Bioorganic & medicinal chemistry letters, 2006-07, Vol.16 (14), p.3674-3678
2006
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Details
- Autor(en) / Beteiligte
- Titel
- Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2006-07, Vol.16 (14), p.3674-3678
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2006
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Biaryl urea lead compound 1 was discovered earlier in our MCH antagonist program. Novel benzimidazole analogues with increased chemical stability, devoid of the potential carcinogenic liability associated with a biarylamine moiety, were synthesized and evaluated to be potent MCH R1 antagonists. Two compounds in this series have demonstrated in vivo efficacy in a rodent obesity model.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2006.04.062Titel-ID: cdi_proquest_miscellaneous_17187908
- Format
- –
- Schlagworte
- Administration, Oral, Animals, Antagonist, Anti-Obesity Agents - chemical synthesis, Anti-Obesity Agents - pharmacology, Benzimidazoles - chemical synthesis, Benzimidazoles - pharmacology, Biological and medical sciences, Body Weight - drug effects, Disease Models, Animal, Drug Design, Hormones. Endocrine system, Medical sciences, Melanin-concentrating hormone receptor, Obesity, Pharmacology. Drug treatments, Rats, Receptors, Pituitary Hormone - antagonists & inhibitors, Structure-Activity Relationship