Medicinal Chemistry Approaches to Tuberculosis and Trypanosomiasis

Medicinal Chemistry Approaches to Tuberculosis and Trypanosomiasis

1st Edition - September 6, 2019

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  • Editor: Kelly Chibale
  • eBook ISBN: 9780128175576
  • Hardcover ISBN: 9780128175569

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Some of the more recent efforts in tuberculosis (TB) and trypanosomiasis drug discovery from both Product Development Partnerships (PDPs) and academia are highlighted in this this volume. Drug discovery approaches include both target- and phenotypic whole cell screening- approaches. Regarding the latter, mechanism of action studies through target identification are also illustrated.

Key Features

  • Provides an overview of the status of some of the current novel compounds in development as well as new emerging treatment options targeting novel mechanisms of action
  • Identification of hits from phenotypic whole cell screening, followed by target identification
  • Strategies aimed at improving the efficacy of existing clinically used anti-TB drugs by taking advantage inhibitors of mycobacterial transcriptional regulators to boost the anti-tubercular activity, and circumvent acquired-resistance


Medicinal chemists, synthetic chemists, biologists, pharmacologists and clinicians

Table of Contents

  • 1. Tuberculosis
    Steven J. Berthel, Christopher B. Cooper and Nader P. Fotouhi
    2. Antituberculosis agents: Beyond medicinal chemistry rules
    Marco Pieroni
    3. Development of MmpL3 inhibitors for tuberculosis treatment
    Giovanna Poce, Sara Consalvi, Giulia Venditti, Cristina Scarpecci and Mariangela Biava
    4. Inhibitors of enzymes in the electron transport chain of Mycobacterium tuberculosis
    Andrew M. Thompson and William A. Denny
    5. Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance
    Nicolas Willand, Marion Flipo, Baptiste Villemagne, Alain Baulard and Benoit Deprez
    6. Sustainable anti-trypanosomatid drugs: An aspirational goal for medicinal chemistry
    Maria Laura Bolognesi

Product details

  • No. of pages: 188
  • Language: English
  • Copyright: © Academic Press 2019
  • Published: September 6, 2019
  • Imprint: Academic Press
  • eBook ISBN: 9780128175576
  • Hardcover ISBN: 9780128175569

About the Serial Volume Editor

Kelly Chibale

Kelly Chibale
Kelly Chibale is a full Professor of Organic Chemistry at the University of Cape Town (UCT) where he holds the Neville Isdell Chair in African-centric Drug Discovery and Development. He is also a Full Member of the UCT Institute of Infectious Disease & Molecular Medicine, a Tier 1 South Africa Research Chair in Drug Discovery, founding Director of the South African Medical Research Council (SAMRC) Drug Discovery and Development Research Unit at UCT and the Founder and Director of the UCT Drug Discovery and Development Centre (H3D). Kelly obtained his PhD in Synthetic Organic Chemistry from the University of Cambridge in the UK (1989-1992). This was followed by postdoctoral stints at the University of Liverpool in the UK (1992-94) and at the Scripps Research Institute in the USA (1994-96). He was a Sandler Sabbatical Fellow at the University of California San Francisco (2002), a US Fulbright Senior Research Scholar at the University of Pennsylvania School of Medicine (2008) and a Visiting Professor at Pfizer in the UK (2008).

Affiliations and Expertise

University of Cape Town, South Africa

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