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Fundamentals of Medicinal Chemistry and Drug Metabolism 1st Edition by M O Faruk Khan, Ashok E Philip ISBN 9781681086873 1681086875

Name: Fundamentals of Medicinal Chemistry and Drug Metabolism 1st Edition by M O Faruk Khan, Ashok E Philip ISBN 9781681086873 1681086875
SKU: EB-51632086
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Fundamentals of Medicinal Chemistry and Drug Metabolism 1st Edition M. O. Faruk Khan Digital Instant Download

Author(s): M. O. Faruk Khan; Ashok E. Philip

ISBN(s): 9781681086873, 1681086875

Edition: 1

File Details: PDF, 18.90 MB

Year: 2018

Language: English

SKU: EB-51632086 Category: Uncategorized Tags: Ashok E. Philip, M. O. Faruk Khan

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Fundamentals of Medicinal Chemistry and Drug Metabolism 1st Edition by M O Faruk Khan, Ashok E Philip – Ebook PDF Instant Download/Delivery: 9781681086873 ,1681086875
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ISBN 10: 1681086875
ISBN 13: 9781681086873
Author: M O Faruk Khan, Ashok E Philip

The primary objective of this 4-volume book series is to educate PharmD students on the subject of medicinal chemistry. The book set serves as a reference guide to pharmacists on aspects of chemical basis of drug action. This first volume of the series is comprised of 8 chapters focusing on basic background information about medicinal chemistry. It takes a succinct and conceptual approach to introducing important fundamental concepts required for a clear understanding of various facets of pharmacotherapeutic agents, drug metabolism and important biosynthetic pathways that are relevant to drug action. Notable topics covered in this first volume include the scope and importance of medicinal chemistry in pharmacy education, a comprehensive discussion of the organic functional groups present in drugs, and information about four major types of biomolecules (proteins, carbohydrates, lipids, nucleic acids) and key heterocyclic ring systems. The concepts of acid-base chemistry and salt formation, and their applications to the drug action and design follow thereafter. These include concepts of solubility and lipid-water partition coefficient (LWPC), isosterism, stereochemical properties, mechanisms of drug action, drug receptor interactions critical for pharmacological responses of drugs, and much more. Students and teachers will be able to integrate the knowledge presented in the book and apply medicinal chemistry concepts to understand the pharmacodynamics and pharmacokinetics of therapeutic agents in the body.

Fundamentals of Medicinal Chemistry and Drug Metabolism 1st Edition Table of contents:

Drugs Affecting Renin-Angiotensin System
M. O. Faruk Khan1,* and Karrie Murphy1
HISTORICAL BACKGROUND
INTRODUCTORY CONCEPTS
The Renin-Angiotensin System (RAS)
Angiotensin-Converting Enzyme Inhibitors (ACEIs)
Structure of ACE Active Site and Mechanism of Ang I Hydrolysis
Inhibition of ACE – The ACEI-ACE Interaction
Pharmacophore and SAR Summary of ACEIs
SAR Summary
The Individual ACEIs and their Structural and Therapeutic Evaluations
Sulfhydryl-Containing Inhibitor – Captopril
Dicarboxylate Containing Inhibitors
Phosphinate Containing Inhibitor – Fosinopril
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBS)
The AT1R Binding Pockets
Pharmacophore of ARBs and Structure-Activity Relationship
SAR Summary
The Individual ARBs and their Structural and Therapeutic Evaluations
Recalls of the ARBs
Therapeutic Considerations of ACEI and ARBs
RENIN INHIBITOR ALISKIREN (TEKTURNA®)
CASE STUDY
DRUG DISCOVERY CASE STUDIES
Discovery of ACEIs
Teprotide-the First Clue
Carboxypeptidase A – the Homology Model
Development of Captopril
Development of Enalapril and Lisinopril
Development of ARBs
From Saralasin to Losartan and Eprosartan
STUDENT SELF-STUDY GUIDE
STUDENT SELF-ASSESSMENT QUESTIONS
REFERENCES
Ca+2 Channel Blockers
Taufiq Rahman1 and M. O. Faruk Khan2,*
HISTORICAL BACKGROUNDS OF CA2+-CHANNEL BLOCKERS
INTRODUCTORY CONCEPTS
The Voltage Gated Ca2+-Channels (VGCCs) and their Clinical Significance
Sub-classes of VGCC
CALCIUM CHANNEL BLOCKERS
The 1,4-Dihydropyridines (DHPs)
Structure Activity Relationship (SAR) of DHP Derivatives
NO-Releasing Activity of 1,4-Dihydropyridines
Individual 1,4-Dihydropyridine Drugs
Phenylalkylamines (PAAs)
Structure-Activity Relationship of the Phenylalkylamines
Verapamil
Benzothiazepines (BTZs)
Structure-Activity Relationships of Benzothiazepines
Diltiazem
Diaminopropanol Ethers
CLINICAL CASE STUDIES
Case 1
Case 2
Case 3
DRUG DISCOVERY CASE STUDIES
Discovery of Verapamil
Discovery of Nifedipine and its Analogues
STUDENT SELF-STUDY GUIDE
STUDENT SELF-STUDY QUESTIONS
Part I: Multiple Choice Questions.
Questions 6 – 8 are Based on the Following Structures:
REFERENCES
Diuretics
David J. Weldon1, Krista G. Brooks2 and M. O. Faruk Khan3,*
HISTORICAL PERSPECTIVES
INTRODUCTORY CONCEPTS
OSMOTIC DIURETICS
Mechanism of Action of the Osmotic Diuretics
Available Therapeutic Agents (Table 2)
CARBONIC ANHYDRASE INHIBITORS
Mechanism of Action of CAIs
SAR Summary of Sulfonamides as CAIs
Available Therapeutic Agents (Tables 3 and 4)
THIAZIDE DIURETICS
Mechanism of Action of Thiazide Diuretics
SAR Summary of Thiazide Diuretics
Available Therapeutic Agents (Table 5)
LOOP DIURETICS
Mechanism of Action of Loop Diuretics
SAR Summary of Loop Diuretics
Available Therapeutic Agents
POTASSIUM-SPARING DIURETICS
Aldosterone Antagonists
Available Agents
Non-Steroidal MRA: Finerenone (Kerendia®)
Epithelial Sodium Channel (ENaC) Antagonists
Available Agents (Table 8)
CASE STUDIES
Case 1
Case 2
Case 3
DRUG DISCOVERY CASE STORIES
Discovery of Carbonic Anhydrase Inhibitor: Acetazolamide
Discovery of the Thiazide Diuretic Chlorothiazide
Discovery of Loop Diuretic Furosemide
STUDENT SELF-STUDY GUIDE
STUDENT SELF-ASSESSMENT QUESTIONS
REFERENCES
Anticoagulants, Antiplatelets and Thrombolytic Agents
M. O. Faruk Khan1,* and A. R. M. Ruhul Amin2
HISTORICAL BACKGROUND
INTRODUCTORY CONCEPTS
Hemostasis
Biochemical Pathway of Clotting
Blood Coagulation Risk Factors
ANTICOAGULANTS
Heparin and Derivatives
UFHs and LMWHs
Mechanism of Action
Adverse Effects, Contraindications, Antidotes and Pharmacokinetics
Fondaparinux (Arixtra®)
Warfarin
Chemistry, Mechanism of Action, and Therapeutic Uses
Pharmacokinetics
Monitoring of Warfarin Therapy
Food and Drug Interactions
DIRECT THROMBIN INHIBITORS (DTIS)
Hirudin and its Recombinant Derivatives
Argatroban
Oral Direct Thrombin Inhibitor: Dabigatran
DIRECT FACTOR XA INHIBITORS
Rivaroxaban (Xarelto®)
Apixaban (Eliquis®)
Edoxaban (Savaysa®)
Betrixaban (Bevyxxa®)
ANTIPLATELET AGENTS
Cyclooxygenase Inhibitor: Aspirin
Glycoprotein IIb/IIIa Receptor Blockers
Abciximab (ReoPro®)
Eptifibatide (Integrilin®)
Tirofiban (Aggrastat®)
P2Y12 Receptor Blockers: Clopidogrel, Ticlopidine, Prasugrel, Ticagrelor
Thienopyridine Derivatives
ADP Analog: Cangrelor (Kengreal®)
Cyclopentyltriazolopyrimidine: Ticagrelor
Phosphodiesterase (PDE) Inhibitors
Dipyridamole
Cilostazol (Pletal®)
Anagrelide (Xagrid®)
PROTEASE ACTIVATED RECEPTOR 1 (PAR-1) ANTAGONIST
Vorapaxar (Zontivity®)
THROMBOLYTICS
Streptokinase
Alteplase
Reteplase (Retavase®)
Tenecteplase (TNKase®; Metalyse®; Elaxim®)
Defibrotide (Defitelio®)
ANTIDOTES OF ANTICOAGULANTS AND ANTIPLATELETS
Protamine
Andexanet Alfa (Andexxa®)
Idarucizumab (Praxbind®)
Vitamin K
PLATELET STIMULATING AGENTS
Thrombopoietin Receptor Agonists
Eltrombopag (Promacta®)
Romiplostim (Nplate®)
Antifibrinolytic Agents
Tranexamic Acid
ε-Aminocaproic Acid (Amicar®)
CLINICAL CASE STUDY
Case 1
Case 2
DRUG DISCOVERY CASE STUDY
Discovery of Warfarin
Discovery of Ticagrelor
Discovery of Apixaban
STUDENT SELF-STUDY GUIDE
STUDENT SELF-ASSESSMENT QUESTIONS
Match the drug structures (A-H) with the appropriate names (20-26).
REFERENCES
Antihistamines, Proton Pump Inhibitors and Related Drugs
M. O. Faruk Khan1,*
HISTORICAL BACKGROUND
INTRODUCTORY CONCEPTS
Histamine Receptors
Histamine Structural Considerations
Histamine Agonists
Receptor Structures and Pharmacophore Models of the H1 and H2 Receptors
The Histamine H1 Receptor
The Histamine H2 Receptor
HISTAMINE H1 ANTAGONISTS
General Mechanism of Antihistaminic Action
General Structure and Classification of Antihistamines
Therapeutic Evaluations of Each Class of Antihistamines
The General Structure Activity Relationship (SAR)
The Aminoalkanes and Aminoalkenes (Propylamines)
The Piperazines or Cyclizines
The Piperidines
The Aminoalkyl Ethers – Ethanolamines and Propanolamines
Ethylenediamines
Phenothiazines
Miscellaneous Antihistamines
MAST CELL STABILIZERS
Introductory Concepts
Chemistry and Therapeutic Evaluation of Chromones as Mast Cell Stabilizers
HISTAMINE H2 RECEPTOR ANTAGONISTS
Histamine-H2 Receptor Interaction: Mechanism of Action
The General Pharmacophore and SAR of Histamine H2R Antagonists
Chemistry and Therapeutic Evaluations of Individual H2-Blockers
THE H3- AND H4-RECEPTOR ANTAGONISTS
PROTON PUMP INHIBITORS (PPIS)
The Proton Pump
Chemistry and Mechanism of PPIs
Therapeutic Evaluation of the PPIs
pKa Values of the PPIs
Pharmacokinetic Considerations of the PPIs
Drug Interaction: Concurrent Use of PPI and Antiplatelet Agent
CLINICAL CASE STUDIES
Case 1
Case 2
Case 3
DRUG DISCOVERY CASE STUDIES
Development of Antihistamines
Development of Cimetidine
Development of Omeprazole
STUDENT SELF-STUDY GUIDE
STUDENT SELF-ASSESSMENT QUESTIONS
Questions 8 and 9 are Based on Following Structures:
REFERENCES
Diabetes and Antidiabetic Drugs
M. O. Faruk Khan1,*
HISTORICAL BACKGROUND
INTRODUCTORY CONCEPTS
Clinical Overview, Etiology, Risk Factors and Pathophysiology of Diabetes Mellitus
Insulin: Biosynthesis, Metabolism and Receptor Function
Drug Induced Diabetes
Diabetic Ketoacidosis
Hyperglycemic Hyperosmolar Nonketotic Syndrome (HHNS)
MANAGEMENT AND TREATMENT OF DIABETES MELLITUS
Pharmacological Management of Diabetes
Insulin Human and Insulin Analogs
Intermediate-acting Insulin Preparation: NPH Insulin
Clinical Considerations of the Insulins
Sulfonylureas
Meglitinides
Biguanides: Metformin
PPAR Agonists: Thiazolidinediones
Alpha Glucosidase Inhibitor: Acarbose (Precose®)
GLP-1 Agonists
DPP-4 inhibitors or Gliptins
GLP-1 vs DPP-4 Inhibitors
Amylin Agonist: Pramlintide (Symlin®)
SGLT2 Inhibitors, the Gliflozins
Imeglimin (Twymeeg®) – A Novel Class of Investigational Drug
CLINICAL CASE STUDIES
DRUG DISCOVERY CASE STUDIES
Discovery of Dapagliflozin
Discovery of Pioglitazone
Discovery of Metformin
Discovery of Tolbutamide
STUDENT SELF-STUDY GUIDE
STUDENT SELF-ASSESSMENT QUESTIONS
Part III: Matching Questions:
REFERENCES
Hormoneal Therapy
The Prostanoids
M. O. Faruk Khan1,* and Karrie Murphy1
HISTORICAL BACKGROUND
INTRODUCTORY CONCEPTS
Eicosanoids: Structure and Function
Eicosanoids: Biosynthesis
Prostanoid Receptors
Prostacyclin and Prostaglandin Analogs
PROSTAGLANDIN ANALOGS USED IN GLAUCOMA
Latanoprost
Latanoprost Isopropyl Ester (Xalatan®)
Latanoprostene Bunod (Vyzulta®)
Bimatoprost (Lumigan® and Durysta®)
Travoprost (Travatan®)
Unoprostone
Tafluprost
Clinical Consideration of the Prostaglandin Analogs Used for Glaucoma
OTHER PROSTAGLANDIN ANALOGS
Misoprostol (Cytotec®)
Dinoprostone (Preptidil®)
Carboprost
Alprostadil
PROSTACYCLINS
Epoprostenol (Veletri®; Flolan®)
Iloprost (Ilomedine®; Ventavis®)
Teprostinil (Orenitram®, Tyvaso®, Remodulin®)
Selexipag (Uptravi®)
Clinical Consideration for PGI2 Analogs in PAH
LEUKOTRIENE ANALOGS
Montelukast (Singulair®)
Zafirlukast (Accolate®)
CLINICAL CASE STUDY
Case 1
Case 2
DRUG DISCOVERY CASE STUDY
Discovery of Zafirlukast
Discovery of Latanoprost
STUDENT SELF-STUDY GUIDE
STUDENT SELF-ASSESSMENT QUESTIONS
REFERENCES

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