期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 77, 期 -, 页码 185-192出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.003
关键词
Chromone; Indole; Pyrazole; Interactions; Cyclooxygenase-2; Inhibitors
资金
- Department of Science & Technology, New Delhi
- Council of Scientific & Industrial Research, New Delhi
- UGC, New Delhi
- DST, New Delhi
Conjugates of chromone-indole and chromone-pyrazole were screened for cyclooxygenase-2 (COX-2), cyclooxygenase-1 (COX-1) and 5-lipoxygenase (5-LOX) inhibitory activities. Compounds 8 and 9 were identified as preferred inhibitors of COX-2 over the other two enzymes. Their IC50 for COX-2 was 29 nM and 20 nM, respectively and selectivity indices (SI) for COX-2 over COX-1 was 46 and 337. NMR, mass spectral studies and molecular modelling also indicated preferential interactions of compounds 8 and 9 with COX-2. Tested on albino mice against capsaicin induced algesia, compound 8 exhibited analgesic potential comparable to diclofenac. In addition to the biological profile, the desirable physico-chemical properties of these compounds make them promising leads for anti-inflammatory drugs. (C) 2014 Elsevier Masson SAS. All rights reserved.
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