Diuretic compounds structurally related to furosemide

Scott M. O'Grady, Mark W. Musch, Michael Field

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


This chapter focuses on a group of loop diuretics that are chemically similar to furosemide. More specifically, issues regarding the chemistry, structure-activity relationships, and methods for evaluating the activity of loop diuretics are discussed. The loop diuretics are a group of substituted sulfamyl benzoic acid derivatives that include furosemide, bumetanide, and related compounds. Structure-activity studies using 3-aminobenzoic acid derivatives have focused on substitutions at three positions on the molecule. Diuretic-type drugs can be divided into 3 major categories; (1) carbonic anhydrase inhibitors, (2) thiazide-type diuretics, and (3) loop or high-ceiling diuretics. This chapter also addresses the mechanism of action of these compounds in blocking C1- transport and their use in the molecular characterization of the Na+/K+/2C1 co-transport system which is specifically inhibited by this group of diuretics. The efficacy and order of potency of loop diuretic compounds serve as important criteria in distinguishing the Na+/K+/2CI- cotransport system from other coexisting transport mechanisms present in cell membranes.

Original languageEnglish (US)
Pages (from-to)781-792
Number of pages12
JournalMethods in enzymology
Issue numberC
StatePublished - Jan 1 1990


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