Synthesis and biological evaluation of new heteroaryl carboxylic acid derivatives as anti-inflammatory-analgesic agents.
A series of nicotinic acid derivatives structurally related to niflumic acid and certain pyridazine-containing compounds have been synthesized and characterized by analytical and spectral data. All compounds were screened for their potential analgesic and anti-inflammatory activities. The compounds which displayed analgesic and anti-inflammatory activities were tested for ulcerogenicity and screened for in vivo inhibition of certain inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and cyclooxygenase-2 (COX-2). Compounds 1c, 2a, 2b, and 5a have shown potent analgesic and anti-inflammatory activities.
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt.
Khaled Abouzid Mohamed
KA
Abouzid
Nadia Abdalla
NA
Khalil
Eman Mohamed
EM
Ahmed
Sawsan Abo-Bakr
SA
Zaitone
D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D051546:Cyclooxygenase 2 / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D015850:Interleukin-6 / Q000378:metabolism; D051379:Mice; D009539:Nicotinic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D009544:Niflumic Acid / Q000737:chemistry; D011724:Pyridazines / Q000737:chemistry; D051381:Rats; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism; D014456:Ulcer / Q000188:drug therapy
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D015850:Interleukin-6; D009539:Nicotinic Acids; D011724:Pyridazines; D014409:Tumor Necrosis Factor-alpha; C062482:pyridazine; D009544:Niflumic Acid; D051546:Cyclooxygenase 2