1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT7 receptor ligands

Isaac, Methvin; Tao, Xin; O’Brien, Anne; St-Martin, David; Naismith, Angela; MacLean, Neil; Wilson, Julie M.; Demchyshyn, Lidia; Tehim, Ashok; Slassi, Abdelmalik

doi:10.1016/s0960-894x(02)00438-9

Cited by 11 publications

(7 citation statements)

References 11 publications

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“…To widen the substitution of 1-position of pyrazolo [3,4-b]pyridine-3-ones, we decided to introduce a bromoethane linker in order to incorporate a bicyclic compound such as a saturated pyridodiazepine known to interact with 5-HT 7 /5-HT 1A receptors [11].…”

Section: Resultsmentioning

confidence: 99%

Synthesis of new compounds containing the pyrazolo[3,4‐b]pyridine‐3‐one subunit

Fadel

Suzenet

Hafid

et al. 2009

Journal of Heterocyclic Chem

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in Wiley InterScience (www.interscience.wiley.com).A convenient route for the synthesis of pyrazolo [3,4-b]pyridine-3-ones via condensation of 3-amino-1-phenylpyrazolin-5-one with 4-hydroxy-6-methylpyran-2-one is described. The pyrazolo[3,4-b]pyridine-3-one isomers obtained were functionalized at 1-, 4-, or 6-position by different pharmacophore entities allowing the synthesis of new compounds with promising biological activities.

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Section: Resultsmentioning

confidence: 99%

Synthesis of new compounds containing the pyrazolo[3,4‐b]pyridine‐3‐one subunit

Fadel

Suzenet

Hafid

et al. 2009

Journal of Heterocyclic Chem

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“…Interestingly, the 6-trifluoromethyl substituent led to a slight increase in receptor affinity (K i = 23 nM). The most potent compound (85) was found to be very selective when tested against other serotonin receptors, dopamine receptors and muscarinic receptors [87].…”

Section: Emerging 5-ht 7 Receptor Antagonistsmentioning

confidence: 99%

Recent progress in 5-HT₇receptors: potential treatment of central and peripheral nervous system diseases

Slassi¹,

Isaac²,

Tao³

2004

Expert Opinion on Therapeutic Patents

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In light of the barrage of recent reviews on 5-HT 7 receptor agonists and antagonists, this article will highlight and review the research advances published in the patent literature between January 1997 and December 2003. The article is supplemented with selected references on the design, synthesis and development of novel 5-HT 7 agents to treat central and peripheral nervous system diseases. Emphasis is placed on recent advances in the possible involvement of 5-HT 7 serotonergic agents in the treatment of learning and memory, depression, schizophrenia and migraine. By no means has any attempt been made to exhaustively review the literature, but rather, primary references together with citations to recent literature reviews have been included in each section.

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“…A few years ago, during their studies on the 5-HT 1D receptor, Isaac et al serendipitously discovered a new series of indole-based 5-HT 7 ligands 16 . The most potent agent (4, K i = 3 nM for 5-HT 7 R; % inhibition at 1 µM = 99 for 5-HT 7 R and % inhibition at 1 M ≤35 for 5-HT 1A , 1B , 1D , 1F , 2A , shows an interesting selectivity profile over the other tested G-protein coupled receptors (GPCRs) ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

New insights into homopiperazine-based 5-HT_1A/5-HT₇R ligands: synthesis and biological evaluation

Badarau

Putey

Suzenet

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT7 receptor ligands

Cited by 11 publications

References 11 publications

Synthesis of new compounds containing the pyrazolo[3,4‐b]pyridine‐3‐one subunit

Synthesis of new compounds containing the pyrazolo[3,4‐b]pyridine‐3‐one subunit

Recent progress in 5-HT₇receptors: potential treatment of central and peripheral nervous system diseases

New insights into homopiperazine-based 5-HT_1A/5-HT₇R ligands: synthesis and biological evaluation

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1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT7 receptor ligands

Cited by 11 publications

References 11 publications

Synthesis of new compounds containing the pyrazolo[3,4‐b]pyridine‐3‐one subunit

Synthesis of new compounds containing the pyrazolo[3,4‐b]pyridine‐3‐one subunit

Recent progress in 5-HT7receptors: potential treatment of central and peripheral nervous system diseases

New insights into homopiperazine-based 5-HT1A/5-HT7R ligands: synthesis and biological evaluation

Contact Info

Product

Resources

About

Recent progress in 5-HT₇receptors: potential treatment of central and peripheral nervous system diseases

New insights into homopiperazine-based 5-HT_1A/5-HT₇R ligands: synthesis and biological evaluation