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Heterocycle-substituted 1,5-benzothiazepines : biological properties and structure-activity relationships

Felien Morlion (UGent) , Katarina Magdalenic (UGent) , John Van Camp (UGent) and Matthias D'hooghe (UGent)
(2024) MONATSHEFTE FUR CHEMIE. 155(6). p.535-549
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Abstract
1,5-Benzothiazepines represent key scaffolds in medicinal chemistry because of their applicability in a wide variety of pharmaceuticals. Many cardiovascular, antidepressant, and antipsychotic drugs on the market accommodate this privileged structure, but the biological effects of 1,5-benzothiazepines are much more diverse, including enzyme inhibitory, antimicrobial, central nervous system depressant, anti-inflammatory, and anticancer activity. The introduction of a heterocyclic substituent onto a chemical structure can be beneficial in terms of bioactivity and drug-like properties. In this review, the biological activities of 1,5-benzothiazepines with and without heterocyclic substituents are discussed and compared. In some cases, the addition of a heterocycle proved to be beneficial for enhancing activity, especially the introduction of a 2-thienyl group, and also the position of heteroatoms in the substituent can have an impact on the overall properties of the resulting compounds.
Keywords
Heterocycles, Drug research, Structure-activity relationships, Thiazepines, ANTICANCER EVALUATION, IN-SILICO, DERIVATIVES, INHIBITORS, DESIGN, BENZOTHIAZEPINONES, FIELD

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MLA
Morlion, Felien, et al. “Heterocycle-Substituted 1,5-Benzothiazepines : Biological Properties and Structure-Activity Relationships.” MONATSHEFTE FUR CHEMIE, vol. 155, no. 6, 2024, pp. 535–49, doi:10.1007/s00706-024-03195-3.
APA
Morlion, F., Magdalenic, K., Van Camp, J., & D’hooghe, M. (2024). Heterocycle-substituted 1,5-benzothiazepines : biological properties and structure-activity relationships. MONATSHEFTE FUR CHEMIE, 155(6), 535–549. https://doi.org/10.1007/s00706-024-03195-3
Chicago author-date
Morlion, Felien, Katarina Magdalenic, John Van Camp, and Matthias D’hooghe. 2024. “Heterocycle-Substituted 1,5-Benzothiazepines : Biological Properties and Structure-Activity Relationships.” MONATSHEFTE FUR CHEMIE 155 (6): 535–49. https://doi.org/10.1007/s00706-024-03195-3.
Chicago author-date (all authors)
Morlion, Felien, Katarina Magdalenic, John Van Camp, and Matthias D’hooghe. 2024. “Heterocycle-Substituted 1,5-Benzothiazepines : Biological Properties and Structure-Activity Relationships.” MONATSHEFTE FUR CHEMIE 155 (6): 535–549. doi:10.1007/s00706-024-03195-3.
Vancouver
1.
Morlion F, Magdalenic K, Van Camp J, D’hooghe M. Heterocycle-substituted 1,5-benzothiazepines : biological properties and structure-activity relationships. MONATSHEFTE FUR CHEMIE. 2024;155(6):535–49.
IEEE
[1]
F. Morlion, K. Magdalenic, J. Van Camp, and M. D’hooghe, “Heterocycle-substituted 1,5-benzothiazepines : biological properties and structure-activity relationships,” MONATSHEFTE FUR CHEMIE, vol. 155, no. 6, pp. 535–549, 2024.
@article{01J1A4C77B8B36N5RG8GWXBQDD,
  abstract     = {{1,5-Benzothiazepines represent key scaffolds in medicinal chemistry because of their applicability in a wide variety of pharmaceuticals. Many cardiovascular, antidepressant, and antipsychotic drugs on the market accommodate this privileged structure, but the biological effects of 1,5-benzothiazepines are much more diverse, including enzyme inhibitory, antimicrobial, central nervous system depressant, anti-inflammatory, and anticancer activity. The introduction of a heterocyclic substituent onto a chemical structure can be beneficial in terms of bioactivity and drug-like properties. In this review, the biological activities of 1,5-benzothiazepines with and without heterocyclic substituents are discussed and compared. In some cases, the addition of a heterocycle proved to be beneficial for enhancing activity, especially the introduction of a 2-thienyl group, and also the position of heteroatoms in the substituent can have an impact on the overall properties of the resulting compounds.}},
  author       = {{Morlion, Felien and Magdalenic, Katarina and Van Camp, John and D'hooghe, Matthias}},
  issn         = {{0026-9247}},
  journal      = {{MONATSHEFTE FUR CHEMIE}},
  keywords     = {{Heterocycles,Drug research,Structure-activity relationships,Thiazepines,ANTICANCER EVALUATION,IN-SILICO,DERIVATIVES,INHIBITORS,DESIGN,BENZOTHIAZEPINONES,FIELD}},
  language     = {{eng}},
  number       = {{6}},
  pages        = {{535--549}},
  title        = {{Heterocycle-substituted 1,5-benzothiazepines : biological properties and structure-activity relationships}},
  url          = {{http://doi.org/10.1007/s00706-024-03195-3}},
  volume       = {{155}},
  year         = {{2024}},
}
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