Synthesis and Molluscicidal Activity of Novel N-methyl Carbamate Derivatives Based on Naturally Occurring Monoterpenoids

Abstract: A series of novel N-methyl carbamate derivatives based on naturally ocurring monoterpenoids were synthesized and tested against Helix aspersa snails. The results showed that the new synthesized carbamate derivatives in particularly of broneol proved to be highly potent against the snails. Besides, the joint action effects of the four active derivatives namely; broneol, carvacrol, chlorothymol and thymol with either piperonyl butoxide or Triton-X 100 dramatically enhanced the molluscicidal activity over the standard molluscicide

Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors

New thymol − 1,5-disubstitutedpyrazole hybrids were synthesised as dual COX-2/5-LOX inhibitors. Compounds 8b, 8g, 8c, and 4a displayed in vitro inhibitory activity against COX-2 (IC50 = 0.043, 0.045, 0.063, and 0.068 µM) nearly equal to celecoxib (IC50 = 0.045 µM) with high SI (316, 268, 204, and 151, respectively) comparable to celecoxib (327). All target compounds, 4a–c and 8a–i, showed in vitro 5-LOX inhibitory activity higher than reference quercetin. Besides, they possessed in vivo inhibition of formalin-induced paw oedema higher than celecoxib. In addition, compounds 4a, 4b, 8b, and 8g showed superior gastrointestinal safety profile (no ulceration) as celecoxib and diclofenac sodium in the population of fasted rats. In conclusion, compounds 4a, 8b, and 8g achieved the target goal. They elicited in vitro dual inhibition of COX-2/5-LOX higher than celecoxib and quercetin, in vivo potent anti-inflammatory activity higher than celecoxib and in vivo superior gastrointestinal safety profile (no ulceration) as celecoxib. </p