Synthesis of Newer Substituted Thiadiazolyl and Pyrazolyl Phenothiazines as Potent Anti-Inflammatory Agents

Deepak Kumar¹, R. C. Agarwal¹, Sudhir Kumar Bhati² and Ashok Kumar

¹Department of Chemistry, D.N. (P.G) College, Meerut - 250 002 (India).

²Department of Bio-Technology, I.A.M.R, Ghaziabad (India).

³Medicinal Chemistry Division, Department of Pharmacology, L.L.R.M. Medical College, Meerut - 250 004 (India).

N-(5-((10H-phenothiazin-10-yl)methyl)-1,3,4-thiadiazol-2-yl)-3-(substituted phenyl) acryl- amide (5a-5j) and 1-(3-(5-((10H-phenothiazin-10-yl)methyl)-1,3,4-thiadiazol-2-yl)-5-(sub- stituted phenyl)-4,5-dihydro-1H-pyrazol-1-yl) ethanone (6a-6j), were screened for their anti-inflammatory and analgesic activities at a dose of 50 mg/kg,p.o. The synthesized compounds were screened for their in vitro anti-inflammatory activity against for carrageenan induced rat paw oedema. The compounds were also tested for their analgesic activity against phenyl butazone against induced pain syndrome in mice. Compounds 5e and 6e were found to be most active compounds of this series, which shows 45.68% and 48.63% inflammation inhibitory and 35.86% and 45.15% analgesic activities respectively. The structural assignments of compounds have been made on the basis of elemental analysis, IR.1H-NMR and mass spectral data.

Thiadiazolyl phenothiazine; Pyrazolyl phenothiazine; Anti-inflammatory; Analgesic; Toxicity studies