Elsevier S & T

Progress in Medicinal Chemistry

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Table of contents
  • Cover
  • Progress in Medicinal Chemistry 45iii
  • Copyright Pageiv
  • Contentsvii
  • Prefacev
  • List of Contributorsix
  • Chapter 1. Hit and Lead Identification: Efficient Practices for Drug Discovery1
  • Introduction1
  • Hit and Lead Identification Practices2
  • Lead Identification as Reported for Specific Targets11
  • Conclusion49
  • References50
  • Chapter 2. DPPIV Inhibition: Promising Therapy for the Treatment of Type 2 Diabetes63
  • Introduction64
  • Medicinal Chemistry and Preclinical Studies71
  • Clinical Data for Oral DPPIV Inhibitors96
  • Conclusions101
  • Authors Note102
  • References102
  • Chapter 3. Recent Progress Toward Nonpeptide Ligands for the Melanocortin-4 Receptor111
  • Introduction112
  • Cyclohexylpiperidines as Potent MC4R Agonists115
  • Cyclohexylpiperazines and Phenylpiperidines126
  • Phenylpiperazines as MC4R Agonists128
  • Other Classes of MC4R Agonists133
  • Compounds Mimicking α-MSH and its Peptide Analogues135
  • From Agonists to Antagonists137
  • Small Molecule MC4R Antagonists from Initial Screen Hits141
  • Other Nonpeptide MC4R Ligands144
  • Interaction of the MC4R with Ligands145
  • Medicinal Chemistry155
  • Conclusion158
  • References159
  • Chapter 4. Tuberculosis Chemotherapy: Recent Developments and Future Perspectives169
  • Introduction170
  • TB Drug Development Pipeline173
  • Potential New Drug Targets187
  • Concluding Comments194
  • Acknowledgments195
  • References196
  • Subject Index205
  • Author Index (Vols. 1– 45)209
  • Subject Index (Vols. 1– 45)215
Book details
  • Vendor Elsevier S & T
  • SKU 9780444528087
  • ISBN-13 9780080471310

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The success of any drug discovery project relies upon the quality of the lead that initiates the lead optimization process. What defines a ‘quality lead’, where these ‘quality leads’ come from and how one discovers them has been the subject of intense debate within the pharmaceutical industry, relies upon defining those properties that historically have led to successful drug discovery. This volume addresses these questions and specifically discusses diabetes, obesity and tuberculosis.

*Presents the latest research in the field of drug discovery
*Publishes on an annual basis to bring you the most innovative updates in medicinal chemistry
*Available as an online resource via ScienceDirect