Literature DB >> 15713408

Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.

Brian M Smith1, Jeffrey M Smith, James H Tsai, Jeffrey A Schultz, Charles A Gilson, Scott A Estrada, Rita R Chen, Douglas M Park, Emily B Prieto, Charlemagne S Gallardo, Dipanjan Sengupta, William J Thomsen, Hazel R Saldana, Kevin T Whelan, Frederique Menzaghi, Robert R Webb, Nigel R A Beeley.   

Abstract

We report on the synthesis, biological evaluation and structure-activity relationships for a series of 3-benzazepine derivatives as 5-HT(2C) receptor agonists. The compounds were evaluated in functional assays measuring [3H] phosphoinositol turnover in HEK-293 cells transiently transfected with h5-HT(2C), h5-HT(2A) or h5-HT(2B) receptors. Several compounds are shown to be potent and selective 5-HT(2C) receptor agonists, which decrease food intake in a rat feeding model.

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Year:  2005        PMID： 15713408     DOI： 10.1016/j.bmcl.2004.12.080

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

Review 1.  Serotonergic drugs : effects on appetite expression and use for the treatment of obesity.

Authors:  Jason C G Halford; Joanne A Harrold; Emma J Boyland; Clare L Lawton; John E Blundell
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Review 2.  Pharmacological management of appetite expression in obesity.

Authors:  Jason C G Halford; Emma J Boyland; John E Blundell; Tim C Kirkham; Joanne A Harrold
Journal:  Nat Rev Endocrinol       Date:  2010-03-16       Impact factor: 43.330

3.  Regioselective alkylation of 1,3,4,5-tetrahydrobenzo[d]azepin-2-one and biological evaluation of the resulting alkylated products as potentially selective 5-HT₂c agonists.

Authors:  Navnit Prajapati; Rajani Giridhar; Anshuman Sinha; Ashish M Kanhed; Mange Ram Yadav
Journal:  Mol Divers       Date:  2015-04-28       Impact factor: 2.943

4.  Persistent attenuation of nicotine self-administration in rats by co-administration of chronic nicotine infusion with the dopamine D1 receptor antagonist SCH-23390 or the serotonin 5-HT2C agonist lorcaserin.

Authors:  Devon DiPalma; Amir H Rezvani; Blair Willette; Corinne Wells; Susan Slade; Brandon J Hall; Edward D Levin
Journal:  Pharmacol Biochem Behav       Date:  2018-11-09       Impact factor: 3.697

Review 5.  Pharmabiotics as an Emerging Medication for Metabolic Syndrome and Its Related Diseases.

Authors:  Thi Thanh Binh Nguyen; Yan Yan Jin; Hea-Jong Chung; Seong-Tschool Hong
Journal:  Molecules       Date:  2017-10-24       Impact factor: 4.411

Review 6.  Challenging obesity, diabetes, and addiction: the potential of lorcaserin extended release.

Authors:  Ryan T Hurt; Manpreet S Mundi; Jon O Ebbert
Journal:  Diabetes Metab Syndr Obes       Date:  2018-09-04       Impact factor: 3.168

7.  Synthesis of Chiral Tetrahydro-3-benzazepine Motifs by Iridium-Catalyzed Asymmetric Hydrogenation of Cyclic Ene-carbamates.

Authors:  Bram B C Peters; Pher G Andersson; Somsak Ruchirawat; Winai Ieawsuwan
Journal:  Org Lett       Date:  2022-03-03       Impact factor: 6.005

8.  Production of benzazepine derivatives via four-component reaction of isatins: study of antioxidant activity.

Authors:  Fathali Gholami Orimi; Behrooz Mirza; Zinatossadat Hossaini
Journal:  Mol Divers       Date:  2020-06-10       Impact factor: 2.943
  8 in total

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