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Volumn 18, Issue 11, 2008, Pages 3242-3247

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators

Author keywords

G protein coupled receptor; Melanocortin subtype 4 receptor agonist; Obesity; Oral bioavailability

Indexed keywords

MELANOCORTIN 4 RECEPTOR; PYRROLIDINE DERIVATIVE; TERT BUTYLPYRROLIDINE DERIVATIVE;

EID: 44149120045     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.04.049     Document Type: Article
Times cited : (17)

References (21)
  • 15
    • 44149090396 scopus 로고    scopus 로고
    • Ujjainwalla, F. Presentation (MEDI-275), 230th ACS National Meeting, Washington, DC, August 28-September 1, 2005.
    • Ujjainwalla, F. Presentation (MEDI-275), 230th ACS National Meeting, Washington, DC, August 28-September 1, 2005.
  • 16
    • 44149110743 scopus 로고    scopus 로고
    • Ujjainwalla, F et al., unpublished results (in preparation).
    • Ujjainwalla, F et al., unpublished results (in preparation).
  • 17
    • 44149124746 scopus 로고    scopus 로고
    • note
    • Intermediate 3B was synthesized in a similar way as described in Ref. 3 for compound 1.
  • 18
    • 44149114853 scopus 로고    scopus 로고
    • 50 was defined as the inflection point of the cAMP dose-response curve for any given compounds. Maxi percentage activation [% Max] is the percentage of cAMP accumulation at 10 μM of compound relative to α-MSH.
    • 50 was defined as the inflection point of the cAMP dose-response curve for any given compounds. Maxi percentage activation [% Max] is the percentage of cAMP accumulation at 10 μM of compound relative to α-MSH.
  • 21
    • 44149127334 scopus 로고    scopus 로고
    • note
    • The stereochemistry of 1-tert-butyl-4-aryl pyrrolidine-3-carboxylic acid substructure in 2B is same as in 1 and defined as shown in Ref. 3. The slow eluting isomers discussed in this paper were assumed to have the same stereochemistry as 2B, which is also the slow eluting isomer, under the same chiral HPLC conditions.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.