Home About us Editorial board Ahead of print Current issue Search Archives Submit article Instructions Subscribe Contacts Login 
  • Users Online: 34
  • Home
  • Print this page
  • Email this page
Cover page of the Journal of Health Sciences
Year : 2019  |  Volume : 12  |  Issue : 1  |  Page : 35-43

Design, synthesis, and biological evaluation of novel diclofenac analogs as promising anti-inflammatory agents

Department of Pharmaceutical Chemistry, KLE College of Pharmacy, Hubli, Karnataka, India

Correspondence Address:
Dr. Mahesh B Palkar
Department of Pharmaceutical Chemistry, KLE College of Pharmacy, Vidya Nagar, Hubli - 580 031 Karnataka
Login to access the Email id

Source of Support: None, Conflict of Interest: None

DOI: 10.4103/kleuhsj.kleuhsj_151_18

Rights and Permissions

INTRODUCTION: Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used as analgesics and antipyretics in the treatment of pain, fever, and rheumatoid arthritis. Major side effect with treatment of NSAIDs is gastric irritation. 1,3,4-thiadiazole is an imperative scaffold since several of these derivatives are known to be associated with multiple biological activities such as anti-inflammatory, antibacterial, anti-cancer, anti-tubercular, and immunosuppressive. Literature survey reveals that certain compounds bearing this nucleus possess significant anti-inflammatory activity with reduced ulcerogenic effect. MATERIALS AND METHODS: In the present research work, we have synthesized thirteen 2-(2-[2,6-dichlorophenylamino] phenyl) acetohydrazide derivatives (4a–4m) and four 2,6-dichloro-N-(2-[6-phenylimidazo[2,1-b][1,3,4]thiadiazol-yl] methyl] phenyl) benzenamine derivatives (6a–6d) derived from diclofenac. All these newly synthesized compounds were screened for in vivo acute anti-inflammatory activity by carrageenan-induced rat paw edema method at a dose of 10 mg/kg bw. RESULTS AND DISCUSSION: Structures of these novel compounds were characterized based on their physicochemical and spectral analysis. Perusal of the activity data strongly suggests that compound 4d was most promising with significant anti-inflammatory activity, while moderate to good activity was observed for compounds 4a, 4c, g, 4i, and 4l. Among the imidazo (2,1-b) 1,3,4-thiadiazole series (6a–6d), compound 6b exhibited excellent anti-inflammatory activity, while compounds 6a, 6c and 6d displayed reasonably to good anti-inflammatory activity as compared to standard drug diclofenac. CONCLUSION: Among the series of synthesized compounds, two derivatives (4d and 6b) have displayed the most encouraging results and could be further exploited for developing newer anti-inflammatory agents with better efficacy and safety, which necessitates further investigations.

Print this article     Email this article
 Next article
 Previous article
 Table of Contents

 Similar in PUBMED
   Search Pubmed for
   Search in Google Scholar for
 Related articles
 Citation Manager
 Access Statistics
 Reader Comments
 Email Alert *
 Add to My List *
 * Requires registration (Free)

 Article Access Statistics
    PDF Downloaded122    
    Comments [Add]    

Recommend this journal