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Volumn 18, Issue 2, 2008, Pages 586-595

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists

Author keywords

3 Benzylpiperidine; Ab initio; Acyclic scaffold; Asthma; CCR3 antagonist; Conformational analysis; Eosinophil chemotaxis

Indexed keywords

3 BENZYLPIPERIDINE DERIVATIVE; BMS 639623; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR3; UNCLASSIFIED DRUG;

EID: 38349028685     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.087     Document Type: Article
Times cited : (9)

References (19)
  • 2
    • 38349036959 scopus 로고    scopus 로고
    • note
    • For an abridged etiology of asthma and its eosinophil-contributing component, see Supplement in Ref. 1.
  • 3
    • 38349001787 scopus 로고    scopus 로고
    • note
    • 125I-labeled eotaxin and CHO cells stably transfected with a gene encoding human CCR3 as described in Ref. 4.
  • 5
    • 38349034142 scopus 로고    scopus 로고
    • note
    • 125I-labeled eotaxin and CHO cells stably transfected with a gene encoding a chimeric receptor, consisting of the intracellular domain of human CCR2 with the extracellular and transmembrane domains of human CCR3. This variation was found to give results nearly identical to those obtained using the native CCR3 receptor as shown below:{A figure is presented}Taken from U.S. 2005/0123972, published June 9, 2005.
  • 6
    • 38349046030 scopus 로고    scopus 로고
    • Ko, S. S.; Wang, J.; Clark, C. M.; Srivastava, A. S.; Chaudhari, A.; Batt, D. G.; Houghton, G.; DeLucca, G.; Duncia, J. V.; Welch, P. K.; Wadman, E. A.; Davies, P.; Solomon, K. A.; Graden, D. M.; Yeleswaram, S.; Decicco, C. P.; Carter, P. H., manuscript in preparation.
  • 8
    • 38349012410 scopus 로고    scopus 로고
    • Ab initio calculations were performed as disclosed in the previous letter in this series (Ref. 1, and then see Ref. 6 therein).
  • 10
    • 38349009773 scopus 로고    scopus 로고
    • note
    • It was at this point when the CCR3 discovery research program was concluded. Thus there are no chemotaxis inhibition data.
  • 11
    • 38349029750 scopus 로고    scopus 로고
    • note
    • 13C 2D NMR spectra were obtained at 500 MHz. {A figure is presented}
  • 17
    • 0026640040 scopus 로고
    • For approaches to designing conformationally rigid acyclic scaffolds which mimic conformationally preorganized acyclic natural products, see
    • For approaches to designing conformationally rigid acyclic scaffolds which mimic conformationally preorganized acyclic natural products, see. Hoffmann R.W. Angew. Chem., Int. Ed. Engl. 31 (1992) 1124
    • (1992) Angew. Chem., Int. Ed. Engl. , vol.31 , pp. 1124
    • Hoffmann, R.W.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.