Medicinal Chemistry 1 B.Pharm 5th Semester Books

MEDICINAL CHEMISTRY-1 SEM-V

Author’s Name	Dr. Chandrashekhar Narajji, Mrs. Vibha Chandan Patil
Editions	First Edition
Publishers	Nirali Prakashan

MEDICINAL CHEMISTRY -I (SEM V) B.PHARM

Author’s Name	PRAGI AND VARUN ARORA
Editions	Latest Edition
Publishers	S VIKAS AND COMPANY (PV)

MEDICINAL CHEMISTRY – I, For B. Pharm, 2nd Year, V Semester Students

Author’s Name	Dr. Prashant Kumar Katiyar, Dr. Shriram Bairagi
Editions	First Edition
Publishers	IP Innovative Publication Pvt. Ltd.

Medicinal Chemistry 1 Topic-wise Summary

Introduction to Medicinal Chemistry

1. History and development of medicinal chemistry
   
2. Physicochemical properties in relation to biological action
   
   • Ionization
     
   • Solubility
     
   • Partition coefficient
     
   • Hydrogen bonding
     
   • Protein binding
     
   • Chelation
     
   • Bioisosterism
     
   • Optical and geometrical isomerism
     
3. Drug metabolism
   
   • Principles of drug metabolism
     
     • Phase I
       
     • Phase II
       
   • Factors affecting drug metabolism (including stereochemical aspects)
     

Drugs Acting on Autonomic Nervous System

A. Adrenergic Neurotransmitters

1. Biosynthesis of catecholamines
   
2. Catabolism of catecholamines
   
3. Adrenergic receptors
   
   • Alpha receptors
     
   • Beta receptors
     
   • Distribution of receptors
     

B. Sympathomimetic Agents

1. SAR of Sympathomimetic agents
   
2. Direct acting agents
   
   • Nor-epinephrine
     
   • Epinephrine
     
   • Phenylephrine*
     
   • Dopamine
     
   • Methyldopa
     
   • Clonidine
     
   • Dobutamine
     
   • Isoproterenol
     
   • Terbutaline
     
   • Salbutamol*
     
   • Bitolterol
     
   • Naphazoline
     
   • Oxymetazoline
     
   • Xylometazoline
     
3. Indirect acting agents
   
   • Hydroxyamphetamine
     
   • Pseudoephedrine
     
   • Propylhexedrine
     
4. Agents with mixed mechanism
   
   • Ephedrine
     
   • Metaraminol
     

C. Adrenergic Antagonists

1. Alpha adrenergic blockers
   
   • Tolazoline*
     
   • Phentolamine
     
   • Phenoxybenzamine
     
   • Prazosin
     
   • Dihydroergotamine
     
   • Methysergide
     
2. Beta adrenergic blockers
   
   • SAR of beta blockers
     
   • Propranolol*
     
   • Metibranolol
     
   • Atenolol
     
   • Betaxolol
     
   • Bisoprolol
     
   • Esmolol
     
   • Metoprolol
     
   • Labetolol
     
   • Carvedilol
     

Cholinergic Neurotransmitters

1. Biosynthesis of acetylcholine
   
2. Catabolism of acetylcholine
   
3. Cholinergic receptors
   
   • Muscarinic receptors
     
   • Nicotinic receptors
     
   • Distribution of receptors
     

A. Parasympathomimetic Agents

1. SAR of Parasympathomimetic agents
   
2. Direct acting agents
   
   • Acetylcholine
     
   • Carbachol*
     
   • Bethanechol
     
   • Methacholine
     
   • Pilocarpine
     
3. Indirect acting agents (Cholinesterase inhibitors)
   
   • Reversible: Physostigmine, Neostigmine*, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride
     
   • Irreversible: Isofluorphate, Echothiophate iodide, Parathione, Malathion
     

B. Cholinesterase Reactivator

• Pralidoxime chloride
  

C. Cholinergic Blocking Agents

1. SAR of cholinolytic agents
   
2. Solanaceous alkaloids and analogues
   
   • Atropine sulphate
     
   • Hyoscyamine sulphate
     
   • Scopolamine hydrobromide
     
   • Homatropine hydrobromide
     
   • Ipratropium bromide*
     
3. 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
     

Drugs Acting on Central Nervous System

A. Sedatives and Hypnotics

1. Benzodiazepines (SAR of Benzodiazepines)
   
   • Chlordiazepoxide
     
   • Diazepam*
     
   • Oxazepam
     
   • Chlorazepate
     
   • Lorazepam
     
   • Alprazolam
     
   • Zolpidem
     
2. Barbiturates (SAR of Barbiturates)
   
   • Barbital*
     
   • Phenobarbital
     
   • Mephobarbital
     
   • Amobarbital
     
   • Butabarbital
     
   • Pentobarbital
     
   • Secobarbital
     
3. Miscellaneous
   
   • Amides & imides: Glutethimide
     
   • Alcohol & carbamate derivatives: Meprobamate, Ethchlorvynol
     
   • Aldehyde & derivatives: Triclofos sodium, Paraldehyde
     

B. Antipsychotics

1. Phenothiazines (SAR of Phenothiazines)
   
   • Promazine hydrochloride
     
   • Chlorpromazine hydrochloride*
     
   • Triflupromazine
     
   • Thioridazine hydrochloride
     
   • Piperacetazine hydrochloride
     
   • Prochlorperazine maleate
     
   • Trifluoperazine hydrochloride
     
2. Ring analogues of Phenothiazines
   
   • Chlorprothixene
     
   • Thiothixene
     
   • Loxapine succinate
     
   • Clozapine
     
3. Fluorobutyrophenones
   
   • Haloperidol
     
   • Droperidol
     
   • Risperidone
     
4. Beta amino ketones
   
   • Molindone hydrochloride
     
5. Benzamides
   
   • Sulpiride
     

C. Anticonvulsants

1. SAR of Anticonvulsants
   
2. Mechanism of anticonvulsant action
   
3. Barbiturates
   
   • Phenobarbitone
     
   • Metharbital
     
4. Hydantoins
   
   • Phenytoin*
     
   • Mephenytoin
     
   • Ethotoin
     
5. Oxazolidinediones
   
   • Trimethadione
     
   • Paramethadione
     
6. Succinimides
   
   • Phensuximide
     
   • Methsuximide
     
   • Ethosuximide*
     
7. Ureas and monoacylureas
   
   • Phenacemide
     
   • Carbamazepine*
     
8. Benzodiazepines
   
   • Clonazepam
     
9. Miscellaneous
   
   • Primidone
     
   • Valproic acid
     
   • Gabapentin
     
   • Felbamate
     

Drugs Acting on Central Nervous System

A. General Anesthetics

1. Inhalation anesthetics
   
   • Halothane*
     
   • Methoxyflurane
     
   • Enflurane
     
   • Sevoflurane
     
   • Isoflurane
     
   • Desflurane
     
2. Ultra short-acting barbiturates
   
   • Methohexital sodium*
     
   • Thiamylal sodium
     
   • Thiopental sodium
     
3. Dissociative anesthetics
   
   • Ketamine hydrochloride*
     

B. Narcotic and Non-Narcotic Analgesics

1. Morphine and related drugs (SAR of Morphine analogues)
   
   • Morphine sulphate
     
   • Codeine
     
   • Meperidine hydrochloride
     
   • Anileridine hydrochloride
     
   • Diphenoxylate hydrochloride
     
   • Loperamide hydrochloride
     
   • Fentanyl citrate*
     
   • Methadone hydrochloride*
     
   • Propoxyphene hydrochloride
     
   • Pentazocine
     
   • Levorphanol tartrate
     
2. Narcotic antagonists
   
   • Nalorphine hydrochloride
     
   • Levallorphan tartrate
     
   • Naloxone hydrochloride
     

C. Anti-inflammatory Agents

• Sodium salicylate
  
• Aspirin
  
• Mefenamic acid*
  
• Meclofenamate
  
• Indomethacin
  
• Sulindac
  
• Tolmetin
  
• Zomepirac
  
• Diclofenac
  
• Ketorolac
  
• Ibuprofen*
  
• Naproxen
  
• Piroxicam
  
• Phenacetin
  
• Acetaminophen
  
• Antipyrine
  
• Phenylbutazone