Journal of Medicinal Chemistry p. 568 - 576 (1985)
Update date:2022-08-03
Topics:
Ozaki
Yamada
Oine
Ishizuka
Iwasawa
A number of new 4(1H)-quinazolinones were synthesized and evaluated in the carrageenin-induced paw edema test. Most of the compounds were obtained by the cyclization of the appropriately substituted anthranilamides with acid chlorides, followed by further chemical transformation. Structure-activity data suggest that 2-isopropyl-1-phenyl-, 2-cyclopropyl-1-phenyl-, and 1-isopropyl-2-phenyl-4(1H)-quinazolinones afford optimal potency and the presence of a halogen atom is preferred for activity. Adrenalectomy does not affect the antiinflammatory test results. The best result taking into account both efficacy and side effects was displayed by 1-isoproyl-(2-fluorophenyl)-4(1H)-quinazolinone.
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