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(searched for: doi:10.5155/eurjchem.8.1.76-81.1542)
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Published: 5 February 2021
Antibiotics, Volume 10; doi:10.3390/antibiotics10020162

Abstract:
Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a–d, pyridine-2-one 3–10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis. All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens. The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity. These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 18.17–23.87 µM, and of DHFR, with IC50 values of 4.33–5.54 µM; their potency is near to that of the positive controls. Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes. Finally, molecular docking and some AMED studies were performed.
, Awatef A. Farag, Abeer M. Ali, , Ahmed A. Askar, Doaa M. Elsisi,
Published: 1 November 2020
Bioorganic Chemistry, Volume 104; doi:10.1016/j.bioorg.2020.104164

The publisher has not yet granted permission to display this abstract.
, , Abeer El-Khalafawy, Abeer H. Makhlouf, Ahmed.A. Askar, Yousry A. Ammar
Published: 1 March 2020
Bioorganic Chemistry, Volume 96; doi:10.1016/j.bioorg.2020.103619

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, , , Abeer El-Khalafawy, Abeer H. Makhlouf
European Journal of Medicinal Chemistry, Volume 188; doi:10.1016/j.ejmech.2019.111977

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, Marwa A. M. Sh. El-Sharief, Mohamed A. Salem, Ahmed M. Sh. El-Sharief
Published: 10 January 2020
Synthetic Communications, Volume 50, pp 621-648; doi:10.1080/00397911.2019.1700524

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, , Ahmed M.Sh. El-Sharief, Nermien M. Sabry, Ziad Moussa, Shahenda M. El-Messery, Ahmed R. Elsheakh, , Mardia T. El Sayed
Published: 1 June 2019
Bioorganic Chemistry, Volume 87, pp 679-687; doi:10.1016/j.bioorg.2019.03.075

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Zeid Hassan Abood, Hussein Ali Qabel, Hayder Raheem Ali
Journal of Physics: Conference Series, Volume 1032; doi:10.1088/1742-6596/1032/1/012058

Abstract:
Diazotization of 2-aminobenzothiazole 1 through using sulfuric acid and sodium nitrite resulted in the formation of diazonium salt which reacted with alkaline solution of salicylaldehyde to produce azo-aldehyde derivative of benzothiazole 2. The resulting aldehyde 2 was condensed with the primary aromatic amines involving (4-nitroaniline, 3-nitroaniline, 4-hydroxyaniline, 4-methoxyaniline, 2-methoxyaniline, 4-bromoaniline, 4-chloroaniline and 2,4- dichloroaniline) using microwave irradiation method in absolute ethanol to produce eight imines of benzothiazole 3a-h, respectively. The imine compounds 3a-h have been treated with L-alanine using microwave irradiation in tetrahydrofuran afforded eight new imidazolidines 4a-h containing benzothiazole moiety, respectively. Preliminary antibacterial activity of the target compounds was investigated in vitro using two kinds of bacteria, Escherichia coli (Gram-negative) and Staphylococcus aurous (Gram-positive). The results showed that the newly prepared imidazolidines (compounds 4c, 4d, 4f, 4g, and 4h) exhibited greater activities than gentamycin against Gram-positive bacteria. On the other hand, compounds 4c and 4f were also showed better activities against Gram-negative bacteria when compared with that of the control drug.
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