Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents

被引：48

作者：

Nossier, Eman S. ^{[1
]}

Fahmy, Hoda H. ^{[2
]}

Khalifa, Nagy M. ^{[2
,3
]}

El-Eraky, Wafaa I. ^{[4
]}

Baset, Marawan A. ^{[4
]}

机构：

[1] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Chem, Cairo 11754, Egypt

[2] Natl Res Ctr, Pharmaceut & Drug Ind Div, Dept Therapeut Chem, Giza 12622, Egypt

[3] King Saud Univ, Coll Pharm, Pharmaceut Chem Dept, DEDC, Riyadh 11451, Saudi Arabia

[4] Natl Res Ctr, Pharmacol Dept, Cairo 12622, Egypt

来源：

MOLECULES | 2017年 / 22卷 / 04期

关键词：

1,3-diaryl pyrazole derivatives; anti-inflammatory activity; synthesis; MOLECULAR DOCKING; BIOLOGICAL EVALUATION; IN-VITRO; ACID-DERIVATIVES; COX-2; INHIBITORS; ANTICANCER; CYCLOOXYGENASE-2; ANTIBACTERIAL; MOIETY; CANDIDATES;

D O I：

10.3390/molecules22040512

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 +/- 1.92 and 85.78 +/- 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.

引用

页数：16

共 33 条

[31]

WINTER CA, 1962, P SOC EXP BIOL MED, V111, P544

[32] The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives [J].

Yu, Li-Gang ;

Ni, Teng-Feng ;

Gao, Wei ;

He, Yuan ;

Wang, Ying-Ying ;

Cui, Hai-Wei ;

Yang, Cai-Guang ;

Qiu, Wen-Wei .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 90 :10-20

[33] Synthesis, in vitro and in vivo antitumor activity of pyrazole-fused 23-hydroxybetulinic acid derivatives [J].

Zhang, Hengyuan ;

Zhu, Peiqing ;

Liu, Jie ;

Lin, Yan ;

Yao, Hequan ;

Jiang, Jieyun ;

Ye, Wencai ;

Wu, Xiaoming ;

Xu, Jinyi .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 25 (03) :728-732

← 1 2 3 4 →