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Structure toxicity relationships of synthetic azaspiracid-1 and analogs in mice

机译:合成azaspiracid-1及其类似物对小鼠的结构毒性关系

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摘要

Synthetic azaspiracid-1 (AZA-1, 1), 6-, 10-, 13-, 14-, 16-, 17-, 19-, 20-epi-azaspiracid-1 (C_1-C_(20)-epi-AZA-1,2), and twelve truncated azaspiracid-1 analogs (3-14) were synthesized and tested for their toxicity effects in mice. Of these compounds only AZA-1 (1) and its diastereomer C_1-C_(20)-epi-AZA-1 (2) exhibited significant toxicity in mice with the latter compound (2) being one-fourth as toxic as the former (1). The lack of toxicity exhibited by the severely truncated analogs (3-14) implies that the entire or at least a major part of the structure of AZA-1 (1) is required for biological activity.
机译:合成azaspiracid-1(AZA-1,1),6-,10-,13-,14-,16-,17-,19-,20-epispirazaspiracid-1(C_1-C_(20)-epi-合成了AZA-1,2)和十二个截短的azaspiracid-1类似物(3-14),并测试了它们在小鼠中的毒性作用。在这些化合物中,只有AZA-1(1)及其非对映异构体C_1-C_(20)-epi-AZA-1(2)在小鼠中表现出显着的毒性,后一种化合物(2)的毒性是前者的四分之一( 1)。严重截短的类似物(3-14)表现出的毒性缺乏表明生物活性需要AZA-1(1)结构的全部或至少主要部分。

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