Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds
One of the effective strategies in potential “drug-like” molecules design is using a molecular hybridization approach based on the combination of several pharmacological scaffolds in one molecule. The main argument for using this approach is a polypharmacological theory based on the interaction of m...
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| Format: | Article |
| Language: | English |
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Zaporozhye State Medical University
2020-08-01
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| Series: | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
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| Online Access: | http://pharmed.zsmu.edu.ua/article/view/207117/207475 |
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| author | I. M. Yushyn A. V. Lozynskyi O.-M. V. Fedusevych O. Yа. Vovchuk R. B. Lesyk |
| author_facet | I. M. Yushyn A. V. Lozynskyi O.-M. V. Fedusevych O. Yа. Vovchuk R. B. Lesyk |
| author_sort | I. M. Yushyn |
| collection | DOAJ |
| description | One of the effective strategies in potential “drug-like” molecules design is using a molecular hybridization approach based on the combination of several pharmacological scaffolds in one molecule. The main argument for using this approach is a polypharmacological theory based on the interaction of mentioned hybrid molecules with multiple bio-targets based on selectivity and the resulting reduction of toxicity.
The aim of the work is to synthesize a number of new 5-substituted 2-pyrazolylthiazol-4-ones as potentional biologically active compounds.
Materials and methods. Organic synthesis, 1H NMR spectroscopy.
Results. The synthesis of new 5-ene-2-pyrazolylthiazol-4-ones was carried out via a three-component [2+3]-cyclocondensation reaction of 3-methyl-5-aryl-4,5-dihydropyrazole-1-carbothiamides with chloroacetic acid and the corresponding carbonyl compounds in acetic acid medium. The structure of the synthesized compounds was confirmed by elemental analysis and 1H NMR spectroscopy.
Conclusions. As a result of chemical transformations, a library of new thiazole-pyrazoline conjugates was synthesized based on a hybrid-pharmacophore approach to further anticancer activity evaluation within the DTP NCI protocol. |
| first_indexed | 2024-12-12T05:39:53Z |
| format | Article |
| id | doaj.art-2ca47bbbe0a846ab9f08607c2e7b70a4 |
| institution | Directory Open Access Journal |
| issn | 2306-8094 2409-2932 |
| language | English |
| last_indexed | 2024-12-12T05:39:53Z |
| publishDate | 2020-08-01 |
| publisher | Zaporozhye State Medical University |
| record_format | Article |
| series | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
| spelling | doaj.art-2ca47bbbe0a846ab9f08607c2e7b70a42022-12-22T00:35:57ZengZaporozhye State Medical UniversityAktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki2306-80942409-29322020-08-0113221421810.14739/2409-2932.2020.2.207117Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compoundsI. M. Yushyn0A. V. Lozynskyi1O.-M. V. Fedusevych2O. Yа. Vovchuk3R. B. Lesyk4Danylo Halytsky Lviv National Medical University, UkraineDanylo Halytsky Lviv National Medical University, UkraineDanylo Halytsky Lviv National Medical University, UkraineDanylo Halytsky Lviv National Medical University, UkraineDanylo Halytsky Lviv National Medical University, UkraineOne of the effective strategies in potential “drug-like” molecules design is using a molecular hybridization approach based on the combination of several pharmacological scaffolds in one molecule. The main argument for using this approach is a polypharmacological theory based on the interaction of mentioned hybrid molecules with multiple bio-targets based on selectivity and the resulting reduction of toxicity. The aim of the work is to synthesize a number of new 5-substituted 2-pyrazolylthiazol-4-ones as potentional biologically active compounds. Materials and methods. Organic synthesis, 1H NMR spectroscopy. Results. The synthesis of new 5-ene-2-pyrazolylthiazol-4-ones was carried out via a three-component [2+3]-cyclocondensation reaction of 3-methyl-5-aryl-4,5-dihydropyrazole-1-carbothiamides with chloroacetic acid and the corresponding carbonyl compounds in acetic acid medium. The structure of the synthesized compounds was confirmed by elemental analysis and 1H NMR spectroscopy. Conclusions. As a result of chemical transformations, a library of new thiazole-pyrazoline conjugates was synthesized based on a hybrid-pharmacophore approach to further anticancer activity evaluation within the DTP NCI protocol.http://pharmed.zsmu.edu.ua/article/view/207117/207475hybrid-pharmacophore approachthiazolo-pyrazoline conjugates[2+3]-cyclocondensation reactionnmr spectroscopy |
| spellingShingle | I. M. Yushyn A. V. Lozynskyi O.-M. V. Fedusevych O. Yа. Vovchuk R. B. Lesyk Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki hybrid-pharmacophore approach thiazolo-pyrazoline conjugates [2+3]-cyclocondensation reaction nmr spectroscopy |
| title | Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds |
| title_full | Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds |
| title_fullStr | Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds |
| title_full_unstemmed | Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds |
| title_short | Synthesis of novel 5-substituted 2-pyrazolylthiazol-4-ones as potential bioligically active compounds |
| title_sort | synthesis of novel 5 substituted 2 pyrazolylthiazol 4 ones as potential bioligically active compounds |
| topic | hybrid-pharmacophore approach thiazolo-pyrazoline conjugates [2+3]-cyclocondensation reaction nmr spectroscopy |
| url | http://pharmed.zsmu.edu.ua/article/view/207117/207475 |
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