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Volumn 20, Issue 3, 2010, Pages 1219-1224

Synthesis and evaluation of two series of 4′-aza-carbocyclic nucleosides as adenosine A2A receptor agonists

Author keywords

Adenosine A2A receptor agonists; Anti inflammatory; Carbocyclic nucleosides

Indexed keywords

2 HEXYNYL 5' N ETHYLCARBOXAMIDOADENOSINE; 2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A2A RECEPTOR AGONIST; ANTIINFLAMMATORY AGENT; CARBOCYCLIC NUCLEOSIDE; GW 328267X; PROPIONAMIDE DERIVATIVE; UNCLASSIFIED DRUG; ADENOSINE A2 RECEPTOR AGONIST; ADENOSINE A2A RECEPTOR; CARBOXYLIC ACID; HETEROCYCLIC COMPOUND; NUCLEOSIDE; PYRIMIDINE NUCLEOTIDE;

EID: 74049150722     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.11.131     Document Type: Article
Times cited : (14)

References (38)
  • 15
    • 85081498034 scopus 로고
    • Adenosine-5′-Carboxylic Acid Amides
    • U.S. Patent 3,914,415, Oct. 21
    • Stein, H. H.; Prasad, R. N. Adenosine-5′-Carboxylic Acid Amides. U.S. Patent 3,914,415, Oct. 21, 1975.
    • (1975)
    • Stein, H.H.1    Prasad, R.N.2
  • 17
    • 85081497247 scopus 로고    scopus 로고
    • Chan, C, Cousins, R. P. C, Cox, B. 2-(Purin-9-yl)-tertrahydrofuran-3,4-diol derivatives. WO 99/38877, Aug. 5, 1999
    • Chan, C.; Cousins, R. P. C.; Cox, B. 2-(Purin-9-yl)-tertrahydrofuran-3,4-diol derivatives. WO 99/38877, Aug. 5, 1999.
  • 18
    • 85081503536 scopus 로고    scopus 로고
    • note
    • Electron density calculations were carried out using Jaguar 7.5 from the Schrödinger 2008 modelling suite software to build and minimise the 4′-substituents. For the minimisation: density functional theory was used with the B3LYP functional and 6-311G** basis sets. The default settings were used with an accuracy level of 'accurate'. For the final geometry the electrostatic potential was calculated and displayed. For the images the range of the colour ramp was set the same for all of the three substituents shown in Figure 2.
  • 32
    • 85081503134 scopus 로고    scopus 로고
    • note
    • 6 cells/ml (neutrophil purity >97%) and 50 μl dispensed per assay well (Sigmacote® treated). Test article was added (50 μl) and after a 30 min preincubation at 37 °C solutions of lucigenin (50 μl of a 400 μM solution) and then formylated tripeptide MLP (fMLP) (50 μl of a 4 μM solution) were added. Release of reactive oxygen species was assessed from the chemiluminescence generated over the 4 min incubation period following fMLP addition.
  • 38
    • 85081527332 scopus 로고    scopus 로고
    • note
    • 2A receptor mediated.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.