Concepedia

Heterocycle Replacement

Heterocycle Replacement is a bioisosteric strategy in medicinal chemistry wherein a heterocyclic ring system in a bioactive compound is substituted with a structurally or electronically similar ring system to modulate physicochemical, pharmacokinetic, or pharmacodynamic properties while maintaining biological activity.

322

Publications

9.8K

Citations

1.4K

Authors

375

Institutions

Publications per year

2017–2026

30

Variants

Heterocycle Replacements

Parents

Children

Publications

322

The synthetic utility of oxazolines in aromatic substitution

Michael Reuman, A. I. MEYERS · Tetrahedron · 1985 · 322 citations

, , +14

1,5,‐Electrocyclizations—An Important Principle of Heterocyclic Chemistry

Rolf Huisgen · Angewandte Chemie International Edition in English · 1980 · 251 citations

, , +15

Investigation of a Bicyclo[1.1.1]pentane as a Phenyl Replacement within an LpPLA <sub>2</sub> Inhibitor

Nicholas D. Measom, Kenneth Down, David J. Hirst et al. · ACS Medicinal Chemistry Letters · 2016 · 246 citations · Full text

, , +17

Eco-friendly synthesis and biological evaluation of substituted pyrano[2,3-c]pyrazoles

Santhosh Reddy Mandha, Sravanthi Siliveri, Manjula Alla et al. · Bioorganic & Medicinal Chemistry Letters · 2012 · 200 citations

, , +14

Syntheses and antitumor activity of cis-restricted combretastatins: 5-Membered heterocyclic analogues

Koji Ohsumi, Toshihiro Hatanaka, Koichi Fujita et al. · Bioorganic & Medicinal Chemistry Letters · 1998 · 183 citations · Full text

, , +14

1–5 of 322

Authors

1.4K

  1. AR
    Alan R. Katritzky

    University of Florida, United States

    5 publications · 119 citations

    5

    h-index

  2. GK
    Goro Kobayashi

    Nagasaki University, Japan

    3 publications · 51 citations

    3

    h-index

  3. YM
    Yoshiro Matsuda

    Nagasaki University, Japan

    3 publications · 51 citations

    3

    h-index

  4. GB
    G. B. BARLIN

    Australian National University, Australia

    3 publications · 50 citations

    3

    h-index

  5. GJ
    Georges J. Hoornaert

    KU Leuven, Belgium

    3 publications · 142 citations

    3

    h-index

1–5 of 1.4K

Institutions

375

  1. Centre National de la Recherche Scientifique

    Paris, France

    13 h-index

    61 publications

    1.9K citations

  2. Laboratoire de Chimie Organique

    Paris, France

    6 h-index

    21 publications

    649 citations

  3. AstraZeneca (United Kingdom)

    Cambridge, United Kingdom

    5 h-index

    15 publications

    609 citations

  4. The University of Tokyo

    Tokyo, Japan

    5 h-index

    18 publications

    1K citations

  5. Wayne State University

    Detroit, United States

    5 h-index

    21 publications

    959 citations

  6. Indian Institute of Chemical Technology

    Hyderabad, India

    4 h-index

    18 publications

    1.3K citations

  7. National Academy of Sciences of Ukraine

    Kyiv, Ukraine

    4 h-index

    7 publications

    286 citations

  8. Novartis (Switzerland)

    Basel, Switzerland

    4 h-index

    11 publications

    352 citations

1–8 of 375

Venues

  1. Tetrahedron

    35 publications · 1.1K citations

    20

    h-index

  2. Tetrahedron Letters

    33 publications · 865 citations

    18

    h-index

  3. Bioorganic & Medicinal Chemistry Letters

    24 publications · 992 citations

    18

    h-index

  4. Journal of Organometallic Chemistry

    17 publications · 355 citations

    13

    h-index

  5. European Journal of Medicinal Chemistry

    12 publications · 366 citations

    11

    h-index

1–5