Medicinal Chemistry-I: Question /answer Session

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Question /Answer Session

Medicinal Chemistry-I
S. Y. B. Pharm. Sem IV (2020-21)

K. K. Wagh Education Society’s

K. K. Wagh College of Pharmacy


(Affiliated to Dr. Babasaheb Ambedkar Technological University)
07/29/2021 Prof. M. G. Shinde & Prof. S. D.Malode 1
Disclaimer
1. Attendance for this Q.A. Session is 100% Compulsory.

2. Separate Note book should be prepared and all Q.A to be noted down
carefully.

3. These are very carefully selected & prepared Q & A by your teachers

4. So, prepare and recite them without fail

5. Strict Disciplinary Action shall be taken against those who not abide by
above points as well as remain absent, including calling parents 2

07/29/2021
Syllabus for MC-I theory
Unit I
Introduction to Medicinal Chemistry
History and development of medicinal chemistry,
Physicochemical properties in relation to biological action- Ionization, Solubility, Partition
Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and
Geometrical isomerism.
Drug metabolism Drug metabolism principles- Phase I and Phase II. Factors affecting drug
metabolism including stereo chemical aspects
Unit II
• Drugs acting on Autonomic Nervous System
Adrenergic Neurotransmitters: Biosynthesis and catabolism of catecholamine. Adrenergic receptors
(Alpha & Beta) and their distribution.
Sympathomimetic agents: SAR of Sympathomimetic agents
 Direct acting: Nor-epinephrine, Epinephrine, Phenylephrine*, Dopamine, 89 Methyldopa,
Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazoline,
Oxymetazoline and Xylometazoline.
 Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.
 Agents with mixed mechanism: Ephedrine, Metaraminol. .
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Prof M.G.Shinde
Syllabus for MC-I theory
Unit II
Adrenergic Antagonists:
Alpha adrenergic blockers: Tolazoline*, Phentolamine, Phenoxybenzamine, Prazosin,
Dihydroergotamine, Methysergide.
Beta adrenergic blockers: SAR of beta blockers, Propranolol*, Metibranolol, Atenolol,
Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetolol, Carvedilol.

Unit III
Cholinergic neurotransmitters: Biosynthesis and catabolism of acetylcholine. Cholinergic
receptors (Muscarinic & Nicotinic) and their distribution.
Parasympathomimetic agents: SAR of Parasympathomimetic agents
Direct acting agents: Acetylcholine, Carbachol*, Bethanechol, Methacholine, Pilocarpine.
Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible): Physostigmine,
Neostigmine*, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium
chloride, Isofluorphate, Echothiophate iodide, Parathione, Malathion. Cholinesterase
reactivator: Pralidoxime chloride.

07/29/2021 Prof M.G.Shinde/ Prof. S.D.Malode 4


Syllabus for MC-I theory
Unit III
Cholinergic Blocking agents: SAR of cholinolytic agents
Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine
hydrobromide, Homatropine hydrobromide, Ipratropium bromide*.
Synthetic cholinergic blocking agents: Tropicamide, Cyclopentolate hydrochloride, Clidinium
bromide, Dicyclomine hydrochloride*, Glycopyrrolate, Methantheline bromide, Propantheline
bromide, Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride, Procyclidine
hydrochloride*, Tridihexethyl chloride, Isopropamide iodide, Ethopropazine hydrochloride.
Unit IV
Drugs acting on Central Nervous System
A. Sedatives and Hypnotics:
Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide, Diazepam*, Oxazepam,
Chlorazepate, Lorazepam, Alprazolam, Zolpidem
Barbiturtes: SAR of barbiturates, Barbital*, Phenobarbital, Mephobarbital, Amobarbital,
Butabarbital, Pentobarbital, Secobarbital
Miscelleneous: Amides & imides: Glutethmide. Alcohol & their carbamate derivatives:
Meprobomate, Ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.
07/29/2021 5
Prof M.G.Shinde
Syllabus for MC-I theory
Unit IV
Drugs acting on Central Nervous System
B. Antipsychotics
 Phenothiazeines: SAR of Phenothiazeines - Promazine hydrochloride, Chlorpromazine
hydrochloride*, Triflupromazine, Thioridazine hydrochloride, Piperacetazine hydrochloride,
Prochlorperazine maleate, Trifluoperazine hydrochloride.
 Ring Analogues of Phenothiazeines: Chlorprothixene, Thiothixene, Loxapine succinate, Clozapine.
 Fluro buterophenones: Haloperidol, Droperidol, Risperidone.
 Beta amino ketones: Molindone hydrochloride.
 Benzamides: Sulpieride.
C. Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant action
 Barbiturates: Phenobarbitone, Methabarbital.
 Hydantoins: Phenytoin*, Mephenytoin, Ethotoin
 Oxazolidine diones: Trimethadione, Paramethadione
 Succinimides: Phensuximide, Methsuximide, Ethosuximide*
 Urea and monoacylureas: Phenacemide, Carbamazepine*
 Benzodiazepines: Clonazepam
 Miscellaneous: Primidone, Valproic acid , Gabapentin, Felbamate
07/29/2021 6
Prof M.G.Shinde
Syllabus for MC-I theory
Unit V
Drugs acting on Central Nervous System
General anesthetics:
Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane,
Desflurane. Ultra short acting barbitutrates: Methohexital sodium*, Thiamylal sodium, Thiopental
sodium. Dissociative anesthetics: Ketamine hydrochloride.*
Narcotic and non-narcotic analgesics
Morphine and related drugs: SAR of Morphine analogues, Morphine sulphate, Codeine,
Meperidine hydrochloride, Anilerdine hydrochloride, Diphenoxylate hydrochloride, Loperamide
hydrochloride, Fentanyl citrate*, Methadone hydrochloride*, Propoxyphene hydrochloride,
Pentazocine, Levorphanol tartarate.
Narcotic antagonists: Nalorphine hydrochloride, Levallorphan tartarate, Naloxone hydrochloride.
Anti-inflammatory agents:
Sodium salicylate, Aspirin, Mefenamic acid*, Meclofenamate, Indomethacin,
Sulindac, Tolmetin, Zomepriac, Diclofenac, Ketorolac, Ibuprofen*, Naproxen, Piroxicam,
Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone

07/29/2021 7
Prof M.G.Shinde
Question Paper Pattern
Q I. Multiple Choice Questions (MCQs) = 20 x 1 = 20
(Answer all the questions)
OR
Q I. Objective Type Questions (10 x 2) = 10 x 2 = 20
(Answer all the questions)
Q 2. Long Answers (Answer 2out of 3) = 2x 10 = 20
Q 3. Short Answers (Answer 7 out of 9) = 2 x 5 = 10
Total = 70 marks

07/29/2021 Prof M.G.Shinde/ Prof. S.D.Malode 8


MULTIPLE CHOICE QUESTIONS
(M.C.Qs)

Some questions have more than one correct answer.


Select the best answer or answers from the choices given.

Marks 01 Each
07/29/2021 Prof M.G.Shinde/ Prof. S.D.Malode 9
Q.No.1 M.C.Q. 1 mark each
1*. Bioisoterism is the process of :
(a) Replacement of similar group (b) Replacement of Similar mass (c) Replacement of similar
valence group (d) Addition of different mass number group
Correct : (c) Replacement of similar valence group

2*. Dimercaprol is Chelating agent and used in treatment of...


a)Arsenic Poisoning b)Iron Poisoning c) Lead Poisoning d) Vanadium Poisoning
Correct : a)Arsenic Poisoning

3*. Phase –I Reactions are also called as ………


a) Biotransformation
b) Functionalization reaction
c) Conjugation Reaction
d) Reduction Reaction
Correct : b) Functionalization reaction
07/29/2021 Dr. R.D.Amrutkar / Prof M.G.Shinde
M.C.Q 10
4. Azo and nitro groups are metabolized by….. Recation
a) Acetylation b) Oxidation c) Hydrolysis d) Reduction
Correct : d) Reduction

5*. Which of the following metabolic reaction forms unstable hemiacetal or hemiketal intermediate
a) N-hydroxylation b) o-dealkylation C) N-oxidation d) Reduction
Correct : C) N-oxidation

6. Which of the following is factor affecting drug metabolism


a) Environmental Factor
b) Genetic factor
c) Chemical factor
d) All of these
Correct : d) All of these

07/29/2021 Dr. R.D.Amrutkar / Prof M.G.Shinde


M.C.Q 11
• 7. A _____ is a drug that is intended to induce sleep by depressing the central nervous
system.
a)Antipsychotics
b)Sedatives
c)None of the above
d) Hypnotics

Correct : d. Hypnotics

8 Which of the following is tricyclic antipsychotic having propyl dialkylamino side chain?
a. Trifluoropramozine
b. Haloperidol
c. Sulpiride
d. Thiothixene
Correct Answer: Trifluoropramozine

07/29/2021 Dr. R.D.Amrutkar / Prof M.G.Shinde


M.C.Q 12
9. Anxiolytics are also called as ..

a. Antipanic
b. Hypnotics
c. Sedatives
d. All of the above
Ans: a Antipanic
10. When malonic acid esters are condensed with ………..it give barbiturates

a. Urea or Thiourea

b. Alcohols

c. Ethers

d. Esters

Ans: a. Urea or Thiourea


11. Zolpidem contains which heterocyclic ring system….

a. Imidazo [1,2-b] Pyridine

b. Imidazo [2,3-b] Pyridine

c. Imidazo [1,2-b] Pyrimidine

d. Imidazo [1,2-b] Pyrazole

Ans: a. Imidazo [1,2-b] Pyridine


12. Nitrazepam contains which heterocyclic ring system

a. 1,5-benzodiazepam

b. 1,3-benzodiazepam

c. 1,2-benzodiazepam

d. 1,4-benzodiazepam

Ans: d. 1,4-benzodiazepam
13. Which of the following drug not comes under sedative and hypnotics Class?

a. Chloral Hydrate

b. Paraldehyde

c. Glutetheamide

d. None of the above

Ans: d. None of the above


14. Replacement of C=O with C=S in barbiturate structure gives ?

a. Long on set of action


b. Longer duration of action
c. Short duration of action
d. Abolish the activity
Ans: Short duration of action
15. Unsubstituted 5th position barbituric acid is ?
a. Short acting
b. Long acting
c. Not active
d. Long active
Ans: Not active
16. Saturation of double bond at 4,5 position of benzodiazepine will..?

a. Increases the activity

b. Reduces the activity

c. Abolishes the activity

d. Not affect the activity of parent molecule

Ans: Reduces the activity


Thank you

07/29/2021 Prof.S.D.Malode 21

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