Novel carbazole derivatives as NPY Y1 antagonists

Leslie, Colin P.; Fabio, Romano Di; Bonetti, Francesca; Borriello, Manuela; Braggio, Simone; Forno, Giovanna Dal; Donati, Daniele; Falchi, Alessandro; Ghirlanda, Damiano; Giovannini, Riccardo; Pavone, Francesca; Pecunioso, Angelo; Pentassuglia, Giorgio; Pizzi, D.; Rumboldt, Giovanna; Stasi, Luigi

doi:10.1016/j.bmcl.2006.11.034

Cited by 20 publications

(9 citation statements)

References 12 publications

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“…These findings, associated with the fact that 1229U91 markedly suppressed food intake of Zucker fatty rat but induced a slight suppression in Zucker lean rats, suggest that NPY also regulates daily food intake in normal animals without overeating and that the NPY-ergic system might be overactivated in Zucker fatty rats (170,178 (179). Most of Y 1 antagonists reported, however, present pharmacokinetic weaknesses that limit CNS exposure after oral administration (180). For this reason, a series of carbazole derivatives with improved pharmacokinetic properties were synthesized (180,181), including a high-affinity Y 1 ligand that shows high brain penetration and modest oral bioavailability (180).…”

Section: A Npy Receptor Antagonistsmentioning

confidence: 71%

“…Most of Y 1 antagonists reported, however, present pharmacokinetic weaknesses that limit CNS exposure after oral administration (180). For this reason, a series of carbazole derivatives with improved pharmacokinetic properties were synthesized (180,181), including a high-affinity Y 1 ligand that shows high brain penetration and modest oral bioavailability (180). These data may be helpful in future development studies of pharmaceutical agents.…”

Section: A Npy Receptor Antagonistsmentioning

confidence: 99%

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Neuropeptide Y Receptor Selective Ligands in the Treatment of Obesity

Kamiji

Inui

2007

Endocrine Reviews

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Section: A Npy Receptor Antagonistsmentioning

confidence: 71%

Section: A Npy Receptor Antagonistsmentioning

confidence: 99%

Neuropeptide Y Receptor Selective Ligands in the Treatment of Obesity

Kamiji

Inui

2007

Endocrine Reviews

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“…Contrave, the candidate of Orexigen Therapeutics, is a combination therapy containing bupropion (91), an antidepressant that upheaves dopamine signaling, and naltrexone (92), an antiaddiction drug that acts as an opioid receptor antagonist. Both compounds are already FDA-approved and have established safety records.…”

Section: Bupropionmentioning

confidence: 99%

New Trends in Medicinal Chemistry Approaches to Antiobesity Therapy

Lee¹,

Song²,

Kang³

et al. 2009

CTMC

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The prevalences of overweightedness and obesity are increasing globally at frightening rates, driven by social and economic changes. Furthermore, obesity is associated with the pathogeneses of major diseases, particularly diabetes and cardiovascular diseases. However, no satisfactorily safe, effective obesity drugs are commercially available at the present time. Only two drugs have been approved in the United States for the long-term treatment of obesity, sibutramine and orlistat. However, these drugs are minimally effective and have significant side effects, which are likely inhibit their use. Therefore, there is a huge opportunity to make a significant impact on the lives of obese people through the discovery and development of additional pharmacotherapeutic options. In this review article, the authors focus on selected trends in medicinal chemistry and the approaches used to develop drugs for treating obesity.

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“…22 Compound 47 was found to have a high affi nity for NPY, but had poor permeability properties in vivo with a B/P ratio of 0.1. 22 Compound 47 was found to have a high affi nity for NPY, but had poor permeability properties in vivo with a B/P ratio of 0.1.…”

Section: B P K Amentioning

confidence: 99%