ChemInform Abstract: Conformationally Restricted TRH Analogues: Constraining the Pyroglutamate Region.
Abstract
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ChemInform Abstract
Adding constraints to the pyroglutamate region of TRH leads to a significantly improved method for varying the nature of the constraint. This approach gives rise to the synthesis of analogues bearing an ethylene (XI), an ethane (XII), and a propane bridge in this region. However, altering the original bridge in the pyroglutamate region affords no improvement in the affinity or potency of the analogue for TRH-R.
