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Hantzsch Reaction Approach for Determination of Teicoplanin and Vancomycin in Real Human Plasma: Application to Pharmaceutical Preparations and to Synthetic Mixture with Rifampicin for Drug-Resistant Strain of Staphylococcus aureus

Research Abstract
Teicoplanin (TEIC) and vancomycin hydrochloride (VAN) are glycopeptide antimicrobial drugs against methicillin-resistant Staphylococcus aureus and Gram-positive organisms. So, simple, quick, cost-effective and ultrasensitive spectrofluorimetric method was developed and bio-analytically validated for assay of TEIC and VAN. The proposed method is based on the reaction of acetylacetone with primary amine moiety in the presence of formaldehyde producing highly fluorogenic product measured at 485 nm (λex at 420 nm). The calibration range was constructed from (50–400 ng mL−1) and (70–800 ng mL−1) for TEIC and VAN, respectively. The presented method exhibited low LOD (7.04 and 3.55 ng mL−1) and LOQ (21.33 and 10.77 ng mL−1) values for TEIC and VAN, respectively. The presented method was effectively applied to determine TEIC and VAN in real human plasma with percentage of recovery ranged from 95.57 ± 2.06% to 97.43 ± 1.66% for the studied drugs. Also, the developed method was applied for the first time to study synthetic mixtures of the studied drugs with rifampicin (RIF), as a combination therapy to treat drug-resistant strains of Staphylococcus aureus without interferences from RIF. The synthetic mixtures of TEIC or VAN with RIF were prepared in three different ratios in order to measure the stability of the studied drugs TEIC or VAN in presence of RIF in pure forms and human plasma.
Research Authors
Mostafa A. Marzouq, Baher I. Salman, Samiha A. Hussein, Marwa F.B. Ali
Research Journal
Microchemical Journal
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 147
Research Website
https://doi.org/10.1016/j.microc.2019.03.002
Research Year
2019

Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

Research Abstract
The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.
Research Authors
Abdelrahman M. Mahmoud, Samia G. Abdel-Moty, Ola I. A Salem,
Abdel-Alim M. Abdel-Alim and Ahmed S. Aboraia
Research Journal
Journal of Advances in Chemistry
Research Publisher
NULL
Research Rank
1
Research Vol
11(5):
Research Website
http://cirjac.com/ojs/index.php/jac/article/view/504
Research Year
2015

Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

Research Abstract
The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.
Research Authors
Abdelrahman M. Mahmoud, Samia G. Abdel-Moty, Ola I. A Salem,
Abdel-Alim M. Abdel-Alim and Ahmed S. Aboraia
Research Journal
Journal of Advances in Chemistry
Research Member
Abdul Aleem Muhammad Abdul Aleem Abul Qasim
Research Publisher
NULL
Research Rank
1
Research Vol
11(5):
Research Website
http://cirjac.com/ojs/index.php/jac/article/view/504
Research Year
2015

Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

Research Abstract
The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.
Research Authors
Abdelrahman M. Mahmoud, Samia G. Abdel-Moty, Ola I. A Salem,
Abdel-Alim M. Abdel-Alim and Ahmed S. Aboraia
Research Journal
Journal of Advances in Chemistry
Research Publisher
NULL
Research Rank
1
Research Vol
11(5):
Research Website
http://cirjac.com/ojs/index.php/jac/article/view/504
Research Year
2015

Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

Research Abstract
The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.
Research Authors
Abdelrahman M. Mahmoud, Samia G. Abdel-Moty, Ola I. A Salem,
Abdel-Alim M. Abdel-Alim and Ahmed S. Aboraia
Research Journal
Journal of Advances in Chemistry
Research Publisher
NULL
Research Rank
1
Research Vol
11(5):
Research Website
http://cirjac.com/ojs/index.php/jac/article/view/504
Research Year
2015

Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

Research Abstract
The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.
Research Authors
Abdelrahman M. Mahmoud, Samia G. Abdel-Moty, Ola I. A Salem,
Abdel-Alim M. Abdel-Alim and Ahmed S. Aboraia
Research Journal
Journal of Advances in Chemistry
Research Publisher
NULL
Research Rank
1
Research Vol
11(5):
Research Website
http://cirjac.com/ojs/index.php/jac/article/view/504
Research Year
2015

A Hybrid In Silico/In Vitro Target Fishing Study to Mine
Novel Targets of Urolithin A and B: A Step Towards a Better
Comprehension of Their Estrogenicity

Research Abstract
NULL
Research Authors
Luca Dellafiora,* Marco Milioli, Angela Falco, Margherita Interlandi,
Abdelrahman Mohamed, Martin Frotscher, Benedetta Riccardi, Paola Puccini,
Daniele Del Rio, Gianni Galaverna, and Chiara Dall’Asta
Research Journal
Journal of Molecular Nutrition & Food Research.
Research Publisher
NULL
Research Rank
1
Research Vol
NULL
Research Website
NULL
Research Year
2020

Synthesis and antimicrobial evaluation of some new thiazoline and
thiazolidinone derivatives incorporating [1, 2, 4] triazolo [1, 5-a]
benzimidazole.

Research Abstract
NULL
Research Authors
Abdelrahman Mohamed Mahmoud, Ola Ibrahim Abdel Razek, Samia
Galal Abdel-Moty, and Abdel-Alim Mohammed Abdel-Alim.
Research Journal
Indian Journal of Pharmaceutical Sciences
Research Publisher
NULL
Research Rank
1
Research Vol
NULL
Research Website
NULL
Research Year
2013

Synthesis and antimicrobial evaluation of some new thiazoline and
thiazolidinone derivatives incorporating [1, 2, 4] triazolo [1, 5-a]
benzimidazole.

Research Abstract
NULL
Research Authors
Abdelrahman Mohamed Mahmoud, Ola Ibrahim Abdel Razek, Samia
Galal Abdel-Moty, and Abdel-Alim Mohammed Abdel-Alim.
Research Journal
Indian Journal of Pharmaceutical Sciences
Research Member
Abdul Aleem Muhammad Abdul Aleem Abul Qasim
Research Publisher
NULL
Research Rank
1
Research Vol
NULL
Research Website
NULL
Research Year
2013

Synthesis and antimicrobial evaluation of some new thiazoline and
thiazolidinone derivatives incorporating [1, 2, 4] triazolo [1, 5-a]
benzimidazole.

Research Abstract
NULL
Research Authors
Abdelrahman Mohamed Mahmoud, Ola Ibrahim Abdel Razek, Samia
Galal Abdel-Moty, and Abdel-Alim Mohammed Abdel-Alim.
Research Journal
Indian Journal of Pharmaceutical Sciences
Research Publisher
NULL
Research Rank
1
Research Vol
NULL
Research Website
NULL
Research Year
2013
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