Pharmacologyonline 2: 172-186 (2007) Raut et al. 172 ANTI-INFLAMMATORY, ANALGESIC, ULCEROGENIC ACTIVITIES OF SOME NEW NON-ACIDIC DICLOFENAC AND 1, 3, 4- OXADIAZOLE DERIVATIVES IN ANIMAL MODELS Mayuresh K. Raut, Shashikant V. Bhandari, Kailash G. Bothara, Ajit A. Patil, Aniket P. Sarkate Department of Pharmaceutical Chemistry, A.I.S.S.M.S College of Pharmacy, Pune, India. Summary Diclofenac sodium is an important component of prescriptions of arthritis patients since last 25 years. But even this drug is not an exception to the limitations of gastrointestinal adverse effects associated with the traditional non-selective NSAIDs. The free –COOH group is reported to be the main culprit responsible for GI toxicity of these NSAIDs. Derivatives of 1, 3, 4-oxadiazole are also known to have a broad spectrum of biological activities. Schiff bases and 1, 3, 4-oxadiazole derivatives of diclofenac were tested in vivo for their anti-inflammatory activity. The compounds, which showed significant analgesic and anti-inflammatory activities comparable to the standard drug diclofenac, were screened for their ulcerogenic potential to make sure that designed and synthesized compounds lack ulcerogenecity associated with parent prototype Diclofenac Sodium from traditional non-selective NSAIDs. The study showed that compound 3k possessed most significant anti-inflammatory and analgesic activity compared to parent drug Diclofenac Sodium. The compound also showed non ulcerogenic action at 12 times the therapeutic dose in animal models. The ulcers in rats were analyzed by histopathological studies. Results showed that compound 3e, 3g, 3k, 4c, 4e and control group were unremarkable, and were also devoid of mucosal hemorrhages, mucosal congestion and ulceration compared to that of standard drug Diclofenac. Key words: Diclofenac, 1, 3, 4-oxadiazole, anti-inflammatory, analgesic, ulcerogenicity. Corresponding author: Prof. Shashikant V. Bhandari Department of Pharmaceutical Chemistry, A.I.S.S.M.S College of Pharmacy, Near RTO, Kennedy Road, Pune-411001, Maharashtra, India. Email: drugdesign1@gmail.com drugdesign1@rediffmail.com Phone: - +91 20 26058204; Telefax:- +91 20 26058208