Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers
Abstract
Chemical evolution of mibefradil resulted in the identification of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers. A SAR study, in vitro and in vivo DMPK properties as well as the in vivo antihypertensive effect in rats are presented.
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THN-fused C3-spirooxindoles should possess good druglikeness because THN and spirooxindole derivatives are privileged drug-like architectures.
“We started with THN54, 55, 56, 57, 58, 59, 60, 61 and spirooxindole derivatives62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72 because they are privileged drug-like architectures, so the resulting THN-fused C3-spirooxindoles should possess good druglikeness (Fig. 2C).”
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Wang, B., Peng, F., Huang, W., Zhou, J., Zhang, N., Sheng, J., Haruehanroengra, P., He, G., & Han, B. (2020) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2019.12.013 · Cited by 73 · see citing works
- Authors
- Renneberg, D., Hubler, F., Rey, M., Hess, P., Delahaye, S., Gatfield, J., Iglarz, M., & Hilpert, K.
- Affiliations
- Actelion (Switzerland) (CH)
- Corresponding author
- Renneberg, Dorte
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 2015-09
- Volume
- 25
- Issue
- 18
- Pages
- 3941-3946
- ISSN
- 0960-894X (ISSN-L)
- OpenAlex
- W1020710735
- Cited by
- 5
- References
- 19
- Citations by year
- 2025: 1 · 2019: 1 · 2018: 1 · 2017: 1 · 2016: 1
- FWCI
- 0.43
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Bioorganic & Medicinal Chemistry Letters (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Blood Pressure and Hypertension Studies
- Keywords
- tetrahydronaphthalene derivatives, T-type calcium channel blockers, L-type calcium channel blockers, mibefradil, structure-activity relationship, drug metabolism and pharmacokinetics, antihypertensive effect, chemical evolution
- MeSH terms
- Animals, Calcium Channel Blockers, Dose-Response Relationship, Drug, Molecular Conformation, Rats, Inbred SHR, Structure-Activity Relationship, Tetrahydronaphthalenes, Calcium Channels, Rats, Drug Discovery
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