quinethazone - CAS 73-49-4
Catalog number: 73-49-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C10H12ClN3O3S
Molecular Weight:
289.74
COA:
Inquire
Targets:
Carbonic Anhydrase
Description:
Quinethazone is a thiazide-like diuretic. It is a carbonic anhydrase inhibitor and can be used for the treatment of hypertension.
Purity:
98%
Appearance:
Light Beige Solid
Synonyms:
2-Ethyl-7-chloro-1,2,3,4-tetrahydro-4-oxoquinazoline-6-sulfonamide; 2-Ethyl-7-chloro-2,3-dihydro-4(1H)-quinazolone-6-sulfonamide; Aquamox; CL 36010; Hydromox; Idrokin; Quimethazin; Quinethazon; Quinethazonum; 7-Chloro-2-ethyl-1,2,3,4-tetrahydro-4-oxo-6-quinazolinesulfonamide; 7-Chloro-2-ethyl-1,2,3,4-tetrahydro-4-oxo-6-sulfamoylquinazoline; 7-Chloro-2-ethyl-6-sulfamyl-1,2,3,4-tetrahydro-4-quinazolinone;
Solubility:
DMSO (Slightly), Methanol (Slightly)
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
hypertension
Quality Standard:
usp
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
No Data Available
Melting Point:
>273℃ (dec.)
InChIKey:
AGMMTXLNIQSRCG-UHFFFAOYSA-N
InChI:
InChI=1S/C10H12ClN3O3S/c1-2-9-13-7-4-6(11)8(18(12,16)17)3-5(7)10(15)14-9/h3-4,9,13H,2H2,1H3,(H,14,15)(H2,12,16,17)
Canonical SMILES:
CCC1NC2=CC(=C(C=C2C(=O)N1)S(=O)(=O)N)Cl
Current Developer:
Originator Pfizer
1.Diuretics with carbonic anhydrase inhibitory action: a patent and literature review (2005 - 2013).
Carta F1, Supuran CT. Expert Opin Ther Pat. 2013;23(6):681-91. doi: 10.1517/13543776.2013.780598. Epub 2013 Mar 14.
INTRODUCTION: The benzothiadiazines and high ceiling diuretics (hydrochlorothiazide, hydroflumethiazide, quinethazone, metolazone, chlorthalidone, indapamide, furosemide and bumetanide) contain primary sulfamoyl moieties acting as zinc-binding groups in the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). These drugs are widely used clinically and were recently shown to weakly inhibit isoforms CA I and II, but to possess stronger activity against isoforms involved in other important pathologies, for example, obesity, cancer, epilepsy and hypertension.
2.Liquid chromatographic screening of diuretics in urine.
Fullinfaw RO, Bury RW, Moulds RF. J Chromatogr. 1987 Apr 10;415(2):347-56.
We describe a liquid chromatographic screening procedure for the detection, in urine, of twelve of the fifteen potassium-depleting diuretics available in Australia. A 2-ml urine sample was acidified with NaH2PO4 (pH 4.1) and extracted with 4 ml ethyl acetate. The sample was cleaned up further by washing with 5 ml Na2HPO4 (pH 7.5). The ethyl acetate was then evaporated to dryness, the residue reconstituted in 100 microliters mobile phase and 5 microliter were injected onto a Merck LiChrosorb RP-18 (5 microns) column. The ultraviolet absorbance of the eluent was monitored at 271 nm for 10 min. The screen was evaluated by giving each of thirty volunteers the lowest recommended dose of one of the diuretics in the study and obtaining urine samples 4, 8 and 24 h after having taken the dose. Twelve diuretics, chlorothiazide, hydrochlorothiazide, quinethazone, chlorthalidone, methyclothiazide, clopamide, frusemide, metolazone, mefruside, bendrofluazide, cyclopenthiazide and bumetanide, were all detectable up to 24 h after a dose.
3.Sequential method for combined screening antihypertensive and diuretic agents in the same spontaneously hypertensive rat (SHR).
Chan PS, Poorvin D. Clin Exp Hypertens. 1979;1(6):817-30.
A combined method for detecting compounds with antihypertensive and diuretic activity simultaneously in the same spontaneously hypertensive (SH) rat is described. The present method, utilizing the advantages of sequential probability test analysis, the spontaneously hypertensive rats and the direct measurement of arterial blood pressure, proves to be feasible and efficient in detecting both activities. This ia s 3-stage sequential test requires one to three rats per compound. One adult SH rat was dosed by gavage with compound at 100 mg/kg, p.o. and loaded with 0.9% NaCl at 25 ml/kg, p.o. at 0-hr. The rat was put in a metabolism cage. The 0-5 hr. urine was collected and urinary Na+, K+ and CL- were determined. A second identical dose was given without NaCl loading at 24-hr. Mean arterial blood pressure (MABP) of conscious rats was measured directly by fermoral-iliac artery puncture at 28-hr. The criteria to accept, retest or reject a compound were based on the testing of known antihypertensives and diuretics.
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