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6-Chloro-3-(dichloromethyl)-1,1-dioxo-3,4-dihydro-2H-benzo[e] [1,2,4]thiadiazine-7-sulfonamide.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 380.7 g/mol |
2 | Physical appearance | White crystalline powder |
3 | Melting point | 270oC |
4 | Solubility | 1 gm is soluble in 10 ml acetone. |
5 | Octanol/water partition coefficient | 0.62 |
5 | Presence of ring | Benzothiazine |
6 | Number of chiral centers | Not present |
General structure activity of thiazide diuretics can be summarized as:
Reaction of 4-amino-6-chloro-1,3-benzenedisulfonamide with dichloroacetaldehyde diethyl acetal produces trichlormethiazide.
Trichlormethiazide is used for:
Side effects of trichlormethiazide are:
Q.1 What can be the correct IUPAC nomenclature of Trichlormethiazide?
a) 6-fluoro-1,1-dioxo-2H-1,2,4-benzothiadiazine-7-sulfonamide
b) 6-Chloro-3-(dichloromethyl)-1,1-dioxo-3,4-dihydro-2H-benzo[e] [1,2,4]thiadiazine-7-sulfonamide
c) 1-[(4-Chlorophenyl)(phenyl)methyl]-4-methylpiperazine
d) (RS)-3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
Q.2 Which amongst the following statements is/are correct related to the SAR of thiazide diuretics?
I. Substitution on hydrogen at 6 position gives little diuretic activity, whereas, substitution with chloro and trifluoromethyl groups gives highly active compounds.
II. Substitution of electron donating group at position 6 significantly reduces the diuretic activity.
III. Replacement or removal of sulfonamide groups from position 7 significantly reduces the diuretic activity.
a) I, III
b) II, III
c) I, II
d) I, II, III
Q.3 Number of chiral carbons present in the structure of trichlormethiazide is?
a) 1
b) 2
c) 3
d) 0
Q.4 Side effects of drug Trichlormethiazide is/are?
a) Fatigue
b) Loss of appetite
c) Muscle spasms
d) All of the above
Q.5 Match the following drugs with their correct Octanol water partition coefficient-
i. Trichlormethiazide | A. 1.42 |
ii. Methyclothiazide | B. 1.9 |
iii. Omeprazole | C. 0.62 |
iv. Polythiazide | D. 2.23 |
a) i-C, ii-B, iii-A, iv-D
b) i-C, ii-A, iii-D, iv-B
c) i-A, ii-D, iii-C, iv-B
d) i-A, ii-C, iii-B, iv-D
Q.6 An example of drug from class Thiazide diuretics?
a) Trichlormethiazide
b) Amplodipine
c) Hydroxyamphetamine
d) Pseudoephedrine
Q.7 The type of ring system found in the structure of drug Trichlormethiazide is?
a) Dihydroopyridine
b) Benzothiazine
c) Naphthalene
d) Pyrimidine
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ANSWERS
1-b
2-a
3-b
4-d
5-d
6-d
7-b
REFERENCES
[1] Lemke TL, Williams DA, editors. Foye’s principles of medicinal chemistry. Lippincott Williams & Wilkins; 2012 Jan 24. [2] DAS 1 147 233 (Ciba; appl. 4.10.1960; USA-prior. 8.10.1959, 16.10.1959).
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