Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.

Abstract:

: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-isopropyl-(2-fluorophenyl)-4-(1H)-quinazolinone (50).

journal_name

J Med Chem

authors

Ozaki K,Yamada Y,Oine T,Ishizuka T,Iwasawa Y

doi

10.1021/jm50001a006

subject

Has Abstract

pub_date

1985-05-01 00:00:00

pages

568-76

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

28

pub_type

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