Concepedia

Bioisosteric Lead Optimization

Bioisosteric Lead Optimization is a medicinal chemistry strategy that replaces a phenyl ring or other aromatic moiety in a lead compound with a structurally distinct but functionally analogous bioisostere to improve pharmacokinetic, pharmacodynamic, or synthetic properties while preserving target affinity.

14

Publications

3.3K

Citations

83

Authors

28

Institutions

Publications per year

2017–2026

4

Parents

Publications

14

Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design

Nicholas A. Meanwell · Journal of Medicinal Chemistry · 2011 · 2.8K citations · Full text

, , +11

The use of bioisosteric groups in lead optimization.

Olesen Ph · PubMed · 2001 · 75 citations

, , +17

Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties

Kato Bredael, Silke Geurs, Dorien Clarisse et al. · Journal of Chemistry · 2022 · 64 citations · Full text

, , +17

Optimization of a Small Tropomyosin-Related Kinase B (TrkB) Agonist 7,8-Dihydroxyflavone Active in Mouse Models of Depression

Xia Liu, Chi-Bun Chan, Qi Qi et al. · Journal of Medicinal Chemistry · 2012 · 59 citations · Full text

, , +17

Catecholic Flavonoids Acting as Telomerase Inhibitors

Maria Menichincheri, Dario Ballinari, Alberto Bargiotti et al. · Journal of Medicinal Chemistry · 2004 · 57 citations · Full text

, , +17

1–5 of 14

Authors

83

  1. CZ
    Chariklia Zika

    Aristotle University of Thessaloniki, Greece

    1 publications · 51 citations

    1

    h-index

  2. IN
    Ioannis Nicolaou

    Aristotle University of Thessaloniki, Greece

    1 publications · 51 citations

    1

    h-index

  3. JS
    Jinwen Shan

    New York University Shanghai, China

    1 publications · 41 citations

    1

    h-index

  4. JK
    Julien Korac

    Euroscreen (Belgium), Belgium

    1 publications · 39 citations

    1

    h-index

  5. EV
    Ermes Vanotti

    Nerviano Medical Sciences, Italy

    1 publications · 57 citations

    1

    h-index

1–5 of 83

Institutions

28

  1. Euroscreen (Belgium)

    Charleroi, Belgium

    1 h-index

    11 publications

    429 citations

  2. New York University Shanghai

    Shanghai, China

    1 h-index

    2 publications

    82 citations

  3. EA Pharma (Japan)

    Tokyo, Japan

    1 h-index

    9 publications

    198 citations

  4. University of Copenhagen

    Copenhagen, Denmark

    1 h-index

    1 publications

    47 citations

  5. Bristol-Myers Squibb (United States)

    New York, United States

    1 h-index

    1 publications

    2.8K citations

  6. Torino e-district

    Turin, Italy

    1 h-index

    8 publications

    376 citations

  7. Bristol-Myers Squibb (Germany)

    Munich, Germany

    1 h-index

    1 publications

    2.8K citations

  8. Northwestern University

    Evanston, United States

    1 h-index

    1 publications

    59 citations

1–8 of 28

Venues

  1. Journal of Medicinal Chemistry

    5 publications · 3K citations

    5

    h-index

  2. Bioorganic & Medicinal Chemistry Letters

    2 publications · 29 citations

    2

    h-index

  3. MedChemComm

    1 publications · 47 citations

    1

    h-index

  4. Journal of Agricultural and Food Chemistry

    1 publications · 23 citations

    1

    h-index

  5. PubMed

    Repository · 1 publications · 75 citations

    1

    h-index

1–5