102064-36-8Relevant articles and documents
HETEROCYCLIC COMPOUNDS AND IMAGING AGENTS FOR IMAGING HUNTINGTIN PROTEIN
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, (2021/12/31)
Provided herein are certain compounds and imaging agents useful for detecting a disease or condition associated with protein aggregation, especially huntingtin protein aggregation, compositions thereof, and methods of their use.
Synthesis, Antimalarial Activity, and Molecular Modeling of New Pyrrolo[1,2-a]quinoxalines, Bispyrrolo[1,2-a]quinoxalines, Bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and Bispyrrolo[1,2-a]thieno[3,2-e]pyrazines
Guillon, Jean,Grellier, Philippe,Labaied, Mehdi,Sonnet, Pascal,Léger, Jean-Michel,Déprez-Poulain, Rébecca,Forfar-Bares, Isabelle,Dallemagne, Patrick,Lema?tre, Nicolas,Péhourcq, Fabienne,Rochette, Jacques,Sergheraert, Christian,Jarry, Christian
, p. 1997 - 2009 (2007/10/03)
Three pyrrolo[1,2-a]quinoxalines, 15 bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines were synthesized from various substituted nitroanilines or nitropyridines and tested for their in vitro activity upon the erythrocytic development of Plasmodium falciparum strains with different chloroquine-resistance status. Bispyrrolo[1,2-a]quinoxalines showed superior antimalarial activity with respect to monopyrrolo[1,2-a]quinoxalines. The best activity was observed with bispyrrolo[1,2-a]quinoxalines linked by a bis(3-aminopropyl)piperazine. Moreover, it was observed that the presence of a methoxy group on the pyrrolo[1,2-a]quinoxaline nucleus increased the pharmacological activity. Drug effects upon β-hematin formation were assayed and showed similar or higher inhibitory activities than CQ. A possible mechanism of interaction implicating binding of pyrroloquinoxalines to β-hematin was supported by molecular modeling.
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines
Prunier, Hervé,Rault, Sylvain,Lancelot, Jean-Charles,Robba, Max,Renard, Pierre,Delagrange, Philippe,Pfeiffer, Bruno,Caignard, Daniel-Henri,Misslin, René,Guardiola-Lemaitre, Béatrice,Hamon, Michel
, p. 1808 - 1819 (2007/10/03)
In continuation of our previous work on piperazinopyrrolothienopyrazine derivatives, three series of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines were prepared and evaluated as 5-HT3 receptor ligands. The chemical modifications performed within these new series led to structure-activity relationships regarding both high affinity and selectivity for the 5-HT3 receptors that are in agreement with those established previously for the pyrrolothienopyrazine series. The best compound (8a) obtained in these new series is in the picomolar range of affinity for 5-HT3 receptors with a selectivity higher than 106. Four of the high-affinity 5-HT3 ligands (8a, 15a,b, and 16d) were selected in both the pyridopyrrolopyrazine and the pyrroloquinoxaline series and were characterized in vitro and in vivo as agonists or partial agonists. Compound 8a was also evaluated in the light/dark test where it showed potential anxiolytic-like activity at very low doses per os.
Tricyclic pyrrolopyrazine 5-HT3 -active compounds
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, (2008/06/13)
The present invention relates to a compound selected from these of formula (I): STR1 in which A and R1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to the 5-HT3 receptors.
Pyridopyrrolopyrazines
Lancelot, Jean-Charles,Rault, Sylvain,Laduree, Daniel,Robba, Max
, p. 2798 - 2802 (2007/10/02)
Pyridopyrrolopyrazines are prepared by intramolecular cyclization of (pyrrolyl-1)-2 pyridine derivatives.Proton magnetic resonance (1H-HMR) are studied.