The post AMLODIPINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 408.9 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 199-201oC |
4 | Solubility | Slightly soluble in water |
5 | Octanol/water partition coefficient | 3 |
5 | Presence of ring | Dihydropyridine, phenyl |
6 | Number of chiral centers | 1 |
General structure activity of dihydropyridines calcium channel blockers can be summarized as:
i. Ethyl-4-chloroacetoacetate reacts with 3-azidoethanol in presence of sodium hydride to give ethyl-4—(2-azidoethoxy)-acetoacetate.
ii. The last reacts with 2-chlorobenzaldehyde and methyl-3-aminocrotonate to give 3-ethyl-5-methyl-2-[(-azidoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinecarboxylate.
iii. On reduction of the above formed compound, amplodipine is formed. [1]
Amlodipine is used for the treatment of:
Side effects of Amlodipine are:
MCQs
Q.1 “3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate” is the IUPAC nomenclature of which drug?
a) Carvedilol
b) Pentazocine
c) Amlodipine
d) Tropicamide
Q.2 Melting point of drug Amlodipine is?
a) 408.9oC
b) 199-201 oC
c) 345 oC
d) 741 oC
Q.3 Match the following with correct classifications of the drugs.
i. Amplodipine | A. Narcotic antagonist |
ii. Phenacemide | B. Anticonvulsant |
iii. Pentobarbital | C. Sedative-hypnotics |
iv. Nalorphine | D. Calcium channel blocker |
a) i-C, ii-A, iii-D, iv-B
b) i-D, ii-C, iii-A, iv-B
c) i-D, ii-B, iii-C, iv-A
d) i-C, ii-D, iii-B, iv-A
Q.4 Mechanism of action of the drug Amlodipine includes?
I. Amlodipine blocks the entry of calcium ions into vascular smooth muscles and cardiac muscles at the time of depolarization.
II. Amplodipine can bind with dihydropyridine and nondihydropyridine receptor sites present on the cell membrane.
III. There is stronger effect of this drug on vascular smooth muscles than on cardiac muscles which helps in reducing the peripheral vascular esistance, which results in lowering the blood pressure.
a) I, II, III
b) II, III
c) I, III
d) I, II
Q.5 Correct sequence for True and False for the given statements related with the SAR of Thiazide diuretics can be?
a) TFF
b) FFT
c) TTT
d) FFF
Q.6 Number of chiral carbons present in the structure of amlodipine is?
a) 0
b) 1
c) 2
d) 3
Q.7 The drug amlodipine is mainly used for?
a) Chronic stable angina
b) Treatment of hypertesnsion
c) Treatment of vasospastic angina
d) All of the above
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ANSWERS
1-c
2-b
3-c
4-a
5-c
6-b
7-d
REFERENCES
[1] Vardanyan R, Hruby V. Synthesis of essential drugs. Elsevier; 2006 Mar 10.
The post AMLODIPINE 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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