Key result
Novel molecules combining sulfonamide diuretic moieties with non-sulfhydryl ACE inhibitors demonstrated ACE inhibitory activity with IC50 values as low as 7 nM and discernable diuretic activity.
Novel dual-action molecules combining ACE inhibition and diuretic properties show promising in vitro potency, suggesting potential for single-molecule combination therapy in hypertension.
Hypothesis-generating for dual ACE inhibitor-diuretic molecules; human trials needed before clinical consideration.
A series of molecules 1 having sulfonamide diuretic moieties covalently linked to non-sulfhydryl angiotensin-converting enzyme inhibitors (ACEI) were prepared and tested for both activities. IC50 values for ACEI as low as 7 nM were observed. Discernable diuretic activity was seen for several hydrochlorothiazide-based molecules. Effects of the ACEI and diuretic structures on the respective potencies are discussed.
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Barton et al. (1990) studied this question. Novel [[N-(1-carboxyl-3-phenylpropyl)amino]acyl]glycine derivatives was evaluated on ACE inhibitory activity (IC50) and diuretic activity. Novel molecules combining sulfonamide diuretic moieties with non-sulfhydryl ACE inhibitors demonstrated ACE inhibitory activity with IC50 values as low as 7 nM and discernable diuretic activity.
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