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Analgesic, anti-inflammatory activity and docking study of 2-(substituted phenyl)-3-(naphthalen-1-yl)thiazolidin-4-ones
Author : Neetu Agrawal*, Prabhat K. Upadhyay, Somdutt Mujwar and Pradeep Mishra
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ABSTRACT
A potential analgesic and anti-inflammatory activities have been reported in 4-thiazolidinone analogs as well as some drugs bearing naphthyl moiety such as naproxen. Thus a reported series of 2-(substituted phenyl)-3-(naphthalen-1-yl)thiazolidin-4-ones (Tz1-10) was explored for analgesic and anti-inflammatory activities. The analgesic activity was determined using tail immersion and acetic acid-induced writhing model while the anti-inflammatory activity was determined using carageenan-induced paw edema method. The docking studies were also carried out to gain understanding of binding modes of the potent compounds in the COX-2 enzyme active cavity. The compounds Tz1, Tz5 and Tz6 emerged as potent analgesic and anti-inflammatory agents. The compounds displayed excellent binding interaction with the receptor with Tz6 showing the highest binding energy (–11.08 kcal/mol). Moreover, the synthesized compounds are predicted to have good oral bioavailability as shown by their physicochemical properties calculated using software. The naphthalenyl substituted thiazolidinones reported in the present study provide basis for further studies and future prospects for development of new anti-inflammatory and analgesic agents.
KEYWORD
4-Thiazolidinone, analgesic, anti-inflammatory, naphthylamine, Schiff’s base