PHARMACEUTICAL MEDICINAL CHEMISTRY- Dealing with the structure- Part- II
In the previous post we covered some basic funda's regarding chemistry. Now with the basics done its time to move ahead and master the subject of interest- "Pharmaceutical Medicinal Chemistry". This subject basically will deal with the SAR- Structure Activity Relationship, MOA- Mechanism of Action and chemical synthesis of pharmaceutical agents or simply 'drugs'.
In SAR, we should try to focus on the functional groups in a particular moiety which are responsible for the action of the drug/ binding with the receptors. It can also include the 'prodrug' approach as well. E.g. Which functional group is susceptible for the making prodrug.
In MOA, it is sometimes essential to know the sequence of reactions which actually take place with the drug (especially prodrug) in the body on administration. MOA is more of concern in 'pharmacology' which we would cover in the upcoming posts. Rather, I would personally suggest to study pharmacology and medicinal chemistry at the same time. It will serve 2 purposes-
1. Time-saving activity.
2. After knowing structure, SAR and chemical synthesis of particular class of drugs in chemistry (for e.g. anti-viral agents), you can look its MOA, ADR (Adverse Drug Reactions), S/E (Side-effects) and other aspects in pharmacology. Thus, you will immediately link the chemistry and pharmacological actions of the drug instantly and trust me, it really helps a lot.. Its like hitting 2 bird with a single stone !!
In this post we will also try to cover 'Biochemistry'. Most of the questions regarding with biochemistry is more centered around the biochemical pathways. Glycolysis, TCA cycle are favourite ones. Questions may or may not be asked on enzyme kinetics, enzyme immobilization, nucleic acids- DNA, RNA etc., genetic mutations etc. These topics are more of a concern in NIPER-JEE preparation. We would also cover guidance and tips about NIPER-JEE too once GPAT series ends.
Recommended books for reading-
PHARMACEUTICAL MEDICINAL CHEMISTRY
1. Thomas L. Lemke, David A. Williams, Victoria F. Roche, S. William Zito, "Foye's Principles of Medicinal Chemistry", 7th Edition, Lippincott Williams and Wilkins Publishers, 2013.
2. John M. Beale Jr., John H. Block, "Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry", 12th Edition, South Asian Edition, Lippincott Williams and Wilkins Publishers, 2010.
The above books were for referring SAR, MOA, uses etc. stuff of drugs. Now for synthesis of drugs we would recommend to refer-
3. Daniel Lednicer, "The Organic Chemistry of Drug Synthesis", Wiley, Volumes- 1 to 7.
4. Douglas S. Johnson and Jie Jack Li, "The Art of Drug Synthesis".Wiley Interscience, 2007.
PHARMACEUTICAL MEDICINAL CHEMISTRY
Basic Principles- 1
Drug metabolism and Concept of Prodrugs; Principles of Drug Design (Theoretical Aspects)- 1
Synthetic Procedures, Mode of Action, Uses, Structure Activity Relationships including Physicochemical Properties of the Following Classes of Drugs:
a. Drugs acting at synaptic and neuro-effector junction sites: Cholinergics, anti-cholinergics and cholinesterase inhibitors, Adrenergic drugs, Antispasmodic and anti-ulcer drugs, Local Anesthetics, Neuromuscular blocking agents- 1,2
b, Autacoids- 1,2
c. Steroidal Drugs- 2
d. Drugs acting on the central nervous system- 1,2
e. Diuretics; Cardiovascular drugs- 1,2
f. Thyroid and Anti thyroid drugs; Insulin and oral hypoglycemic agents- 1
g. Chemotherapeutic Agents used in bacterial, fungal, viral, protozoal, parasitic and other infections, Antibiotics: ß-Lactam, macrolides, tetracyclines, aminoglycosides, polypeptide
antibiotics, fluoroquinolones- 1,2
h. Anti-metabolites (including sulfonamides); Anti-neoplastic agents; Anti-viral agents (including anti–HIV);
Immunosuppressives and immunostimulants; Diagnostic agents; Pharmaceutical Aids- 1,2
BIOCHEMISTRY-
1. David L. Nelson and Michael M. Fox, "Lehninger Principles of Biochemistry", 6th Edition, Macmillan Publishers, 2013,
2. Robert K. Murray, Peter J. Kenelly, David A. Bender, Kethleen M. Bothan, P. Anthony Weil, Victor W. Rodwell, "Harpers Illustrated Biochemistry", 29th Edition, Tata Mc-Graw Hill Publishers, 2012.
BIOCHEMISTRY-
Biochemistry in pharmaceutical sciences- 1,2
Enzymes- 1,2
Co-enzymes- 1,2
Carbohydrate Metabolism- 1,2
The Citric Acid Cycle- 1,2
Lipids Metabolism- 1,2
Essential fatty acids & eicosanoids- Refer Foye and Wilson of Medicinal Chemistry.
Biological Oxidation- 1,2
Metabolism of ammonia and nitrogen containing monomers- 1,2
Purine biosynthesis- 1,2
Pyrimidine biosynthesis and formation of deoxyribounucleotides.
Biosynthesis of Nucleic Acids- 1,2
Mutation- 2
Genetic Code and Protein Synthesis- 1,2
Enzyme Immobilization- 1,2.
This was all about 'MEDICINAL CHEMISTRY' and 'BIOCHEMISTRY'. In the next part we would cover all of 'PHARMACEUTICAL ANALYSIS'.
Hope you would have liked this part, too.. Any kind of feedback and suggestions are welcome by our team !!!
-Darwin
[GPAT-2014- All India Rank (AIR)- 619)
NIPER-JEE-2014 AIR-25 and
In the previous post we covered some basic funda's regarding chemistry. Now with the basics done its time to move ahead and master the subject of interest- "Pharmaceutical Medicinal Chemistry". This subject basically will deal with the SAR- Structure Activity Relationship, MOA- Mechanism of Action and chemical synthesis of pharmaceutical agents or simply 'drugs'.
In SAR, we should try to focus on the functional groups in a particular moiety which are responsible for the action of the drug/ binding with the receptors. It can also include the 'prodrug' approach as well. E.g. Which functional group is susceptible for the making prodrug.
In MOA, it is sometimes essential to know the sequence of reactions which actually take place with the drug (especially prodrug) in the body on administration. MOA is more of concern in 'pharmacology' which we would cover in the upcoming posts. Rather, I would personally suggest to study pharmacology and medicinal chemistry at the same time. It will serve 2 purposes-
1. Time-saving activity.
2. After knowing structure, SAR and chemical synthesis of particular class of drugs in chemistry (for e.g. anti-viral agents), you can look its MOA, ADR (Adverse Drug Reactions), S/E (Side-effects) and other aspects in pharmacology. Thus, you will immediately link the chemistry and pharmacological actions of the drug instantly and trust me, it really helps a lot.. Its like hitting 2 bird with a single stone !!
In this post we will also try to cover 'Biochemistry'. Most of the questions regarding with biochemistry is more centered around the biochemical pathways. Glycolysis, TCA cycle are favourite ones. Questions may or may not be asked on enzyme kinetics, enzyme immobilization, nucleic acids- DNA, RNA etc., genetic mutations etc. These topics are more of a concern in NIPER-JEE preparation. We would also cover guidance and tips about NIPER-JEE too once GPAT series ends.
Recommended books for reading-
PHARMACEUTICAL MEDICINAL CHEMISTRY
1. Thomas L. Lemke, David A. Williams, Victoria F. Roche, S. William Zito, "Foye's Principles of Medicinal Chemistry", 7th Edition, Lippincott Williams and Wilkins Publishers, 2013.
2. John M. Beale Jr., John H. Block, "Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry", 12th Edition, South Asian Edition, Lippincott Williams and Wilkins Publishers, 2010.
The above books were for referring SAR, MOA, uses etc. stuff of drugs. Now for synthesis of drugs we would recommend to refer-
3. Daniel Lednicer, "The Organic Chemistry of Drug Synthesis", Wiley, Volumes- 1 to 7.
4. Douglas S. Johnson and Jie Jack Li, "The Art of Drug Synthesis".Wiley Interscience, 2007.
PHARMACEUTICAL MEDICINAL CHEMISTRY
Basic Principles- 1
Drug metabolism and Concept of Prodrugs; Principles of Drug Design (Theoretical Aspects)- 1
Synthetic Procedures, Mode of Action, Uses, Structure Activity Relationships including Physicochemical Properties of the Following Classes of Drugs:
a. Drugs acting at synaptic and neuro-effector junction sites: Cholinergics, anti-cholinergics and cholinesterase inhibitors, Adrenergic drugs, Antispasmodic and anti-ulcer drugs, Local Anesthetics, Neuromuscular blocking agents- 1,2
b, Autacoids- 1,2
c. Steroidal Drugs- 2
d. Drugs acting on the central nervous system- 1,2
e. Diuretics; Cardiovascular drugs- 1,2
f. Thyroid and Anti thyroid drugs; Insulin and oral hypoglycemic agents- 1
g. Chemotherapeutic Agents used in bacterial, fungal, viral, protozoal, parasitic and other infections, Antibiotics: ß-Lactam, macrolides, tetracyclines, aminoglycosides, polypeptide
antibiotics, fluoroquinolones- 1,2
h. Anti-metabolites (including sulfonamides); Anti-neoplastic agents; Anti-viral agents (including anti–HIV);
Immunosuppressives and immunostimulants; Diagnostic agents; Pharmaceutical Aids- 1,2
BIOCHEMISTRY-
1. David L. Nelson and Michael M. Fox, "Lehninger Principles of Biochemistry", 6th Edition, Macmillan Publishers, 2013,
2. Robert K. Murray, Peter J. Kenelly, David A. Bender, Kethleen M. Bothan, P. Anthony Weil, Victor W. Rodwell, "Harpers Illustrated Biochemistry", 29th Edition, Tata Mc-Graw Hill Publishers, 2012.
BIOCHEMISTRY-
Biochemistry in pharmaceutical sciences- 1,2
Enzymes- 1,2
Co-enzymes- 1,2
Carbohydrate Metabolism- 1,2
The Citric Acid Cycle- 1,2
Lipids Metabolism- 1,2
Essential fatty acids & eicosanoids- Refer Foye and Wilson of Medicinal Chemistry.
Biological Oxidation- 1,2
Metabolism of ammonia and nitrogen containing monomers- 1,2
Purine biosynthesis- 1,2
Pyrimidine biosynthesis and formation of deoxyribounucleotides.
Biosynthesis of Nucleic Acids- 1,2
Mutation- 2
Genetic Code and Protein Synthesis- 1,2
Enzyme Immobilization- 1,2.
This was all about 'MEDICINAL CHEMISTRY' and 'BIOCHEMISTRY'. In the next part we would cover all of 'PHARMACEUTICAL ANALYSIS'.
Hope you would have liked this part, too.. Any kind of feedback and suggestions are welcome by our team !!!
-Darwin
[GPAT-2014- All India Rank (AIR)- 619)
NIPER-JEE-2014 AIR-25 and
ICT-BPT-CET-2014 AIR-7 ]
Ist year M, Tech (Bioprocess Technology-BPT)-2014-16,
Institute of Chemical Technology, Matunga, Mumbai.
Ist year M, Tech (Bioprocess Technology-BPT)-2014-16,
Institute of Chemical Technology, Matunga, Mumbai.
