TY - JOUR
T1 - Diuretic compounds structurally related to furosemide
AU - O'Grady, Scott M.
AU - Musch, Mark W.
AU - Field, Michael
PY - 1990/1/1
Y1 - 1990/1/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0025697510&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0025697510&partnerID=8YFLogxK
U2 - 10.1016/0076-6879(90)91047-A
DO - 10.1016/0076-6879(90)91047-A
M3 - Article
C2 - 2074782
AN - SCOPUS:0025697510
SN - 0076-6879
VL - 191
SP - 781
EP - 792
JO - Methods in Enzymology
JF - Methods in Enzymology
IS - C
ER -