TY - JOUR
TI - Synthesis of compounds as melatonin agonists and antagonists
AU - Garratt, P.J.
AU - Tsotinis, A.
JO - Mini Reviews in Medicinal Chemistry
PY - 2007
VL - 7
TODO - 10
SP - 1075-1088
PB - 
SN - 1389-5575
TODO - 10.2174/138955707782110132
TODO - 1,2,3,4 tetrahydrocarbazole derivative;  6,7,8,9 tetrahydro 5h benzene;  anthracene derivative;  benzocycloheptane;  benzodioxane derivative;  benzodithiane derivative;  benzofuran derivative;  benzooxathiane derivative;  benzopyran derivative;  benzothiophene;  benzoxazole derivative;  carbazole derivative;  chroman derivative;  dioxane derivative;  hormone receptor affecting agent;  indan derivative;  indene derivative;  indole derivative;  melatonin;  melatonin 1 receptor;  melatonin 2 receptor;  melatonin agonist;  melatonin antagonist;  melatonin derivative;  naphthalene derivative;  phenanthrene derivative;  tetralin derivative;  unclassified drug, binding affinity;  chirality;  circular dichroism;  cis trans isomerism;  drug activity;  drug conformation;  drug receptor binding;  drug structure;  drug synthesis;  enantiomer;  high performance liquid chromatography;  human;  nonhuman;  pineal body;  racemic mixture;  review;  stereochemistry;  X ray crystallography, Animals;  Drug Design;  Humans;  Indoles;  Melatonin;  Molecular Conformation
TODO - The functions of melatonin, the hormone of the pineal gland, are of considerable current interest. Synthetic melatonin analogues as agonists and antagonists have been explored in some detail and the molecule can be considered as consisting of an indole core, acting mainly as a spacer, and the 5-methoxyl and 3-amidoethyl side chains acting as the functional components, as originally proposed by Heward and Hadley. This review focuses on the synthetic routes to these melatonin analogues, first of the core, then of the substituents that have teen attached to the core, and finally those compounds with restricted conformations and those that are chiral. The importance of the various factors involved in the activity of the compounds as agonist or antagonists is indicated, as is the difference in activity of enantiomers. © 2007 Bentham Science Publishers Ltd.
ER -