Synthesis, in vitro biological analysis and molecular docking studies of new thiadiazole-based thiourea derivatives as dual inhibitors of a-amylase and a-glucosidase DOI Creative Commons

Imran Khan,

Wajid Rehman, Fazal Rahim

et al.

Arabian Journal of Chemistry, Journal Year: 2023, Volume and Issue: 16(9), P. 105078 - 105078

Published: June 17, 2023

Diabetes mellitus is a syndrome that caused due to the imbalance of insulin production in body. In present study we have synthesized class fifteen compounds (1–15) based on thiadiazole-bearing thiourea were assessed for vitro alpha-amylase and alpha-glucosidase inhibitory potentials against standard drug acarbose. this series, all scaffolds recognized as inhibitors both targeted enzymes, α-amylase having varied range from IC50 values = 35.70 ± 0.70 µM 1.30 0.05 acarbose (10.30 0.20 µM) while α-glucosidase 37.60 0.80 2.20 0.10 (9.80 µM). Among nine such 4, 6, 7, 9, 8, 11, 12, 14 15 showed excellent activity a-amylase a-glucosidase found many folds more potent than drugs change nature number/s substituent along entire skeleton. A molecular docking was conducted active understand binding modes synthetic analogs how they show interaction with part enzymes. To confirm structure different spectroscopic techniques will be used like NMR HREI-MS.

Language: Английский

Power of sulfur – Chemistry, properties, laser ignition and theoretical studies of energetic perchlorate-free 1,3,4-thiadiazole nitramines DOI
Jagadish Das,

Daniel Shem‐Tov,

Shijie Zhang

et al.

Chemical Engineering Journal, Journal Year: 2022, Volume and Issue: 443, P. 136246 - 136246

Published: April 6, 2022

Language: Английский

Citations

28
Recent advances in the synthesis and performance of 1,2,4,5-tetrazine-based energetic materials DOI Creative Commons
Леонид Л. Ферштат

FirePhysChem, Journal Year: 2022, Volume and Issue: 3(1), P. 78 - 87

Published: Sept. 20, 2022

In recent years, the development of novel advanced energetic materials has significantly shifted toward nitrogen heterocyclic derivatives, which demonstrate a great potential for multipurpose application patterns. Among known heterocycles tetrazine ring is well-known structural scaffold used in preparation various high-energy materials. The majority energy-rich substances incorporating subunit exhibit high thermal stability, good detonation performance and low sensitivity to mechanical stimuli defines their practical usability. this review, main achievements on synthesis tetrazine-based reported last decade are summarized. Potential applications presented compounds especially emphasized.

Language: Английский

Citations

28
Thiophene‐containing compounds with antimicrobial activity DOI
Gheorghe Roman

Archiv der Pharmazie, Journal Year: 2022, Volume and Issue: 355(6)

Published: March 15, 2022

Thiophene, as a member of the group five-membered heterocycles containing one heteroatom, is simplest heterocyclic systems. Many synthetic strategies allow accurate positioning various functionalities onto thiophene ring. This review provides comprehensive, systematic and detailed account developments in field antimicrobial compounds featuring at least ring their structure, over last decade.

Language: Английский

Citations

27
Push–Pull Derivatives Based on 2,4′-Biphenylene Linker with Quinoxaline, [1,2,5]Oxadiazolo[3,4-B]Pyrazine and [1,2,5]Thiadiazolo[3,4-B]Pyrazine Electron Withdrawing Parts DOI Creative Commons
Egor V. Verbitskiy,

Pascal Le Poul,

Filip Bureš

et al.

Molecules, Journal Year: 2022, Volume and Issue: 27(13), P. 4250 - 4250

Published: June 30, 2022

A series of novel V-shaped quinoxaline, [1,2,5]oxadiazolo[3,4-

Language: Английский

Citations

23
Synthesis, in vitro biological analysis and molecular docking studies of new thiadiazole-based thiourea derivatives as dual inhibitors of a-amylase and a-glucosidase DOI Creative Commons

Imran Khan,

Wajid Rehman, Fazal Rahim

et al.

Arabian Journal of Chemistry, Journal Year: 2023, Volume and Issue: 16(9), P. 105078 - 105078

Published: June 17, 2023

Diabetes mellitus is a syndrome that caused due to the imbalance of insulin production in body. In present study we have synthesized class fifteen compounds (1–15) based on thiadiazole-bearing thiourea were assessed for vitro alpha-amylase and alpha-glucosidase inhibitory potentials against standard drug acarbose. this series, all scaffolds recognized as inhibitors both targeted enzymes, α-amylase having varied range from IC50 values = 35.70 ± 0.70 µM 1.30 0.05 acarbose (10.30 0.20 µM) while α-glucosidase 37.60 0.80 2.20 0.10 (9.80 µM). Among nine such 4, 6, 7, 9, 8, 11, 12, 14 15 showed excellent activity a-amylase a-glucosidase found many folds more potent than drugs change nature number/s substituent along entire skeleton. A molecular docking was conducted active understand binding modes synthetic analogs how they show interaction with part enzymes. To confirm structure different spectroscopic techniques will be used like NMR HREI-MS.

Language: Английский

Citations

15