A study of anti-inflammatory activity of some novel alpha-amino naphthalene and beta-amino naphthalene derivatives.
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.
Sharma
Shalabh
S
Medicinal Chemistry Division, Department of Pharmacology, Lala Lajpat Rai Memorial Medical College, Meerut, India. drshalabhsharma@gmail.com
Singh
Tripti
T
Mittal
Rajan
R
Saxena
K K
KK
Srivastava
Virendra Kishore
VK
Kumar
Ashok
A
D000700:Analgesics / Q000138:chemical synthesis* / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000633:toxicity; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000633:toxicity; D010147:Pain Measurement; D010437:Peptic Ulcer / Q000139:chemically induced; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D009281:Naphthalenes; D011451:Prostaglandin-Endoperoxide Synthases