TRH mimetics: Differentiation of antiamnesic potency from antidepressant effect

…, TI Korotenko, NI Sokolenko, AI Dyadenko…

Index: Mazurov, Anatoly A.; Andronati, Sergei A.; Korotenko, Tamara I.; Sokolenko, Nikolai I.; Dyadenko, Alexei I.; Shapiro, Yury E.; Gorbatyuk, Vitalii Ya.; Voronina, Tatyana A. Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 11 p. 2029 - 2040

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Citation Number: 7

Abstract

For the purpose of rational modification of the TRH molecule, we were pursuing an approach that consists of two steps:(1)'obligatory'replacement of histidine with glutamine in TRH and (2) the application of conformational constraints for putative bioactive conformation I stabilized by an intramolecular hydrogen bond between C-terminal carboxamide proton and α-carbonyl of histidyl (glutaminyl), and conformation II formed by an intramolecular ...