We found a match
Your institution may have rights to this item. Sign in to continue.
- Title
Indole Derivatives as Cyclooxygenase Inhibitors: Synthesis, Biological Evaluation and Docking Studies.
- Authors
Bhat, Mashooq Ahmad; Al-Omar, Mohamed A.; Raish, Mohammad; Ansari, Mushtaq Ahmad; Abuelizz, Hatem A.; Bakheit, Ahmed H.; Naglah, Ahmed M.
- Abstract
A new series of 2-(5-methoxy-2-methyl-1<italic>H</italic>-indol-3-yl)-<italic>N</italic>′-[(<italic>E</italic>)-(substituted phenyl) methylidene] acetohydrazide derivatives (<bold>S1</bold>–<bold>S18</bold>) were synthesized and evaluated for their anti-inflammatory activity, analgesic activity, ulcerogenic activity, lipid peroxidation, ulcer index and cyclooxygenase expression activities. All the synthesized compounds were in good agreement with spectral and elemental analysis. Three synthesized compounds (<bold>S3</bold>, <bold>S7</bold> and <bold>S14</bold>) have shown significant anti-inflammatory activity as compared to the reference drug indomethacin. Compound <bold>S3</bold> was further tested for ulcerogenic index and cyclooxygenase (COX) expression activity. It was selectively inhibiting COX-2 expression and providing the gastric sparing activity. Docking studies have revealed the potential of these compounds to bind with COX-2 enzyme. Compound <bold>S3</bold> formed a hydrogen bond between OH of Tyr 355 and NH2 of Arg 120 with carbonyl group and this hydrogen bond was similar to that formed by indomethacin. This study provides insight for compound <bold>S3</bold>, as a new lead compound as anti-inflammatory agent and selective COX-2 inhibitor.
- Subjects
INDOLE derivatives; HETEROCYCLIC compound derivatives; CYCLOOXYGENASE inhibitors; CHEMICAL synthesis; ANTI-infective agents; DRUG efficacy; CHEMICAL reactions
- Publication
Molecules, 2018, Vol 23, Issue 6, p1250
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23061250