Koechel D A, Rankin G O
J Med Chem. 1978 Aug;21(8):764-9. doi: 10.1021/jm00206a009.
Various Mannich base derivatives of selected phenoxyacetic acid type diuretics were synthesized and their diuretic potency was evaluated in dogs. It is concluded that the Mannich bases possess little, if any, diuretic activity of their own. Those Mannich bases that do possess diuretic activity undoubtedly do so as a consequence of an elimination reaction (a retro-Michael type reaction) which yields the corresponding pharmacologically active alpha,beta-unsaturated ketone.
合成了多种选定苯氧乙酸类利尿剂的曼尼希碱衍生物,并在犬类中评估了它们的利尿效力。得出的结论是,曼尼希碱自身几乎不具有利尿活性(如果有的话)。那些确实具有利尿活性的曼尼希碱无疑是由于消除反应(逆迈克尔型反应)产生了相应的具有药理活性的α,β-不饱和酮。