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1,1-Dioxo-6-(trifluoromethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 331.3 g/mol |
2 | Physical appearance | White to cream colored crystalline powder |
3 | Melting point | 272-273oC |
4 | Solubility | Freely soluble in acetone; soluble in alcohol |
5 | Octanol/water partition coefficient | 0.36 |
5 | Presence of ring | Benzothiazine |
6 | Number of chiral centers | Not present |
General structure activity of thiazide diuretics can be summarized as:
i. Chlorosulfonylation of 3-trifluoromethylamiline using chlorosulfonic acid to get 4-amino-6-(trifluoromethyl)benzene-1,3-disulfonyl dichloride.
ii. The last is reacted with ammonia to get the compound 4-amino-6-trifluoromethylbenzene-1,3disulfamide.
iii. Cyclization of the above formed compound using paraformaldehyde to get hydroflumethiazide drug.
Hydroflumethiazide is used for:
Side effects of hydroflumethiazide are:
Q.1 Match the following with correct SAR of thiazide diuretics-
i. Substitution of electron withdrawing groups at position 6th | A. Increases the diuretic activity |
ii. Removal of sulfonamide group from position 7 | B. Decreased the diuretic activity |
C. Increases the diuretic activity | |
D. Decreases the diuretic activity |
a) i-A, ii-C
b) i-A, ii-D
c) i-B, ii-C
d) i-B, ii-D
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) FFTF
b) FFFF
c) TFFT
d) TTTT
Q.3 Molecular weight of drug hydroflumethiazide is?
a) 475 gm/mol
b) 452.3 gm/mol
c) 331.3 gm/mol
d) 978.1 gm/mol
Q.4 Mechanism of action of hydroflumethiazide includes?
a) Alkylation of genetic material
b) Inhibition of Sodium-Chloride symportor in the DCT
c) Inhibition of hydrogen-potassium pump
d) All of the above
Q.5 Which amongst the following is a therapeutic use of drug hydroflumethiazide?
a) Management of hypertension
b) Treatment of peptic ulcers
c) As an antipsychotic
d) As an anesthetic
Q.6 Which of the following drug and their classification are correct?
I. Hydroflumethiazide: Diuretics
II. Nifedipine: Diuretics
III. Disopyramide: Calcium channel Blocker
IV. Verapamil: α-adrenergic agonist
a) I
b) II, IV
c) I, II, III, IV
d) I, III
Q.7 Type of ring present in the structure of Hydroflumethiazide?
a) Benzothiazine
b) Pyridine
c) Pyrimidine
d) Pyridine
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ANSWERS
1-d
2-b
3-c
4-b
5-a
6-a
7-a
REFERENCES
[1] Lemke TL, Williams DA, editors. Foye’s principles of medicinal chemistry. Lippincott Williams & Wilkins; 2012 Jan 24. [2] Holdrege, C.T. et al.: J. Am. Chem. Soc. (JACSAT) 81, 4807 (1959).
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