Endocrinology · 1951 · 15 citations · 0 references
Life SciencesBiochemistryPharmacologyBioisosterismMetabolismStructure-activity RelationshipsAmino Acid MetabolismStructure-activity Relationship AnalysisStructure-metabolism RelationshipsThyroid Hormone BiochemistryAmino Acid Side Chain ChemistryThyroid Hormone AnaloguesThyroid Hormone Metabolites
IN THE literature of the study of the portions of the thyroxine molecule structure which are required for physiological activity, three general points of attack are prominent: (1) the specific type as well as number of atoms of halogen, (2) the diphenyl ether skeleton, (3) the alanine sidechain. The work has recently been summarized by Frieden and Winzler (1948), who concluded that thyroxine-like activity was dependent upon the following combination of features: with R a wide variety of active groups. Because of the recent report by Harington (1948) concerning activity shown by the thio-ether analogue, this modification should also be included. It is the purpose of this paper to report work bearing principally upon the number and type of halogens and influence of the R side-chain. The animals used were young adult male albino rats of the Sprague-Dawley strain, 300–350 grams in weight.