1. Academic Validation
  2. Acetoxybenzhydrols as highly active and stable analogues of 1'S-1'-acetoxychavicol, a potent antiallergic principal from Alpinia galanga

Acetoxybenzhydrols as highly active and stable analogues of 1'S-1'-acetoxychavicol, a potent antiallergic principal from Alpinia galanga

  • Bioorg Med Chem Lett. 2009 Jun 1;19(11):2944-6. doi: 10.1016/j.bmcl.2009.04.065.
Tomohisa Yasuhara 1 Yoshiaki Manse Takayuki Morimoto Wang Qilong Hisashi Matsuda Masayuki Yoshikawa Osamu Muraoka
Affiliations

Affiliation

  • 1 School of Pharmacy, Kinki University, Higashiosaka, Osaka, Japan.
Abstract

Through SAR studies on 1'S-1'-acetoxychavicol acetate (1) against Type I antiallergic activity by indexing release of beta-hexosaminidase, a marker of antigen-IgE-mediated degranulation in RBL-2H3 cells, more stable and potent analogue, 4-(methoxycarbonyloxyphenylmethyl)phenyl acetate (16), has been developed. The compound 16 also strongly inhibited the antigen-IgE-mediated TNF-alpha and IL-4 production.

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