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Search Results (3)

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Keywords = Bischler–Napieralski reaction

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12 pages, 1822 KiB  
Article
Spasmolytic Activity of 1,3-Disubstituted 3,4-Dihydroisoquinolines
by Miglena Milusheva, Mihaela Stoyanova, Vera Gledacheva, Iliyana Stefanova, Mina Todorova and Stoyanka Nikolova
Biomedicines 2024, 12(7), 1556; https://doi.org/10.3390/biomedicines12071556 - 13 Jul 2024
Viewed by 1326
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 [...] Read more.
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. Full article
(This article belongs to the Special Issue Advances in Angiogenesis, Inflammation, and Oxidative Stress in Inflammatory Bowel Diseases)
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5 pages, 1347 KiB  
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1-(2-Chlorophenyl)-6,7-dimethoxy-3-methyl-3,4-dihydroisoquinoline
by Miglena Milusheva, Vera Gledacheva, Iliyana Stefanova and Stoyanka Nikolova
Molbank 2023, 2023(2), M1608; https://doi.org/10.3390/M1608 - 23 Mar 2023
Cited by 1 | Viewed by 1654
Abstract
This article concerns the synthesis and in silico evaluation of 1-(2-chlorophenyl)-6-7-dimethoxy-3-methyl-3,4-dihydrogioquinoline (DIQ). A variety of in silico simulations were applied to assess the potential biological activity and toxicity of the compound. Based on these analyses, the target molecule DIQ was chosen for the [...] Read more.
This article concerns the synthesis and in silico evaluation of 1-(2-chlorophenyl)-6-7-dimethoxy-3-methyl-3,4-dihydrogioquinoline (DIQ). A variety of in silico simulations were applied to assess the potential biological activity and toxicity of the compound. Based on these analyses, the target molecule DIQ was chosen for the synthesis. DIQ was synthesized from starting 2-chloro-N-(1-(3,4-dimethoxyphenyl)propan-2-yl)benzamide applied in the Bischler–Napieralski reaction. The newly obtained 3,4-dihydroisoquinoline derivative was fully analyzed and characterized. Based on the in silico calculations, the target molecule was synthesized with respect to its contractile activity, which is a permanent interest of our studies. Thus, further investigation into the possible medicinal applications of this compound is warranted in the future. Full article
(This article belongs to the Section Organic Synthesis and Biosynthesis)
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2 pages, 212 KiB  
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1,2,3,4-Tetrahydroisoquinoline from Acid Catalysed Cyclisation of N,N'-Dibenzylethylenediamine
by N. Peerzada
Molecules 1997, 2(8), M25; https://doi.org/10.3390/M25 - 12 Aug 1997
Viewed by 3394
Abstract
1,2,3,4-Tetrahydroisoquinolines have been traditionally prepared by the Bischler- Napieralski, Pictet-Gams, Pictet-Spengler, Pomeranz-Fritsch reactions and various Friedel- Crafts cyclization procedures of N-(haloalkyl)aryl derivatives [1].[...] Full article
(This article belongs to the Section Molbank Section of Molecules, 1997-2001)
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