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KMID : 0043319990220020184
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Archives of Pharmacal Research
1999 Volume.22 No. 2 p.184 ~ p.188
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Bioisosterism: Interchange of 4-OH to 4-NH2 in Vanillin or Homovanillin Ring of Capsaicinoids
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Cho Sung-Ju
Jung Young-Sik
Seong Churl-Min
Park Woo-Kyu
Kong Jae-Yang
Park No-Sang
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Abstract
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A series of 4-amino Capsaincin anallogs 15, 17 and 19 were prepared to investigate the bioisosteric effect of 4-amino group, and all these compounds exhibited moderate or weak potency from their analgesic test. From our previous results and others, 4-hydroxyl group as well as 3-methoxy substituent could be crucial for high analgesic activity. This biological results also shows that the activity is sensitive to alkyl chain length in hydrophobic region and the phenylacetic amides 19 are more active than the corresponding urea derivatives 17.
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KEYWORD
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Capsaicin, Analgesics, Bioisosteric Effect, Capsaicinoids
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