共 53 条
1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities
被引:70
作者:

Abuo-Rahma, Gamal El-Din A. A.
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h-index: 0
机构:
Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt

Abdel-Aziz, Mohamed
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机构:
Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt

Beshr, Eman A. M.
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Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt

Ali, Taha F. S.
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Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt
机构:
[1] Minia Univ, Dept Med Chem, Fac Pharm, Al Minya 61519, Egypt
关键词:
1,2,4-Triazole;
Nitric oxide donors;
Anti-inflammatory;
Ulcerogenicity;
Antiproliferative;
IN-VITRO;
BIOLOGICAL EVALUATION;
ANTITUMOR-ACTIVITY;
MUCOSAL DAMAGE;
DERIVATIVES;
DESIGN;
CYTOTOXICITY;
ULCEROGENICITY;
PATHOGENESIS;
INJURY;
D O I:
10.1016/j.ejmech.2013.11.006
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
A series of novel nitric oxide (NO) donating triazole/oxime hybrids was prepared and evaluated for their anti-inflammatory activity and antiproliferative activity. Most of the tested compounds showed significant anti-inflammatory activity using carrageenan-induced rat paw edema method compared to indomethacin. Calculation of the ulcer indices and histopathological investigation indicated that the prepared NO-donating oximes exhibited less ulcerogenicity compared to their ketone intermediates and indomethacin. The NO-donating oximes 7i and 7k achieved remarkable cell growth inhibition activity against most of the tested cell lines. Compound 7k was found to be with high selectivity against CNS subpanel with selectivity ratio of 11.99 at GI(50) level. (C) 2013 Elsevier Masson SAS. All rights reserved.
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页码:185 / 198
页数:14
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