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Volumn 20, Issue 15, 2010, Pages 4399-4405

Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity

Author keywords

Agonist; Amide; MC4R; Melanocortin subtype 4 receptor; MK 0489; Obesity; Privileged structure; Spiroindane

Indexed keywords

DEXFENFLURAMINE; MELANOCORTIN RECEPTOR AGONIST; MK 0489; SPIROINDANE; UNCLASSIFIED DRUG;

EID: 77955418066     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.06.062     Document Type: Article
Times cited : (15)

References (35)
  • 26
    • 77955425131 scopus 로고    scopus 로고
    • In this communication, the lower case r or s in the compound number designates the R or S configuration at the stereogenic carbon of the spiroindane
    • In this communication, the lower case r or s in the compound number designates the R or S configuration at the stereogenic carbon of the spiroindane.
  • 27
    • 77955430327 scopus 로고    scopus 로고
    • All data are mean values for at least three separate experiments. For a detailed description of the assay protocols, see
    • All data are mean values for at least three separate experiments. For a detailed description of the assay protocols, see.
  • 31
    • 77955432463 scopus 로고    scopus 로고
    • We were able to establish the R/S configuration analog 9r and 9s (see discussion later in the text)
    • We were able to establish the R/S configuration analog 9r and 9s (see discussion later in the text).
  • 32
    • 77955430117 scopus 로고    scopus 로고
    • note
    • 2 (0.5 mL) and treated with 4 M HCl in dioxane (2 mL) at rt. Upon completion of de-Boc, the mixture was concentrated in vacuo. The residue was dissolved in DMF (2 mL) and treated with N-methylmorpholine (NMM) (94 μL, 0.858 mmol), followed by HOAt (58 mg, 0.429 mmol), HATU (163 mg, 0.429 mmol) and acid 5 (49 mg, 0.172 mmol). The mixture was stirred overnight at rt. The mixture was then treated with 3,3-difluoroazetidine HCl salt (185 mg, 1.43 mmol) and NMM (314 μL, 2.86 mmol) at rt. Upon completion of reaction, the mixture was purified by reverse HPLC to give the analog 28s.
  • 34
    • 84855634809 scopus 로고    scopus 로고
    • 50) on mouse MC3R.
    • 50) on mouse MC3R.
  • 35
    • 77955421835 scopus 로고    scopus 로고
    • Control 1 was discovered previously in our laboratories. Ujjainwalla, F; Sings, H. L. unpublished results.
    • Control 1 was discovered previously in our laboratories. Ujjainwalla, F; Sings, H. L. unpublished results.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.