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Volumn 15, Issue 4, 2007, Pages 1586-1605

4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors

Author keywords

Acetylene; Adenosine kinase; Analgesic; Inhibitor

Indexed keywords

5 (3 BROMOPHENYL) 7 (6 MORPHOLIN 4 YLPYRIDIN 3 YL)PYRIDO[2,3 D]PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 (2 MORPHOLIN 4 YLPYRIMIDIN 5 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 (4 DIMETHYLAMINOPHENYLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 (4 MORPHOLIN 4 YLPHENYLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 (5 MORPHOLIN 4 YLPYRIDIN 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 (6 DIMETHYLAMINOPYRIDIN 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 (6 MORPHOLIN 4 YLPYRIDIN 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 (4 CHLOROPHENYL) 6 [6 [(2 METHOXYETHYL)METHYLAMINO]PYRIDIN 3 YLETHYNYL]PYRIMIDIN 4 YLAMINE; 5 (4 DIMETHYLAMINOPHENYL) 6 (6 MORPHOLIN 4 YLPYRIDIN 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 BENZO[1,3]DIOXOL 5 YL 6 (6 MORPHOLIN 4 YLPYRIDIN 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 BENZO[B]THIOPHEN 2 YL 6 (6 MORPHOLIN 4 YLPYRIDINE 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 5 BENZOFURAN 2 YL 6 (6 MORPHOLIN 4 YLPYRIDIN 3 YLETHYNYL)PYRIMIDIN 4 YLAMINE; 6 (6 MORPHOLIN 4 YLPYRIDIN 3 YLETHYNYL) 5 THIOPHEN 2 YLPYRIMIDIN 4 YLAMINE; ABT 702; FORMALDEHYDE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 33847771147     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2006.12.029     Document Type: Article
Times cited : (29)

References (69)
  • 7
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    • note
    • See the supplemental section for a list of key references.
  • 29
    • 0000509322 scopus 로고
    • Trost B.M., and Fleming I. (Eds), Pergamon, Oxford
    • Sonogashira K. In: Trost B.M., and Fleming I. (Eds). Comprehensive Organic Synthesis Vol. 3 (1991), Pergamon, Oxford 521-549
    • (1991) Comprehensive Organic Synthesis , vol.3 , pp. 521-549
    • Sonogashira, K.1
  • 36
    • 33847791642 scopus 로고    scopus 로고
    • note
    • These bis acetylene analogs were screened and found to be inactive as AK inhibitors.
  • 45
    • 33847776256 scopus 로고    scopus 로고
    • note
    • Palladium scavengers were not attempted.
  • 60
    • 33847771780 scopus 로고    scopus 로고
    • note
    • cell) as well.
  • 61
    • 33847778410 scopus 로고    scopus 로고
    • Leo, A. c log P, v 4.81 program available from Biobyte corp. Claremont, CA. Biobyte home page. http://biobyte.com. Purchased from Daylight.
  • 62
    • 33847789962 scopus 로고    scopus 로고
    • note
    • % MPE = % maximal protective effect ([postdrug latency] - [vehicle latency])/([maximum latency] - [vehicle latency]) × 100%, where maximum (cutoff) latency was 180 s. Values represent means within ±8% and p < 0.05 to vehicle treated mice.
  • 65
    • 33847790114 scopus 로고    scopus 로고
    • note
    • Initial attempts to synthesize a C(2)′ analog were unsuccessful. Studies were carried out on the C(5)′ and C(6)′ compounds only.
  • 66
    • 33847770817 scopus 로고    scopus 로고
    • note
    • In previous studies (unreported), it was found the ABT-702 was metabolized primarily at the morpholine ring to give three components.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.