In the present study, some naphthalene derivatives have been synthesized by incorporating azetidinyl and thiazolidinyl moieties at its alpha- or beta-positions such as alpha-(3-chloro-2-oxo-4-substituted)aryl-1-azetidinyl)naphthalenes 6-10, alpha-((substituted)aryl-4-oxo-1,3-thiazolidin-3-yl)naphthalenes 11-15, beta-(3-chloro-2-oxo-4-substituted aryl-1-azetidinyl)naphthalenes 21-25, and beta-(substituted aryl-4-oxo-1,3-thiazolidin-3-yl)naphthalenes 26-30. These compounds have also been screened for acute toxicity and anti-inflammatory and analgesic activities. Compounds which showed better anti-inflammatory and analgesic activities were also examined for their ulcerogenic liability and underwent a cyclooxygenase assay. Two compounds, 12 and 28, were found to exhibit potent anti-inflammatory activity as compared to the standard drugs phenylbutazone and naproxen.
A Study of Antiinflammatory Activity of Some Novel α-Amino Naphthalene and β-Amino Naphthalene Derivatives. -A series of naphthalene derivatives bearing azetidinyl-or thiazolidinyl moieties at their αor β-positions is synthesized and evaluated for acute toxicity, antiinflammatory and analgesic activities. Compounds (VIIb), (VIIc) and (VIIIb) are found to possess more potent antiinflammatory activity compared to the standard phenylbutazone. Compound (VIIc) exhibits even better effects than naproxen. In general, the β-substituted naphthalene derivatives possess better biological properties than their α-naphthalene congeners. -(SHARMA*, S.; SINGH, T.; MITTAL, R.; SAXENA, K. K.; SRIVASTAVA, V. K.; KUMAR, A.; Arch. Pharm. (Weinheim, Ger.) 339 (2006) 3, 145-152; Dep. Pharmacol., Lala Lajpat Rai Mem. Med. Coll., Meerut 250 004, India; Eng.) -M. Kowall 28-127
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