SYNTHESIS AND ANTI-INFLAMMATORY ACTIVITY OF NEW (5 (SUBSTITUTED PHENYL)-2,3-DIHYDRO-3-PHENYLPYRAZOL-1-YL) (PYRIDIN-3-YL) METHANONE DERIVATIVES

被引：0

作者：

Tabassum, Ruby ^{[1
]}

Mohammad, Noor ^{[1
]}

Kumari, Poonam ^{[1
]}

Bharatia, Rakesh ^{[2
]}

Srivastava, Neha ^{[1
]}

Yogi, Bhumika ^{[1
]}

Sinha, Anshuman ^{[2
]}

Gupta, Sujeet K. ^{[1
]}

机构：

[1] Hygia Inst Pharmaceut Educ & Res, Dept Pharmaceut Chem, Lucknow, Uttar Pradesh, India

[2] Hygia Inst Pharmaceut Educ & Res, Dept Pharmacol, Lucknow, Uttar Pradesh, India

来源：

INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY | 2017年 / 27卷 / 01期

关键词：

Pyrazolines; Anti-inflammatory; Chalcone; Carrageenan-induced paw edema model; PYRAZOLE DERIVATIVES; ANTIMICROBIAL EVALUATION; ANTIFUNGAL ACTIVITY; ANTIDEPRESSANT; 3-METHYL;

D O I：

暂无

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of 5 (substituted phenyl)-2,3-dihydro-3-phenylpyrazol-1-yl) (pyridin-3-yl) methanone derivatives (2a-h) has been synthesized starting from acetophenone. All the synthesized compounds were evaluated for anti-inflammatory activity using carrageenan-induced inflammation in rat paw edema model. Substituted chalcone derivatives (1a-h) on treatment with isoniazid in the presence of glacial acetic acid afforded corresponding pyrazoline derivatives (2a-h). The structure of the final analogs has been confirmed on the basis of elemental analysis, Fourier transform infrared (FTIR), nuclear magnetic resonance (H-1 NMR), and mass spectra. Among all synthesized compounds, compounds 2c and 2b were found to be most potent in comparison with standard diclofenac. In addition, the compounds 2c and 2b were found to be less ulcerogenic.

引用

页码：107 / 112

页数：6

共 27 条

[1] Synthesis of novel pyrazole derivatives and evaluation of their antidepressant and anticonvulsant activities
Abdel-Aziz, Mohamed
Abuo-Rahma, Gamal El-Din A.
Hassan, Alaa A.
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (09) : 3480 - 3487
[2] Amir M, 2005, INDIAN J CHEM B, V44, P2532
[3] [Anonymous], 2013, ORG MED CHEM LETT
[4] Arora R., 2012, CURR RES CHEM, V4, P76, DOI [DOI 10.3923/CRC.2012.76.87, 10.3923/crc.2012.76.87]
[5] Synthesis and Anti-inflammatory Activity of Some Novel Pyrazole Derivatives of Gallic Acid
Arunkumar, S.
Ilango, K.
Manikandan, R. S.
Ramalakshmi, N.
[J]. E-JOURNAL OF CHEMISTRY, 2009, 6 : S123 - S128
[6] NSAID-induced gastrointestinal damage - Epidemiology, risk and prevention, with an evaluation of the role of misoprostol. An Asia-Pacific perspective and consensus
Champion, GD
Feng, PH
Azuma, T
Caughey, DE
Chan, KH
Kashiwazaki, S
Liu, HC
Nasution, AR
Nobunaga, M
Prichanond, S
Torralba, TP
Udom, V
Utis, D
Wang, SR
Wong, WS
Yang, DJ
Yoo, MC
[J]. DRUGS, 1997, 53 (01) : 6 - 19
[7] Chandrashekhar K.B., 2013, J PHARM SCI INNOV, V2, P55
[8] Synthesis and selective inhibitory activity of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives against monoamine oxidase
Chimenti, F
Bolasco, A
Manna, F
Secci, D
Chimenti, P
Befani, O
Turini, P
Giovannini, V
Mondovì, B
Cirilli, R
La Torre, F
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (08) : 2071 - 2074
[9] Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives
Hassan, Seham Y.
[J]. MOLECULES, 2013, 18 (03) : 2683 - 2711
[10] The use of NSAIDs in rheumatic disorders 2005: A global perspective
Kean W.F.
Buchanan W.W.
[J]. InflammoPharmacology, 2005, 13 (4) : 343 - 370

← 1 2 3 →