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

被引：2

作者：

Morlion, Felien ^{[1
]}

Magdalenic, Katarina ^{[1
]}

Van Camp, John ^{[2
]}

D'hooghe, Matthias ^{[1
]}

机构：

[1] Univ Ghent, Fac Biosci Engn, Dept Green Chem & Technol, SynBioC Res Grp, Coupure Links 653, B-9000 Ghent, Belgium

[2] Univ Ghent, Fac Biosci Engn, Dept Food Technol Safety & Hlth, Lab Food Chem & Human Nutr, Coupure Links 653, B-9000 Ghent, Belgium

来源：

MONATSHEFTE FUR CHEMIE | 2024年 / 155卷 / 06期

关键词：

Heterocycles; Drug research; Structure-activity relationships; Thiazepines; ANTICANCER EVALUATION; IN-SILICO; DERIVATIVES; INHIBITORS; DESIGN; BENZOTHIAZEPINONES; FIELD;

D O I：

10.1007/s00706-024-03195-3

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：535 / 549

页数：15

共 49 条

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