Exploring physicochemical space via a bioisostere of the trifluoromethyl and ethyl groups (BITE): attenuating lipophilicity in fluorinated analogues of Gilenya® for multiple sclerosis-Reference-Cited by-同舟云学术

Exploring physicochemical space via a bioisostere of the trifluoromethyl and ethyl groups (BITE): attenuating lipophilicity in fluorinated analogues of Gilenya® for multiple sclerosis

Published:2018 Issue:85 Volume:54 Page:12002-12005
ISSN:1359-7345
Container-title:Chemical Communications
language:en
Short-container-title:Chem. Commun.

Author:

Erdeljac Nathalie¹²³⁴,Kehr Gerald¹²³⁴^ORCID,Ahlqvist Marie⁵⁶⁷,Knerr Laurent⁸⁶⁷,Gilmour Ryan¹²³⁴⁹^ORCID

Affiliation:

1. Organisch-Chemisches Institut

2. Westfälische Wilhelms-Universität Münster

3. 48149 Münster

4. Germany

5. Drug Metabolism and Pharmacokinetics, Cardiovascular, Renal and Metabolism IMED Biotech Unit

6. Astrazeneca

7. Sweden

8. Medicinal Chemistry, Cardiovascular, Renal and Metabolism IMED Biotech Unit

9. Excellence Cluster EXC 1003, Cells in Motion Westfälische Wilhems-Universität Münster

Abstract

The BITE bioisostere of Et and CF₃ allows lipophilicity to be tempered in analogues of the multiple sclerosis drug Gilenya®.

Funder

H2020 European Research Council

Deutsche Forschungsgemeinschaft

Westfälische Wilhelms-Universität Münster

Publisher

Royal Society of Chemistry (RSC)

Subject

Materials Chemistry,Metals and Alloys,Surfaces, Coatings and Films,General Chemistry,Ceramics and Composites,Electronic, Optical and Magnetic Materials,Catalysis

Link

http://pubs.rsc.org/en/content/articlepdf/2018/CC/C8CC05643A

Reference50 articles.

1. Fluorine in Medicinal Chemistry

2. The role of fluorine in medicinal chemistry

3. Fluorine in Pharmaceuticals: Looking Beyond Intuition

4. Applications of Fluorine in Medicinal Chemistry

5. Fluorinated amino acids: compatibility with native protein structures and effects on protein–protein interactions

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