Cytochrome P450 3A4 suppression by epimedium and active compound kaempferol leads to synergistic anti-inflammatory effect with corticosteroid
Discussion: Inhibition of CYP3A4 function by epimedium and its active compound kaempferol leads to enhancement of CS anti-inflammatory effect. (Source: Frontiers in Pharmacology)
Source: Frontiers in Pharmacology - January 30, 2023 Category: Drugs & Pharmacology Source Type: research
Design and evaluation of dibenzoazepine-tetrahydroisoquinoline hybrids as potential P-glycoprotein inhibitors against multidrug resistant K562/A02 cells
In this study, fourteen novel dibenzoazepine-tetrahydroisoquinoline hybrids were prepared as potential P-gp inhibitors to surmount MDR caused by P-gp. Amongst them, 8a displayed the most potent inhibition effect on P-gp, thus effectively reversing P-gp-mediated drug resistance with a reversal fold (RF) value of 93.17 in K562/A02 cells. Excitingly, the EC50 value of 8a on MDR reversing effect was 48.74 nM, which was nearly two thousand-fold lower than its IC50 value (95.94 μM) for intrinsic cytotoxicity on K562/A02 cells. Further investigation showed that 8a exerted the MDR reversal effect through impairing P-gp function r...
Source: European Journal of Medicinal Chemistry - January 28, 2023 Category: Chemistry Authors: Chunyu Jiang Ting Pan Yunxiang Jiang Zhiyu Zhang Meifeng Zeng Shuang Sun Zheng Li Yiqing Wu Jingying Qiu Mingshan Niu Xiaoke Gu Source Type: research
Design and evaluation of dibenzoazepine-tetrahydroisoquinoline hybrids as potential P-glycoprotein inhibitors against multidrug resistant K562/A02 cells
In this study, fourteen novel dibenzoazepine-tetrahydroisoquinoline hybrids were prepared as potential P-gp inhibitors to surmount MDR caused by P-gp. Amongst them, 8a displayed the most potent inhibition effect on P-gp, thus effectively reversing P-gp-mediated drug resistance with a reversal fold (RF) value of 93.17 in K562/A02 cells. Excitingly, the EC50 value of 8a on MDR reversing effect was 48.74 nM, which was nearly two thousand-fold lower than its IC50 value (95.94 μM) for intrinsic cytotoxicity on K562/A02 cells. Further investigation showed that 8a exerted the MDR reversal effect through impairing P-gp function r...
Source: European Journal of Medicinal Chemistry - January 28, 2023 Category: Chemistry Authors: Chunyu Jiang Ting Pan Yunxiang Jiang Zhiyu Zhang Meifeng Zeng Shuang Sun Zheng Li Yiqing Wu Jingying Qiu Mingshan Niu Xiaoke Gu Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
Design, Synthesis, Characterization, and Analysis of Antimicrobial Property of Novel Benzophenone Fused Azetidinone Derivatives through In Vitro and In Silico Approach
Curr Issues Mol Biol. 2022 Dec 23;45(1):92-109. doi: 10.3390/cimb45010007.ABSTRACTA sequence of novel 2-(4-benzoyl-2-methyl-phenoxy)-N-(3-chloro-2-oxo-4-phenyl-azetidin-1-yl)-acetamide analogues 9(a-n) were synthesized by multistep synthesis. The newly synthesized compounds were well characterized, and their antimicrobial activities were carried out by disc diffusion and broth dilution methods. Further, all the novel series of compounds (9a-n), were tested against a variety of bacterial and fungal strains in comparison to Ketoconazole, Chloramphenicol, and Amoxicillin as standard drugs, respectively. Compounds...
Source: Current Issues in Molecular Biology - January 20, 2023 Category: Molecular Biology Authors: Lakshmi Ranganatha Venkataravanappa Mahima Jyothi Hussien Ahmed Khamees Ekaterina Silina Victor Stupin Raghu Ram Achar Mohammed Al-Ghorbani Shaukath Ara Khanum Source Type: research
