2849-92-5Relevant academic research and scientific papers
Benzimidazole-2-carboxylic acid amides and esters: A new structural class of 5-HT3 ligands
Orjales, Aurelio,Alonso-Cires, Luisa,Lopez-Tudanca, Pedro,Tapia, Ines,Mosquera, Ramon,Labeaga, Luis
, p. 415 - 422 (1999)
A series of novel benzimidazole-2-carboxylic acid amides and esters with a quinuclidine or a tropane moiety were synthesized and evaluated for in vitro affinity for the 5-HT3, 5-HT4 and D2 receptors. Compounds 15a, 13j and 13h exhibited affinity for the 5-HT3 receptor (K(i) = 20.2, 18.4 and 12.7 nM, respectively) and no significant affinity for both 5-HT4 and D2 receptors. The amide-ester replacement did not induce significant changes in the affinity profile. The enantioselectivity for the 5-HT3 receptor was reversed with regard to the zacopride pattern and the (R)-enantiomer 13c showed higher affinity (K(i) = 56.4 nM) than the (S)-enantiomer 13d (K(i) = 242.3 nM). An increment of the steric hindrance around the nitrogen atom at the 1-position of the benzimidazole ring led to an improvement in the affinity. The 5-HT3 receptor antagonist activity of compounds with higher affinity was performed by evaluating the inhibition of the 5-HT induced von Bezold-Jarisch reflex. They displayed moderate 5-HT3 antagonist activity (ED50 = 10.6-29.1 μg/kg i.v.).
INHIBITORS OF MYOCARDIN-RELATED TRANSCRIPTION FACTOR AND SERUM RESPONSE FACTOR (MRTF/SRF)-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME
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Paragraph 00188, (2016/06/01)
Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor ("MRTF/SRF"), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
