Diuretic agents related to indapamide. IV--Synthesis and pharmacological activity of N-(4-chloro-3-sulfamoylbenzamido)-methyl-phenyl-pyrrolidines and N1-(4-chloro-3-sulfamoylbenzoyl)-N2-aryl- or aralkyl-alkyl-hydrazines.
A series of N(4-chloro-3-sulfamoylbenzamido) derivatives (6 a-c, 10, 11, 12), structurally related to indapamide and isoindapamide, were synthesized and tested for their diuretic and saluretic activity. In addition, the antihypertensive activity of the most interesting term trans 6a was studied on spontaneously hypertensive rats. All tested compounds with the exception of 10 showed diuretic activity comparable to or higher (trans 6 a) than that of indapamide, taken as reference drug. The antihypertensive activity of trans 6 a was comparable to that of indapamide in potency, but its onset of action was slower.
Istituto di Chimica Farmaceutica dell'Università, Milano, Italy.
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Cignarella
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Barlocco
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Landriani
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Pinna
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Andriuoli
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Donà
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D004232:Diuretics / Q000138:chemical synthesis*; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D007190:Indapamide / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D011188:Potassium / Q000652:urine; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR; D011919:Rats, Inbred Strains; D012964:Sodium / Q000652:urine
D004232:Diuretics; D006834:Hydrazines; D011759:Pyrrolidines; D012964:Sodium; D007190:Indapamide; D011188:Potassium