Saeed Karima - Academia.edu (original) (raw)
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![Research paper thumbnail of 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](https://attachments.academia-assets.com/80890336/thumbnails/1.jpg)
](Scientific Reports
In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-ami... more 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 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 ...
Pharmaceutical Sciences
Biological activity of Boswellia extract (BE) has been attributed to its main active ingredients;... more Biological activity of Boswellia extract (BE) has been attributed to its main active ingredients; i.e. Boswellic acids (BAs). BE/BAs possess a promising therapeutic potential in neurodegenerative disorders; including Alzheimer's disease (AD). The multifactorial nature of AD pathophysiology necessitates the development of the disease-modifying agents (DMA). Recent multi-targeting approaches for the DMAs development have brought more attention to the plant-derived compounds regarding their better human compatibility because of their biologic origin. This review addresses the current knowledge on the anti-AD activity of BE/BAs based on the available in silico, in vitro, in vivo studies and clinical trials. The contribution of BE/BAs in inflammatory pathways, Tau and β-amyloid proteins, microtubule functions, oxidative stress, cholinesterase and diabetes/insulin pathways involved in AD have been discussed. BAs efficacy in different AD-related pathways has been confirmed in vitro and...
Future Oncology
Thyroid cancer, as the most prevalent endocrine malignancy, comprises nearly 1% of all cancers in... more Thyroid cancer, as the most prevalent endocrine malignancy, comprises nearly 1% of all cancers in the world. The metastatic propagation of thyroid cancer is under the control of a number of modulating processes and factors such as signaling pathways and their components, cell division regulators, metabolic reprogramming factors, extracellular matrix remodelers, epithelial to mesenchymal transition modulators, epigenetic mechanisms, hypoxia and cytokines. Identifying the exact molecular mechanisms of these dysregulated processes could help to discover the key targets for therapeutic purposes and utilizing them as diagnostic, prognostic and predictors of the clinical course of patients. In this review article, we describe different aspects of thyroid cancer metastasis by focusing on defective genes and pathways involved in its metastatic spread.
European Journal of Medicinal Chemistry
International Journal of Biological Macromolecules
BioImpacts
Introduction: Beta-Boswellic acid (BBA) is a pentacyclic terpene which has been obtained from fra... more Introduction: Beta-Boswellic acid (BBA) is a pentacyclic terpene which has been obtained from frankincense and its beneficial effects on neurodegenerative disorders such as Alzheimer’s disease (AD) have been addressed. Methods: In the present study, thermodynamic and kinetic aspects of BBA interaction with Tau protein as one of the important proteins involved in AD in the absence and presence of glucose has been investigated using surface plasmon resonance (SPR) method. Tau protein was immobilized onto the carboxy methyl dextran chip and its binding interactions with BBA were studied at physiological pH at various temperatures. Glucose interference with these interactions was also investigated. Results: Results showed that BBA forms a stable complex with Tau (KD=8.45×10-7 M) at 298 K. Molecular modeling analysis showed a hydrophobic interaction between BBA and HVPGGG segment of R2 and R4 repeated domains of Tau. Conclusion: The binding affinity increased by temperature enhancement, ...
Scientific Reports
In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-ami... more 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 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 ...
Pharmaceutical Sciences
Biological activity of Boswellia extract (BE) has been attributed to its main active ingredients;... more Biological activity of Boswellia extract (BE) has been attributed to its main active ingredients; i.e. Boswellic acids (BAs). BE/BAs possess a promising therapeutic potential in neurodegenerative disorders; including Alzheimer's disease (AD). The multifactorial nature of AD pathophysiology necessitates the development of the disease-modifying agents (DMA). Recent multi-targeting approaches for the DMAs development have brought more attention to the plant-derived compounds regarding their better human compatibility because of their biologic origin. This review addresses the current knowledge on the anti-AD activity of BE/BAs based on the available in silico, in vitro, in vivo studies and clinical trials. The contribution of BE/BAs in inflammatory pathways, Tau and β-amyloid proteins, microtubule functions, oxidative stress, cholinesterase and diabetes/insulin pathways involved in AD have been discussed. BAs efficacy in different AD-related pathways has been confirmed in vitro and...
Future Oncology
Thyroid cancer, as the most prevalent endocrine malignancy, comprises nearly 1% of all cancers in... more Thyroid cancer, as the most prevalent endocrine malignancy, comprises nearly 1% of all cancers in the world. The metastatic propagation of thyroid cancer is under the control of a number of modulating processes and factors such as signaling pathways and their components, cell division regulators, metabolic reprogramming factors, extracellular matrix remodelers, epithelial to mesenchymal transition modulators, epigenetic mechanisms, hypoxia and cytokines. Identifying the exact molecular mechanisms of these dysregulated processes could help to discover the key targets for therapeutic purposes and utilizing them as diagnostic, prognostic and predictors of the clinical course of patients. In this review article, we describe different aspects of thyroid cancer metastasis by focusing on defective genes and pathways involved in its metastatic spread.
European Journal of Medicinal Chemistry
International Journal of Biological Macromolecules
BioImpacts
Introduction: Beta-Boswellic acid (BBA) is a pentacyclic terpene which has been obtained from fra... more Introduction: Beta-Boswellic acid (BBA) is a pentacyclic terpene which has been obtained from frankincense and its beneficial effects on neurodegenerative disorders such as Alzheimer’s disease (AD) have been addressed. Methods: In the present study, thermodynamic and kinetic aspects of BBA interaction with Tau protein as one of the important proteins involved in AD in the absence and presence of glucose has been investigated using surface plasmon resonance (SPR) method. Tau protein was immobilized onto the carboxy methyl dextran chip and its binding interactions with BBA were studied at physiological pH at various temperatures. Glucose interference with these interactions was also investigated. Results: Results showed that BBA forms a stable complex with Tau (KD=8.45×10-7 M) at 298 K. Molecular modeling analysis showed a hydrophobic interaction between BBA and HVPGGG segment of R2 and R4 repeated domains of Tau. Conclusion: The binding affinity increased by temperature enhancement, ...