Schultz T W, Ranney T S
College of Veterinary Medicine, University of Tennessee, Knoxville 37901-1071.
Toxicology. 1988 Dec 16;53(1):147-59. doi: 10.1016/0300-483x(88)90243-0.
A series of 8 alkyl-substituted acid hydrazides were assayed for their toxicity and teratogenicity using early embryos of the frog Xenopus laevis. Each acid hydrazide was able to induce the connective tissue defect osteolathyrism. The 96-h toxicity (log LC50) and 96-h teratogenicity (log EC50) endpoints are correlated with hydrophobicity measured by the fragment substitution constant (Fr). These relationships suggest the rate limiting step is the ability of the chemical to reach the site of action. However, the teratogenic index (LC50/EC50) is negatively correlated with molar refractivity (MR), a substituent corrected molar volume term. This latter relationship suggests steric hindrance.
使用非洲爪蟾的早期胚胎，对一系列8种烷基取代的酰肼进行了毒性和致畸性测定。每种酰肼都能够诱发结缔组织缺陷骨软化病。96小时毒性（log LC50）和96小时致畸性（log EC50）终点与通过片段取代常数（Fr）测量的疏水性相关。这些关系表明限速步骤是化学物质到达作用部位的能力。然而，致畸指数（LC50/EC50）与摩尔折射度（MR）呈负相关，摩尔折射度是一个取代基校正的摩尔体积项。后一种关系表明存在空间位阻。
