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Volumn 16, Issue 14, 2010, Pages 4250-4258

General method for the C-labeling of 2-arylpropionic acids and their esters: Construction of a PET tracer library for a study of biological events involved in COXs expression

Author keywords

Anti inflammatory drugs; C c coupling; Cyclooxygenase; Inflammation; Positron emission tomography

Indexed keywords

ACIDS; ALKYLATION; BIOCHEMISTRY; DRUG PRODUCTS; ESTERIFICATION; ESTERS; HYDROLYSIS; LABELING; METHYLATION; PATHOLOGY; POSITRONS; SYNTHESIS (CHEMICAL);

EID: 77950846318     PISSN: 09476539     EISSN: 15213765     Source Type: Journal    
DOI: 10.1002/chem.200903044     Document Type: Article
Times cited : (47)

References (53)
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    • 11C][14]methyl-fatty acids was reported, it requires three steps including methylation, hydrolysis, and decarboxylation to give our desired compounds. See reference
    • 11C][14]methyl-fatty acids was reported, it requires three steps including methylation, hydrolysis, and decarboxylation to give our desired compounds. See reference: K. Ogawa, M. Sasaki, T Nozaki, Appl. Radiat, Isot. 1997, 48, 623-630.
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    • All products were isolated as a racemic mixture. Generally, the S enantiomer of 2-arylproiponic acid is pharmacologically active in terms of the cyclooxygenase inhibition. However, the majority of 2arylpropionic acids are prepared in a racemic mixture because an isomerase enzyme (2-arylpropionyl-CoA pimerase) exists in vivo system that converts the inactive R enantiomer into the active S form, see: a exceptionally, a few inhibitors, such as Flurbiprofen, undergo such a bioconversion to a very little extent in vitro or in vivo systems, see
    • All products were isolated as a racemic mixture. Generally, the S enantiomer of 2-arylproiponic acid is pharmacologically active in terms of the cyclooxygenase inhibition. However, the majority of 2arylpropionic acids are prepared in a racemic mixture because an isomerase enzyme (2-arylpropionyl-CoA pimerase) exists in vivo system that converts the inactive R enantiomer into the active S form, see: a) C. Reichel, R. Brugger, H. Bang, G. Geisslinger, K. Brune, Mol. Pharmacol. 1997, 51, 576-582; exceptionally, a few inhibitors, such as Flurbiprofen, undergo such a bioconversion to a very little extent in vitro or in vivo systems, see:
    • (1997) Mol. Pharmacol. , vol.51 , pp. 576-582
    • Reichel, C.1    Brugger, R.2    Bang, H.3    Geisslinger, G.4    Brune, K.5
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    • note
    • -1; UV detection: 254 nm). If necessary, the use of an optically active PET tracer will be reported with the detailed resolution method in due course.
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    • It should be added that this rapid methylation could also be applied to other 2-arylpropionic acid derivatives of NSAIDs, such as, Benoxaprofen, Cycloprofen, Pranoprofen, etc. to form a larger PET tracer library.
    • It should be added that this rapid methylation could also be applied to other 2-arylpropionic acid derivatives of NSAIDs, such as, Benoxaprofen, Cycloprofen, Pranoprofen, etc. to form a larger PET tracer library.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.