Synthesis and Pharmacological Evaluation of N,N-di-n-Propyldopamine Congeners Containing Phenolic Bioisosteres
作者： Robin D. Clark , Joan M. Caroon , Nancy E. Isaac , Deborah L. McClelland , Anton D. Michel
关键词: Rat model 、 Selectivity 、 Stereochemistry 、 Chemistry 、 In vivo 、 Dopamine receptor D2 、 Stereospecificity 、 Derivative (chemistry) 、 Agonist 、 Pharmaceutical Science
摘要: A series of analogues N,N-di-n-propyldopamine (DPDA) in which the 3-hydroxyl group was replaced by bioisosteric groups prepared and evaluated for D1- D2-receptor affinity. The 3-methanesulfonamide analogue (18) had a higher affinity D2 receptor than DPDA more selective receptor. 3-formamide derivative (15) also retained significant Both these compounds demonstrated vivo cardiovascular renal profiles an anesthetized rat model that were consistent with agonism.
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