<abstract xmlns="http://www.w3.org/1999/xhtml"><p> Affordable and practical synthesis methods in drug development have always been very attractive. Herein, microwave assisted synthesis was utilized to prepare piperazine substituted 5-chloro-2(3H)-benzoxazolone derivatives in 5 minutes. Structural characterization of these 5-chloro-2(3H)-benzoxazolone derivatives was achieved by IR, NMR, ESI-MS and elemental analysis. Since these types of compounds have been shown to have anti-inflammatory and analgesic activities there biological activities were also examined. Indomethacin (INDO) and acetylsalicylic acid (ASA) were used as reference. Carrageenan-induced hind paw edema in mice test was used to study anti-inflammatory activity. Compound 1 (100 mg / kg dose) showed the longest anti-inflammatory activity among the title compounds synthesized. For the analgesic activities, both hot-plate and tail-flick tests were employed. Compound 3 was found to have the highest activity in the hot-plate test whereas in the tail-flick test, compounds 1 and 2 showed higher anti-nociceptive activity.</p></abstract>

Affordable and practical synthesis methods in drug development have always been very attractive. Herein, microwave assisted synthesis was utilized to prepare piperazine substituted 5-chloro-2(3H)-benzoxazolone derivatives in 5 minutes. Structural characterization of these 5-chloro-2(3H)-benzoxazolone derivatives was achieved by IR, NMR, ESI-MS and elemental analysis. Since these types of compounds have been shown to have anti-inflammatory and analgesic activities there biological activities were also examined. Indomethacin (INDO) and acetylsalicylic acid (ASA) were used as reference. Carrageenan-induced hind paw edema in mice test was used to study anti-inflammatory activity. Compound 1 (100 mg / kg dose) showed the longest anti-inflammatory activity among the title compounds synthesized. For the analgesic activities, both hot-plate and tail-flick tests were employed. Compound 3 was found to have the highest activity in the hot-plate test whereas in the tail-flick test, compounds 1 and 2 showed higher anti-nociceptive activity.

Synthesis and analgesic activities of some new 5-chloro-2(3H)-benzoxazolone derivatives

The EuroBiotech Journal

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Affordable and practical synthesis methods in drug development have always been very attractive. Herein, microwave assisted synthesis was utilized to prepare...

Synthesis and analgesic activities of some new 5-chloro-2(3H)-benzoxazolone derivatives

Publié en ligne: 20 juil. 2017

Pages: 235 - 240

DOI: https://doi.org/10.24190/ISSN2564-615X/2017/03.07

© 2018

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.