127792-80-7Relevant articles and documents
Synthesis and biological evaluation of novel pyrrolidine-2,5-dione derivatives as potential antidepressant agents. Part 1
Wróbel, Martyna Z.,Chodkowski, Andrzej,Herold, Franciszek,Gomó?ka, Anna,Kleps, Jerzy,Mazurek, Aleksander P.,Pluciński, Franciszek,Mazurek, Andrzej,Nowak, Gabriel,Siwek, Agata,Stachowicz, Katarzyna,S?awin?ska, Anna,Wolak, Ma?gorzata,Szewczyk, Bernadeta,Sata?a, Grzegorz,Bojarski, Andrzej J.,Tur?o, Jadwiga
, p. 484 - 500 (2013/07/25)
A series of 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives was synthesized and their biological activity was evaluated. The chemical structures of the newly prepared compounds were confirmed by 1H NMR, 13C NMR and ESI-HRMS spectra data. All tested compounds proved to be potent 5-HT1A receptor and serotonin transporter protein (SERT) ligands. Among them, compounds 15, 18, 19 and 30 showed significant affinity for 5-HT1A and SERT. Computer docking simulations carried out for compounds 15, 31 and 32 to models of 5-HT1A receptor and SERT confirm the results of biological tests. Due to high affinity for the 5-HT1A receptor and moderate affinity for SERT, compounds 31, 32, 35, and 37 were evaluated for their affinity for D2L, 5-HT6, 5-HT 7 and 5-HT2A receptors. In vivo tests, in turn, resulted in determining the functional activity of compounds 15, 18, 19 and 30 to the 5-HT1A receptor. The results of these tests indicate that all of the ligands possess properties characteristic of 5-HT1A receptor agonists.
Bisindoles as tachykinin receptor antagonists
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, (2008/06/13)
This invention provides a series of substituted bisindole propanamides which are useful as tachykinin receptor antagonists and as serotonin agonists. This invention also provides methods for the treatment of related disorders as well as pharmaceutical for
1H-indole and benzo(b)thiophene derivatives with 4-(1,2,3,6-tetra:hydro:pyridinyl)- and 4-piperidinyl-groups bound to the heterocyclic ring as inhibitors of serotonin reuptake
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, (2008/06/13)
The pharmaceutical use of novel compounds of formula I: where Z is a structure of formula A-B is -C=CH- or -C(R5)-CH2-; X is S or NR4; R1is H, halo, formyl, C1-C4alkyl, C1-C4alkoxy, thienylmethyloxy, 4,5-dihydrothiazol-2-yl, cyano, nitro, carboxamido, trifluoromethyl or hydroxy; R2is H or halo; R3is H, C1-C4alkyl, (C1-C4alkylene)-aryl, or -CH2-Y-NR7R8; R4is H, C1-C4alkyl, C1-C5acyl, or phenylsulfonyl; R5is H or OH; R6is H or methyl; Y is -CH2- or -C(O)-; R7is pyridinyl; and R8is H or -C(O)-(C3-C6cycloalkyl); and pharmaceutically acceptable salts thereof.