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MEDICINAL CHEMISTRY – I (Theory)



UNIT- I













UNIT- II



1. Drugs acting on Autonomic Nervous System




2. Sympathomimetic agents: SAR of Sympathomimetic agents




3. Adrenergic Antagonists:




UNIT- III



1. Cholinergic neurotransmitters




2. Parasympathomimetic agents: SAR of Parasympathomimetic agents

























3. Cholinergic Blocking agents: SAR of cholinolytic agents


3.1 Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide










4. Synthetic cholinergic blocking agents

NOTE: Search for the drugs in the link provided.




UNIT- IV



1. 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:

Note: Search in the link provided



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












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











UNIT- V




1. 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.










2. 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.





























Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone






Study of the development of the following classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs superscripted (*)


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, 88 Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline.

• Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.

• Agents with mixed mechanism: Ephedrine, Metaraminol.

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.


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.


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


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.



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