Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors.
Various 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2'-substitutedindol-3'-yl)-halosubstituted-4(3H)quinazolinones (5a-5i) and 2-(substituted phenylaminomethyleneacetyl-4'-oxo-1'-thiazolidinyl-3-(2"-substitutedindol-3"-yl) 4(3H)-quinazolinones (6a-6i) have been synthesized in the present studies. The structure of these compounds have been elucidated by elemental (C, H, N) and spectral (IR, 1H NMR and mass) analysis. Furthermore, above said compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic activities and acute toxicity study. Compound 6d was found to be most potent. Compound exihibiting less ulcerogenic liability and ALD(50) >2000mg/kg po.
Kumar
Ashok
A
Medicinal Chemistry Division, Department of Pharmacology, L.L.R.M Medical College, (U.P.)-250004, Meerut, India. rajput_ak@indiatimes.com
Sharma
Shalabh
S
Archana
Bajaj
Kiran
K
Sharma
Shipra
S
Panwar
Hemant
H
Singh
Tripti
T
Srivastava
V K
VK
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007527:Isoenzymes / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects*; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013057:Spectrum Analysis
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D011799:Quinazolines; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases