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Synthesis and Anti-inflammatory Evaluation of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-a]Pyrimidine, Imidazo[1,2-b]Pyrazole and Pyrazolo[5,1-b]Quinazoline Derivatives Containing Indane Moiety
被引:21
作者:
El-Sayed, Elsherbiny H.
[1
]
Mohamed, Khaled S.
[2
]
机构:
[1] Port Said Univ, Fac Sci, Dept Chem, Port Said 42526, Egypt
[2] Higher Inst Engn & Technol, Engn Chem Dept, New Damietta, Egypt
关键词:
Anti-inflammatory activity;
pyrazole;
pyrimidine;
pyrazolo[15-a]pyrimidine;
CARBONIC-ANHYDRASE INHIBITORS;
ANTIMICROBIAL ACTIVITY;
BIOLOGICAL EVALUATION;
SELECTIVE INHIBITORS;
KINASE INHIBITORS;
PYRAZOLOPYRIMIDINES;
POTENT;
SAR;
IDENTIFICATION;
OPTIMIZATION;
D O I:
10.1080/10406638.2019.1653941
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
A new series of pyrazole, pyrimidine, pyrazolo[1,5-a]pyrimidine, imidazo[1,2-b]pyrazole and pyrazolo[5,1-b]quinazoline derivatives containing indane moiety are prepared by using N-(2,3-dihydro-1H-inden-5-yl)carbonohydrazonoyl dicyanide (2) as starting material to synthetic different heterocyclic compounds (3-11) by the reaction with different bifuncation reagents. Moreover, 4-((2,3-dihydro-1H-inden-5-yl)diazenyl)-1H-pyrazole-3,5-diamine (3) was taken as a precursor to prepare different pyrazolo[1,5-a]pyrimidine derivatives (12-20). The structures of newly synthesized compounds were confirmed on the basis of their IR, 1H NMR, 13C NMR, and mass spectral data. All compounds were evaluated as anti-inflammatory activity by using carrageenan-induced rat paw edema test. In comparison to the standard drug diclofenac sodium, compounds 3, 7, 9, and 11 exhibited potent activity than standard drug. The compounds 2 and 8 showed the most significant anti- anti-inflammatory with 64.83 and 63.95% inhibition of edema.
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页码:1077 / 1093
页数:17
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