Journal of Pharmacobio-Dynamics
Online ISSN : 1881-1353
Print ISSN : 0386-846X
ISSN-L : 0386-846X
STRUCTURE-ACTIVITY RELATIONSHIPS FOR THE INHIBITION OF FORMATION OF ACID-FASTNESS IN MYCOBACTERIAL ORGANISMS BY COUMARINS AND CINNAMATES
YOSHIKAZU KONDOTOMOHIRO TOIDAGENJIRO KUSANOJIRO IMAI
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Keywords: cinnamates
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1980 Volume 3 Issue 1 Pages 41-45

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Abstract
The relationships between the structure and inhibitory activity against the formation of acid-fastness in mycobacterial organisms were investigated in naturally occurring or synthetic coumarins and cinnamates. The presence of an OH-group at C7 in the coumarin nucleus proved to be essential for the inhibitory activity. Likewise, the presence of a para-OH-group in cinnamates is also essential. Reduction of a conjugated α, β-double bond in both series resulted in a decrease of the ininhibitory activity. Shortening of the side chain of cinnamates resulted in total loss of the activity. The grouping 〓〓CO2R appeared to be necessary for retaining the inhibitory activity.
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© The Pharmaceutical Society of Japan
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