Design, synthesis and A-glucosidase inhibitors evaluation of novel barbiturates based on carbohydrate

2022 ◽  
Author(s):  
Ali Jabbar Radhi ◽  
Ezzat H. Zimam ◽  
Emad Abbas Jaffar Al-Mulla
Keyword(s):  
Design Synthesis ◽  
Glucosidase Inhibitors

scholarly journals Design, synthesis, molecular docking, and in vitro α-glucosidase inhibitory activities of novel 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines against yeast and rat α-glucosidase

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Fariba Peytam ◽  
Ghazaleh Takalloobanafshi ◽  
Toktam Saadattalab ◽  
Maryam Norouzbahari ◽  
Zahra Emamgholipour ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Study ◽  
Rat Small Intestine ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Mild Conditions ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities

AbstractIn an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a–ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α-azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their inhibitory activities against yeast α-glucosidase enzyme were investigated. Showing IC50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which encouraged us to perform further studies on α-glucosidase enzymes obtained from rat as a mammal source. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines, compound 3k exhibited the highest potency against both Saccharomyces cerevisiae α-glucosidase (IC50 = 16.4 ± 0.36 μM) and rat small intestine α-glucosidase (IC50 = 45.0 ± 8.2 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.

Design, Synthesis, and Biological Evaluation of New Indole-Acrylamide-1,2,3-Triazole Derivatives as Potential α-Glucosidase Inhibitors

2020 ◽  
pp. 1-9
Author(s):  
Seyed Esmaeil Sadat-Ebrahimi ◽  
Hiva Babania ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mohammad Sadegh Asgari ◽  
Somayeh Mojtabavi ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Triazole Derivatives ◽  
Glucosidase Inhibitors ◽  
Synthesis And Biological Evaluation

New acridine-9-carboxamide linked to 1,2,3-triazole-N-phenylacetamide derivatives as potent α-glucosidase inhibitors: design, synthesis, in vitro, and in silico biological evaluations

2020 ◽  
Vol 29 (10) ◽  
pp. 1836-1845
Author(s):  
Nima Sepehri ◽  
Nafise Asemanipoor ◽  
Seyed Ali Mousavianfard ◽  
Seyedhamid Hoseini ◽  
Mohammad Ali Faramarzi ◽  
...  
Keyword(s):  
In Silico ◽  
Design Synthesis ◽  
Glucosidase Inhibitors

Design, synthesis, and biological evaluation of quinazoline derivatives as α-glucosidase inhibitors

2014 ◽  
Vol 24 (5) ◽  
pp. 2227-2237 ◽  
Author(s):  
Venkateshwarlu Gurram ◽  
Ramesh Garlapati ◽  
Chiranjeevi Thulluri ◽  
Nagaraju Madala ◽  
Kumara Swamy Kasani ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Glucosidase Inhibitors ◽  
Quinazoline Derivatives ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis, Molecular Docking, and Kinetic Study of 3-Amino-2,4-Diarylbenzo[4,5]Imidazo[1,2-a]Pyrimidines as Novel, Potent Α-Glucosidase Inhibitor

2021 ◽  
Author(s):  
Fariba Peytam ◽  
Ghazaleh Takalloobanafshi ◽  
Toktam Saadattalab ◽  
Zahra Emamgholipour ◽  
Maryam Norouzbahari ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Kinetic Study ◽  
Docking Study ◽  
Type Ii Diabetes Mellitus ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Glucosidase Inhibitors

Abstract In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a-ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α-azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their α-glucosidase inhibitory activities were investigated. Showing IC50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which may provide new drug candidates in the treatment of type II diabetes mellitus. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines, compound 3k exhibited the highest potency against α-glucosidase (IC50 = 16.4 ± 0.36 μM) which was 45.7 times more potent than acarbose as standard inhibitor (IC50 = 750.0 ± 1.5 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.

New thiosemicarbazide-1,2,3-triazole hybrids as potent α-glucosidase inhibitors: Design, synthesis, and biological evaluation

2019 ◽  
Vol 1192 ◽  
pp. 192-200 ◽  
Author(s):  
Zohreh Bakherad ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Hojjat Sadeghi-Aliabadi ◽  
Sepideh Rezaei ◽  
Afshin Fassihi ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Glucosidase Inhibitors ◽  
Synthesis And Biological Evaluation

Design, synthesis of new phenyl acetylene and isoxazole analogues of arjunolic acid as potent tyrosinase and alpha glucosidase inhibitors

2021 ◽  
pp. 1-6
Author(s):  
Bolatito Eunice Olanipekun ◽  
Mangala Gowri Ponnapalli ◽  
Hemendra Kumar Patel ◽  
Kiran Munipalle ◽  
Karimulla Shaik
Keyword(s):  
Design Synthesis ◽  
Phenyl Acetylene ◽  
Glucosidase Inhibitors ◽  
Arjunolic Acid ◽  
Alpha Glucosidase
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