# Spasmolytic Activity of 1,3-Disubstituted 3,4-Dihydroisoquinolines

**Authors:** Miglena Milusheva, Mihaela Stoyanova, Vera Gledacheva, Iliyana Stefanova, Mina Todorova, Stoyanka Nikolova

PMC · DOI: 10.3390/biomedicines12071556 · Biomedicines · 2024-07-13

## TL;DR

This paper explores new compounds that may help relax smooth muscles and could be useful in treating various disorders.

## Contribution

The study identifies two new compounds with spasmolytic and antioxidant properties that could be used as therapeutic agents.

## Key findings

- Two new compounds show potential as smooth muscle relaxants and meet drug absorption criteria.
- One compound exhibits significant antioxidant activity compared to rutin.
- The compounds may cross the blood-brain barrier, making them promising for drug development.

## Abstract

This article concerns the spasmolytic activities of some novel 1,3-disubstituted 3,4-dihydroisoquinolines. These compounds can be evaluated as potential therapeutic candidates according to Lipinski’s rule of five, showing high gastrointestinal absorption and the ability to cross the blood–brain barrier, which is a very important parameter in the drug discovery processes. In silico simulation predicted smooth muscle relaxant activity for all the compounds. Since smooth muscle contractile failure is a characteristic feature of many disorders, in the current paper, we concentrate on the parameters of the spontaneous contractile responses of smooth muscle (SM) cells compared to the well-known drug mebeverine. Two of the newly synthesized substances can be identified as essential modulating regulators and potentially used as therapeutic molecules. One of these molecules also showed significant DPPH antioxidant activity compared to rutin.

## Linked entities

- **Chemicals:** mebeverine (PubChem CID 4031), rutin (PubChem CID 5280805)

## Full-text entities

- **Chemicals:** 1,3-Disubstituted 3,4-Dihydroisoquinolines (-), DPPH (MESH:C004931), mebeverine (MESH:C005096), rutin (MESH:D012431)

## Full text

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## Figures

6 figures with captions in the complete paper: https://tomesphere.com/paper/PMC11275145/full.md

## References

41 references — full list in the complete paper: https://tomesphere.com/paper/PMC11275145/full.md

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Source: https://tomesphere.com/paper/PMC11275145