New thymol-3,4-disubstitutedthiazole hybrids were synthesised as dual COX-2/5-LOX inhibitors. Compounds , , , and displayed inhibitory activity against COX-2 (IC= 0.037, 0.042, 0.046, and 0.039 µM nearly equal to celecoxib (IC= 0.045 µM. , , and showed SI (379, 341, and 374, respectively) higher than that of celecoxib (327). - elicited 5-LOX inhibitory activity higher than quercetin. -, -, , and possessed inhibition of formalin induced paw edoema higher than celecoxib. , , , -, and showed gastrointestinal safety profile as celecoxib and diclofenac sodium in the population of fasted rats. Induced fit docking and molecular dynamics simulation predicted good fitting of and without changing the packing and globularity of the apo protein. In conclusion, and achieved the target goal as multitarget inhibitors of inflammation.
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| http://dx.doi.org/10.1080/14756366.2024.2309171 | DOI Listing |
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