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| Main Authors: | , , , , , , , , , , , , , , , , , |
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| Format: | Artículo científico |
| Language: | en |
| Published: |
Archiv der Pharmazie
2026
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| Subjects: | |
| Online Access: | https://pubmed.ncbi.nlm.nih.gov/41866767/ |
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| _version_ | 1868266069675737088 |
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| author | Mousavi, Alireza Slapničková, Martina Norouzbahari, Maryam D'Alessandro, Sarah Foroumadi, Parham Peytam, Fariba Perego, Federica Doleželová, Eva Emamgholipour, Zahra Tehrani, Maliheh Barazandeh Sadat-Ebrahimi, Seyed Esmaeil Hosseinzadeh, Elahe Ahadi, Elmira Meghrazi Firoozpour, Loghman Bijanzadeh, Hamidreza Basilico, Nicoletta Zíková, Alena Foroumadi, Alireza |
| author_facet | Mousavi, Alireza Slapničková, Martina Norouzbahari, Maryam D'Alessandro, Sarah Foroumadi, Parham Peytam, Fariba Perego, Federica Doleželová, Eva Emamgholipour, Zahra Tehrani, Maliheh Barazandeh Sadat-Ebrahimi, Seyed Esmaeil Hosseinzadeh, Elahe Ahadi, Elmira Meghrazi Firoozpour, Loghman Bijanzadeh, Hamidreza Basilico, Nicoletta Zíková, Alena Foroumadi, Alireza Mousavi, Alireza Slapničková, Martina Norouzbahari, Maryam D'Alessandro, Sarah Foroumadi, Parham Peytam, Fariba Perego, Federica Doleželová, Eva Emamgholipour, Zahra Tehrani, Maliheh Barazandeh Sadat-Ebrahimi, Seyed Esmaeil Hosseinzadeh, Elahe Ahadi, Elmira Meghrazi Firoozpour, Loghman Bijanzadeh, Hamidreza Basilico, Nicoletta Zíková, Alena Foroumadi, Alireza |
| collection | PubMed - marine biology |
| contents | Exploring Novel Nitrofuryl-1,3,4-Thiadiazole-Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity. Mousavi, Alireza Slapničková, Martina Norouzbahari, Maryam D'Alessandro, Sarah Foroumadi, Parham Peytam, Fariba Perego, Federica Doleželová, Eva Emamgholipour, Zahra Tehrani, Maliheh Barazandeh Sadat-Ebrahimi, Seyed Esmaeil Hosseinzadeh, Elahe Ahadi, Elmira Meghrazi Firoozpour, Loghman Bijanzadeh, Hamidreza Basilico, Nicoletta Zíková, Alena Foroumadi, Alireza Thiadiazoles Drug Design Humans Structure-Activity Relationship Parasitic Sensitivity Tests Antiprotozoal Agents Molecular Structure Trypanocidal Agents Dose-Response Relationship, Drug Trypanosoma brucei brucei Reactive Oxygen Species THP-1 Cells Leishmania Apoptosis Neglected tropical diseases remain a major global health challenge, highlighting the need for new antiparasitic agents. In this study, a series of substituted 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carboxamides was designed, synthesized, and evaluated for in vitro antileishmanial and antitrypanosomal activity. Compound 18 emerged as the most promising derivative, showing submicromolar activity against all tested parasites with acceptable selectivity toward THP-1 cells. Mechanistic studies in T. b. brucei bloodstream cells revealed a reversible cytostatic effect rather than apoptosis, and assessment of cellular and mitochondrial ROS levels indicated that oxidative stress was not a primary contributor to activity. In silico ADME analysis supported the drug-likeness of the synthesized compounds. Taken together, these findings identify 18 as a valuable lead for further antiparasitic drug development. |
| format | Artículo científico |
| id | pubmed_41866767 |
| institution | PubMed |
| language | en |
| publishDate | 2026 |
| publisher | Archiv der Pharmazie |
| record_format | pubmed |
| spellingShingle | Exploring Novel Nitrofuryl-1,3,4-Thiadiazole-Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity. Mousavi, Alireza Slapničková, Martina Norouzbahari, Maryam D'Alessandro, Sarah Foroumadi, Parham Peytam, Fariba Perego, Federica Doleželová, Eva Emamgholipour, Zahra Tehrani, Maliheh Barazandeh Sadat-Ebrahimi, Seyed Esmaeil Hosseinzadeh, Elahe Ahadi, Elmira Meghrazi Firoozpour, Loghman Bijanzadeh, Hamidreza Basilico, Nicoletta Zíková, Alena Foroumadi, Alireza Thiadiazoles Drug Design Humans Structure-Activity Relationship Parasitic Sensitivity Tests Antiprotozoal Agents Molecular Structure Trypanocidal Agents Dose-Response Relationship, Drug Trypanosoma brucei brucei Reactive Oxygen Species THP-1 Cells Leishmania Apoptosis Exploring Novel Nitrofuryl-1,3,4-Thiadiazole-Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity. Mousavi, Alireza Slapničková, Martina Norouzbahari, Maryam D'Alessandro, Sarah Foroumadi, Parham Peytam, Fariba Perego, Federica Doleželová, Eva Emamgholipour, Zahra Tehrani, Maliheh Barazandeh Sadat-Ebrahimi, Seyed Esmaeil Hosseinzadeh, Elahe Ahadi, Elmira Meghrazi Firoozpour, Loghman Bijanzadeh, Hamidreza Basilico, Nicoletta Zíková, Alena Foroumadi, Alireza Thiadiazoles Drug Design Humans Structure-Activity Relationship Parasitic Sensitivity Tests Antiprotozoal Agents Molecular Structure Trypanocidal Agents Dose-Response Relationship, Drug Trypanosoma brucei brucei Reactive Oxygen Species THP-1 Cells Leishmania Apoptosis Neglected tropical diseases remain a major global health challenge, highlighting the need for new antiparasitic agents. In this study, a series of substituted 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carboxamides was designed, synthesized, and evaluated for in vitro antileishmanial and antitrypanosomal activity. Compound 18 emerged as the most promising derivative, showing submicromolar activity against all tested parasites with acceptable selectivity toward THP-1 cells. Mechanistic studies in T. b. brucei bloodstream cells revealed a reversible cytostatic effect rather than apoptosis, and assessment of cellular and mitochondrial ROS levels indicated that oxidative stress was not a primary contributor to activity. In silico ADME analysis supported the drug-likeness of the synthesized compounds. Taken together, these findings identify 18 as a valuable lead for further antiparasitic drug development. |
| title | Exploring Novel Nitrofuryl-1,3,4-Thiadiazole-Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity. |
| topic | Thiadiazoles Drug Design Humans Structure-Activity Relationship Parasitic Sensitivity Tests Antiprotozoal Agents Molecular Structure Trypanocidal Agents Dose-Response Relationship, Drug Trypanosoma brucei brucei Reactive Oxygen Species THP-1 Cells Leishmania Apoptosis |
| url | https://pubmed.ncbi.nlm.nih.gov/41866767/ |