Online resource; title from PDF title page (ScienceDirect, viewed July 16, 2015).

Includes bibliographical references.

Front Cover; Prodrug Design; Copyright Page; Dedication; Contents; Preface; 1 Introduction; 1.1 Background; 1.2 Drug Development; 1.3 The Drug Discovery Process; 1.3.1 Goal of Drug Discovery; 1.3.2 Constraints in Drug Discovery; 1.4 Current Scenario in Prodrug Research; 1.5 Need of the Study; References; 2 Concept of Prodrug; 2.1 Concept of Prodrug; 2.2 Undesirable Properties Associated with Drug Molecules; 2.3 Prodrug Design: Past to Present; 2.4 Definitions of Prodrug; 2.5 Rationale for the Use of Prodrugs; 2.6 Targeted Prodrug Design; 2.7 Double Prodrug Concept; 2.8 Steps in Prodrug Design.

2.8.1 Hard Drugs2.8.2 Soft Drugs; 2.9 Objectives in Prodrug Research; 2.9.1 Pharmaceutical Objectives; 2.9.2 Pharmacokinetic Objectives; 2.9.3 Pharmacodynamic Objectives; 2.10 Evaluation of Prodrugs; 2.10.1 Physiochemical Parameters; 2.10.2 Pharmacokinetics Profile; 2.10.3 Pharmacodynamics; References; 3 Types of Prodrugs; 3.1 Classification of Prodrugs; 3.1.1 Research-Related Criteria; 3.1.2 Chemical Criteria; 3.1.2.1 Carrier-Linked Prodrug; 3.1.2.2 Mutual Prodrug; 3.1.2.3 Bioprecursor Prodrug; 3.1.2.3.1 Oxidative Bioactivations; 3.1.2.3.2 Reductive Bioactivations; 3.1.2.4 Polymeric Prodrug.

3.1.2.5 Tripartate Prodrug3.2 Criteria for Prodrug; 3.3 Classifying Prodrugs; 3.4 Challenges and Limitations in Prodrug Design; References; 4 Approaches for Prodrugs; 4.1 Promoiety; 4.2 Functional Groups Compliant for Design of Prodrug; 4.3 Bioreversible Derivatives for Various Functional Groups; 4.4 Phosphate Esters as Prodrugs of Hydroxyl or Amine Functionalities; 4.5 Amides as Prodrugs of Carboxylic Acids and Amines; 4.6 Prodrug for Amides, Imides, and Other Acidic Compounds; 4.6.1 N-Mannich Bases and Acyloxy Derivatives; 4.6.2 N-Acyl Derivatives; 4.6.3 N-Hydroxy Methyl Derivatives.

4.7 Prodrugs for Amines4.7.1 N-(Acyloxy Alkoxy Carbonyl) Derivatives and Amide Derivatives; 4.7.2 Oxazolidines; 4.8 Prodrugs with Carbonyl groups; 4.8.1 Thiazolidines; 4.8.2 Enol Esters; 4.9 Types of Promoieties Used in Designing of Prodrugs; 4.9.1 Amino Acids; 4.9.2 Polysaccharides; 4.9.3 Alcohols; 4.9.4 Phytophenols; 4.9.5 Amines; 4.9.6 Polymers; 4.9.6.1 Requirements for Selecting Polymers as Candidate Drug Carriers; 4.9.6.2 Classification of Polymers Used for Bioconjugation; 4.10 Coupling of Drug and Polymer Through Spacers; References; 5 Applications; 5.1 Applications of Prodrug Designing.

5.1.1 Masking Taste and Odor5.1.2 Minimizing Pain at Injection Site; 5.1.3 Alteration of Drug Solubility; 5.1.4 Enhancement of Chemical Stability; 5.1.5 Prodrugs to Overcome Absorption Problems; 5.1.5.1 Enhancement of Oral Absorption; 5.1.5.2 Enhancement of Ophthalmic Absorption; 5.1.5.3 Enhancement of Percutaneous Absorption; 5.1.6 Prevention of Presystemic Metabolism; 5.1.7 Longer Duration of Action; 5.1.8 To Diminish Local and Systemic Toxicity of Drugs/Reduction of GI Irritability; 5.1.9 Site-Specific Drug Delivery; 5.1.10 Prodrug for Slow and Prolonged Release (Sustained Drug Action).

Prodrug Design: Perspectives, Approaches and Applications in Medicinal Chemistry provides a focused overview of this critical area of drug discovery, as that continuous process strives not only to discover new drug compounds but also to modify the existing ones. This valuable primer supports this mission of drug development and its goal of reducing undesired effects and improving therapeutic effectiveness of drug compounds. Providing a unique compilation of data, insightful case studies, and review of existing literature in the area, the book will promote innovation in medicinal and pharmaceu.