Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents
A series of 1,3-thiazoline-4-one derivatives bearing 2-phenoxyphenyl moiety, were synthesized as potential new analgesic and anti-inflammatory agents. The structures were confirmed by FT-IR, NMR and mass spectra. The abdominal constriction (writing) test was selected to evaluate analgesic activity a...
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| Format: | Article |
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Serbian Chemical Society
2024-01-01
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| Series: | Journal of the Serbian Chemical Society |
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| Online Access: | https://doiserbia.nb.rs/img/doi/0352-5139/2024/0352-51392400064N.pdf |
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| author | Nassiri Koopaei Mansur Monavari Mahshid Vousooghi Nasim Moshirabadi Sadaf Assarzadeh Mohammad Javad Amini Mohsen Almasirad Ali |
| author_facet | Nassiri Koopaei Mansur Monavari Mahshid Vousooghi Nasim Moshirabadi Sadaf Assarzadeh Mohammad Javad Amini Mohsen Almasirad Ali |
| author_sort | Nassiri Koopaei Mansur |
| collection | DOAJ |
| description | A series of 1,3-thiazoline-4-one derivatives bearing 2-phenoxyphenyl moiety, were synthesized as potential new analgesic and anti-inflammatory agents. The structures were confirmed by FT-IR, NMR and mass spectra. The abdominal constriction (writing) test was selected to evaluate analgesic activity and the results showed that nearly all of them were active, and the most potent was 10m with 96 % inhibition when compared to the control. The best compounds were selected to investigate the anti-inflammatory activity by carrageenan induced rat paw edema test. The results showed that compounds 8 and 10h were active from the 2nd to 5th hour of assessment. The ulcerogenic evaluation of two selected compounds showed that they are comparable with the vehicle control group and without any ulcerogenic effect potential. The target compounds showed an acceptable in silico ADME profile. |
| format | Article |
| id | doaj-art-422d997770cf404493e26c990dde662c |
| institution | Kabale University |
| issn | 0352-5139 1820-7421 |
| language | English |
| publishDate | 2024-01-01 |
| publisher | Serbian Chemical Society |
| record_format | Article |
| series | Journal of the Serbian Chemical Society |
| spelling | doaj-art-422d997770cf404493e26c990dde662c2025-01-30T06:45:49ZengSerbian Chemical SocietyJournal of the Serbian Chemical Society0352-51391820-74212024-01-0189111411142210.2298/JSC231029064N0352-51392400064NSynthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agentsNassiri Koopaei Mansur0Monavari Mahshid1https://orcid.org/0000-0001-7561-8823Vousooghi Nasim2https://orcid.org/0000-0002-3392-3640Moshirabadi Sadaf3https://orcid.org/0009-0001-2694-4830Assarzadeh Mohammad Javad4Amini Mohsen5https://orcid.org/0000-0003-3135-2917Almasirad Ali6https://orcid.org/0000-0001-9192-7888Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, IranDepartment of Pharmacology and Toxicology, Faculty of Pharmacy, Tehran Medical Sciences, Islamic Azad University, Tehran, IranDepartment of Applied Cell Sciences, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran + Research Center for Cognitive and Behavioral Sciences, Tehran University of Medical Sciences, Tehran, IranDepartment of Medicinal Chemistry, Faculty of Pharmacy, Tehran Medical Sciences, Islamic Azad University, Tehran, IranDepartment of Medicinal Chemistry, Faculty of Pharmacy, Tehran Medical Sciences, Islamic Azad University, Tehran, IranDepartment of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran + Pharmaceutical Sciences Research Center (PSRC), The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, IranDepartment of Medicinal Chemistry, Faculty of Pharmacy, Tehran Medical Sciences, Islamic Azad University, Tehran, IranA series of 1,3-thiazoline-4-one derivatives bearing 2-phenoxyphenyl moiety, were synthesized as potential new analgesic and anti-inflammatory agents. The structures were confirmed by FT-IR, NMR and mass spectra. The abdominal constriction (writing) test was selected to evaluate analgesic activity and the results showed that nearly all of them were active, and the most potent was 10m with 96 % inhibition when compared to the control. The best compounds were selected to investigate the anti-inflammatory activity by carrageenan induced rat paw edema test. The results showed that compounds 8 and 10h were active from the 2nd to 5th hour of assessment. The ulcerogenic evaluation of two selected compounds showed that they are comparable with the vehicle control group and without any ulcerogenic effect potential. The target compounds showed an acceptable in silico ADME profile.https://doiserbia.nb.rs/img/doi/0352-5139/2024/0352-51392400064N.pdfthiazolinefenamatewriting testcarrageenan induced edemacyclooxygenase |
| spellingShingle | Nassiri Koopaei Mansur Monavari Mahshid Vousooghi Nasim Moshirabadi Sadaf Assarzadeh Mohammad Javad Amini Mohsen Almasirad Ali Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents Journal of the Serbian Chemical Society thiazoline fenamate writing test carrageenan induced edema cyclooxygenase |
| title | Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents |
| title_full | Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents |
| title_fullStr | Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents |
| title_full_unstemmed | Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents |
| title_short | Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents |
| title_sort | synthesis and in silico admet evaluation of new thiazole and thiazolidine 4 one derivatives as non ulcerogenic analgesic and anti inflammatory agents |
| topic | thiazoline fenamate writing test carrageenan induced edema cyclooxygenase |
| url | https://doiserbia.nb.rs/img/doi/0352-5139/2024/0352-51392400064N.pdf |
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