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6-chloro-1,1-dioxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 297.7 g/mol |
2 | Physical appearance | White crystalline powder |
3 | Melting point | 274oC |
4 | Solubility | Freely soluble in DMF, NaOH solution; soluble in ethanol; insoluble in ether |
5 | Octanol/water partition coefficient | -0.07 |
5 | Presence of ring | Benzothiazine |
6 | Number of chiral centers | Not present |
General structure activity of thiazide diuretics can be summarized as:
Cyclization of 4,6-sulfonamido-3-chloroaniline by using paraformaldehyde and simultaneous reduction of double bond at C3-C4 to get the drug hydrochlorothiazide.[2]
Hydrochlorothiazide is used for:
Side effects of hydrochlorothiazide are:
Q.1 Which of the following statements are correct related with the physicochemical properties of drug Hydrochlorothiazide?
I. Molecular weight: 297.7 gm/mol
II. Physical appearance: White crystalline powder
III. Melting point: 45 oC
a) I, II, III
b) I, II
c) II, III
d) I, III
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Hydrochlorothiazide | A. 4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine |
ii. Naproxen | B. 6-chloro-1,1-dioxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide |
iii. Hydroxyzene | C. (+)-(S)-2-(6-Methoxynaphthalen-2-yl)propanoic acid
|
iv. Cyproheptidine | D. (±)-2-(2-{4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl}ethoxy)ethanol |
a) i-B, ii-C, iii-D, iv-A
b) i-D, ii-C, iii-B, iv-A
c) i-D, ii-B, iii-A, iv-C
d) i-B, ii-A, iii-D, iv-C
Q.3 Mechanism of action of drug Hydrochlorothiazide includes?
I. Release if NO
II. Inhibition of reabsorption of sodium and chloride
III. Active synthesis of cGMP
IV. Reduction in reabsorption of water
a) I, III, IV
b) II, IV
c)I, II, III
d) I, II, III, IV
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFFT
b) FFTT
c) FFFF
d) TTTF
Q.5 Which of the following statements related with the SAR of thiazide diuretics is/are correct?
a) Hydrogen atom at the 2-N is most acidic due to presence of electron-withdrawing group.
b) Sulfonamide group at C-7 position provides additional acidity to the drug.
c) Electron withdrawing group is essential at position 6 for diuretic activity of the drug.
d) All of the above
Q.6 Type of rings present in the structure of Hydrochlorothiazide?
I. Dihydropyridine
II. Benzothiazine
III. Dihydrofuran
IV. Cyclobutane
a) II, IV
b) I , II
c) III, IV
d) II
Q.7 Side effect of drug Hydrochlorothiazide is/are?
a) Pale skin
b) Nausea
c) Muscle spasm
d) All of the above
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1-b
2-a
3-b
4-c
5-d
6-d
7-d
The post HYDROCHLOROTHIAZIDE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
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