Synthesis, in vitro bio-evaluation and in silico molecular docking studies of thiadiazole-based Schiff base derivatives
Aim: Recently, thiadiazole-containing drugs have gained greater clinical relevance and are being explored for the development of new antidiabetic, antiurease and antimicrobial agents that target drug resistance. Methods & results: The authors disclose the synthesis of N-(5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl)methanimine derivatives starting from 4-(trifluoromethyl)benzoic acid. All of the synthesized derivatives were evaluated for their biological potential in order to investigate the inhibitory activity against antidiabetic, antiurease and antibacterial profiles. Compounds 1, 2 and 9 showed excellent inhibitory activities due to the hydrogen bonding presence of -OH, -F and -CF3 substitutions attached with the phenyl ring. Conclusion: The present study provides potent antidiabetic, antiurease and antimicrobial agents that can be further optimized to discover novel antidiabetic, antiurease drugs.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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| Enthalten in: |
Future medicinal chemistry - 16(2024), 4 vom: 31. Feb., Seite 335-348 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Khan, Yousaf [VerfasserIn] |
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| Links: |
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| Themen: |
α-amylase |
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| Anmerkungen: |
Date Completed 07.02.2024 Date Revised 07.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0276 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM368038262 |
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| 500 | |a Date Revised 07.02.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Recently, thiadiazole-containing drugs have gained greater clinical relevance and are being explored for the development of new antidiabetic, antiurease and antimicrobial agents that target drug resistance. Methods & results: The authors disclose the synthesis of N-(5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl)methanimine derivatives starting from 4-(trifluoromethyl)benzoic acid. All of the synthesized derivatives were evaluated for their biological potential in order to investigate the inhibitory activity against antidiabetic, antiurease and antibacterial profiles. Compounds 1, 2 and 9 showed excellent inhibitory activities due to the hydrogen bonding presence of -OH, -F and -CF3 substitutions attached with the phenyl ring. Conclusion: The present study provides potent antidiabetic, antiurease and antimicrobial agents that can be further optimized to discover novel antidiabetic, antiurease drugs | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a antibacterial | |
| 650 | 4 | |a molecular docking | |
| 650 | 4 | |a structure–activity relationship | |
| 650 | 4 | |a synthesis | |
| 650 | 4 | |a thiadiazole | |
| 650 | 4 | |a urease | |
| 650 | 4 | |a α-amylase | |
| 650 | 4 | |a α-glucosidase | |
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| 650 | 7 | |a Thiadiazoles |2 NLM | |
| 650 | 7 | |a Anti-Infective Agents |2 NLM | |
| 650 | 7 | |a Hypoglycemic Agents |2 NLM | |
| 700 | 1 | |a Maalik, Aneela |e verfasserin |4 aut | |
| 700 | 1 | |a Rehman, Wajid |e verfasserin |4 aut | |
| 700 | 1 | |a Alanazi, Mohammed M |e verfasserin |4 aut | |
| 700 | 1 | |a Khan, Shoaib |e verfasserin |4 aut | |
| 700 | 1 | |a Hussain, Rafaqat |e verfasserin |4 aut | |
| 700 | 1 | |a Rasheed, Liaqat |e verfasserin |4 aut | |
| 700 | 1 | |a Saboor, Abdul |e verfasserin |4 aut | |
| 700 | 1 | |a Iqbal, Shahid |e verfasserin |4 aut | |
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