Abstract
New series of diarylpyrazoles 8a-f and triarylimidazoline-5-ones 11a-g were synthesized and evaluated for their in vitro cyclooxygenase-1 (COX-1) and COX-2 inhibitory activity and in vivo anti-inflammatory activity. The synthesized compounds showed good selectivity for COX-2; compounds 8a, 8d, 8f, 11a, and 11c exhibited the highest COX-2 selectivity indexes (SI = 4.77-5.43) compared to the reference drug celecoxib (SI = 7.8). All compounds showed good in vivo anti-inflammatory activity, especially compounds 8a, 8f, 11c, and 11d, which also showed some similarities to the time interval pattern of celecoxib at all different time intervals (1, 3, and 6 h).
Keywords:
Anti-inflammatory; Imidazoline; Pyrazole; Selective COX-2 inhibitor.
© 2017 Deutsche Pharmazeutische Gesellschaft.
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Celecoxib / pharmacology
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Cyclooxygenase 1 / drug effects
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Cyclooxygenase 1 / metabolism
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Cyclooxygenase 2 Inhibitors / chemical synthesis
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Cyclooxygenase 2 Inhibitors / chemistry
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Cyclooxygenase 2 Inhibitors / pharmacology*
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Cyclooxygenase Inhibitors / chemical synthesis
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Humans
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Imidazolines / chemical synthesis
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Imidazolines / chemistry
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Imidazolines / pharmacology*
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Male
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Rats
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Rats, Wistar
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Sheep
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors
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Imidazolines
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Pyrazoles
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Cyclooxygenase 1
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Celecoxib