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Synthesis of New 2‐{[(Phenoxy or Phenyl)acetyl]amino}benzoic Acid Derivatives as 3α‐Hydroxysteroid Dehydrogenase Inhibitors and Potential Antiinflammatory Agents
Author(s) -
Daidone Giuseppe,
Plescia Salvatore,
Bajardi Maria Luisa,
Schillaci Domenico
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953281004
Subject(s) - chemistry , anthranilic acid , benzoic acid , stereochemistry , steric effects , yield (engineering) , enzyme , dehydrogenase , in vivo , organic chemistry , materials science , metallurgy , microbiology and biotechnology , biology
A number of 2‐{[(phenoxy or phenyl)acetyl]amino}benzoic acid derivatives were prepared in about 50% yield from (phenoxy or phenyl)acetyl chloride and anthranilic acid derivatives. All the compounds were tested as in vitro inhibitors of 3α‐hydroxysteroid dehydrogenase, since enzyme inhibition predicts potential antiinflammatory activity in vivo The most active compounds 3 1, m, s are about 3.5 times more active than acetylsalicylic acid (ASA). Activity is influenced by electronic as well as steric effects.