Aryl esters (aryl=
m-tolyl,
o-methoxyphenyl, 4-isopropyl-3-methylphenyl, and 2-isopropyl-5-methylphenyl) of
p-aminosalicylic acid (PAS) and 4-amino-2-chlorobenzoic acid (
o-Cl-PABA), and their
p-succinamido compounds,
p-maleylamidosalicylic acid, and
p-phthalylamidosalicylic acid were prepared and their
in vitro tests were carried out with tubercle bacilli, using Dubos medium and strains E
5, H
37Rv, and H
37Rv-R-PAS. The aryl ester of
o-Cl-PABA had antibacterial activity against the H
37Rv-R-PAS strain, differing from PAS compounds, but its
p-succinamido compounds, with the exception of
p-isopropyl-
m-cresyl and thymyl esters, had almost no such antibacterial activity.
p-Maleylamidosalicylic and
p-phthalylamidosalicylic acids showed comparatively good antibacterial activity.
p-Succinamido compounds, whose
in vitro antibacterial power was weaker than that of sodium-PAS and which was expected to increase the antibacterial power by inhibiting the TCA-cycle of tubercle bacilli, did not show any better antibacterial activity than the free amino compounds.
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