases
Drabczyk, Anna K.,Latacz, Gniewomir,Ja?kowska, Jolanta,Ku?aga, Damian,Pla?uk, Damian,Rózga, Karolina,Sata?a, Grzegorz
, (2021/10/29)
Owing to their multifunctional pharmacological profiles (including dual 5-HT1A/5-HT7 action), arylpiperazine derivatives are widely used for treating central nervous system diseases including the depression or neuropathic pain. Herein we describe the design, synthesis and evaluation of biological activity of novel 5-HT7 ligands derived of 2,4,6-triamino-1,3,5-triazine. The studied compounds showed affinity and high selectively towards 5-HT7 receptor with the two most active compounds 34 (Ki = 61 nM), 22 (Ki = 109 nM) showing good metabolic stability and moderate affinity to CYP3A4 isoenzyme. Compound 22 had high hepatotoxicity at a concentration below 50 μM, while compound 34 showed low hepatotoxicity even at a concentration above 50 μM.
Halogenated salt of - 1-[2-(3,4- n)]-3- dichlorophenoxy-ethanedioic acid methyl imidazole as well as preparation method and application thereof (by machine translation)
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Paragraph 0020; 0021, (2020/01/12)
The invention belongs to the technical field of, peasants, and relates to a 1 - [2 - (3,4 - novel plant growth)] regulator (Dichlorphenoxy-phenoxyethyl-3-methylimidazole halide salt, and a. preparation method and application thereof : The results show tha
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl and arylthioethyl-piperidines and pyrrolidines as a novel class of potent 5-HT7 receptor antagonists
Zajdel, Pawel,Grychowska, Katarzyna,Pawlowski, MacIej,Kurczab, Rafal,Satala, Grzegorz,Bojarski, Andrzej J.
supporting information, p. 348 - 360,13 (2012/12/11)
An analysis of the virtual combinatorial library was used for refining a pilot set of 34 derivatives and designing a targeted 38-member library of the arylamide and arylsulfonamide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines. All compounds 24-95 were synthesized according to an elaborated parallel solid-phase method and were biologically evaluated for their affinity for 5-HT7R. Additionally, the targeted library members were tested for 5-HT1A, 5-HT6, and D2 receptors. Selected compounds of particular interest were examined for their intrinsic activity at 5-HT7R in vitro employing a cAMP assay. The study allowed us to identify compound 68 (4-fluoro-N-(1-{2-[(propan-2-yl) phenoxy]ethyl}piperidin-4-yl) benzenesulfonamide) as a potent 5-HT7R ligand (Ki = 0.3 nM) with strong antagonistic properties (K b = 1 nM) and a 1450-fold selectivity over 5-HT1ARs.
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl and arylthioethyl-piperidines and pyrrolidines as a novel class of potent 5-HT7 receptor antagonists
Zajdel, Pawe?,Kurczab, Rafa?,Grychowska, Katarzyna,Sata?a, Grzegorz,Paw?owski, MacIej,Bojarski, Andrzej J.
supporting information, p. 348 - 360 (2013/01/15)
An analysis of the virtual combinatorial library was used for refining a pilot set of 34 derivatives and designing a targeted 38-member library of the arylamide and arylsulfonamide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines. All compounds 24-95 were synthesized according to an elaborated parallel solid-phase method and were biologically evaluated for their affinity for 5-HT7R. Additionally, the targeted library members were tested for 5-HT1A, 5-HT6, and D2 receptors. Selected compounds of particular interest were examined for their intrinsic activity at 5-HT7R in vitro employing a cAMP assay. The study allowed us to identify compound 68 (4-fluoro-N-(1-{2-[(propan-2-yl) phenoxy]ethyl}piperidin-4-yl) benzenesulfonamide) as a potent 5-HT7R ligand (Ki = 0.3 nM) with strong antagonistic properties (K b = 1 nM) and a 1450-fold selectivity over 5-HT1ARs.
The exposure device
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, (2007/10/13)
PROBLEM TO BE SOLVED: To perform position alignment of a mask and a work piece by detecting two alignment marks located outside the depth of focus range without moving an alignment microscope in an optical axis direction. SOLUTION: When the alignment mark of a mask M is detected, a work stage 3 moves to the right side of the drawing, a parallel plate 5 attached to the side face of the work stage 3 is inserted into the optical path of an alignment microscope 4 and the location of the alignment mark of the mask M is detected and memorized. When the alignment mark of a work piece W is detected, the work stage 3 shifts to the location of the drawing. The alignment microscope 4 is inserted into the inside of the work stage 3 so that the work-piece mark WAM may be detected by the alignment microscope 4 via the through tube 3b. When the two alignment marks are detected, the work stage 3 is shifted so that they should become a predetermined positional relationship, and thus, exposing light is irradiated from the light emitter 1 so as to expose the mask pattern to the work piece W. COPYRIGHT: (C)2006,JPOandNCIPI
A practical synthesis of sarpogrelate hydrochloride and in vitro platelet aggregation inhibitory activities of its analogues
Chen, Guo Hua,Wang, Sheng,Wu, Fei Hua
scheme or table, p. 287 - 289 (2010/12/20)
A convenient approach for the preparation of sarpogrelate hydrochloride was developed. Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.
7-NONSUBSTITUTED INDOLE MCL-1 INHIBITORS
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Page/Page column 89, (2008/12/08)
Compounds of formula (I) which inhibit the activity of anti-apoptotic Mcl-1 protein, compositins containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
Novel 4-phenylpiperidines for the treatment of pruritic dermatoses
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, (2008/06/13)
Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R 1, R 2, R 3, W, Y 1, Y 2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment. of pruritic dermatoses including allergic dermatitis and atopy in animals and humans
