Synthesis and Evaluation of Anti-inflammatory and Analgesic Activities of New 1,2,4-triazole Derivatives

被引:33
作者
Ahmadi, Fatemeh [1 ,3 ,4 ]
Ghayahbashi, Mohsen Rezayan [2 ,3 ,4 ]
Sharifzadeh, Mohammad [2 ]
Alipoiur, Eskandar [1 ]
Ostad, Seyed Nasser [2 ]
Vosooghi, Mohsen [3 ,4 ]
Khademi, Hamid Reza [2 ,3 ,4 ]
Amini, Mohsen [3 ,4 ]
机构
[1] Islamic Azad Univ, Fac Chem, North Tehran Branch, Tehran, Iran
[2] Univ Tehran Med Sci, Fac Pharm, Dept Pharmacol & Toxicol, Tehran, Iran
[3] Univ Tehran Med Sci, Fac Pharm & Drug Design, Dept Med Chem, Tehran, Iran
[4] Univ Tehran Med Sci, Res Dev Ctr, Tehran, Iran
关键词
Anti-inflammatory activity; analgesic activity; 1,2,4-tiazole derivatives; diarylheterocyclic compounds; DESIGN; ANALOGS;
D O I
10.2174/1573406410666140613154507
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, the synthesis, anti-inflammatory and analgesic activities of eight new 5-thioalkyl-1,3-diaryl-1,2,4-triazole derivatives were reported. For the anti-inflammatory study, the carrageenan-induced rat paw edema model was used. The test compounds in 50 mg/kg and 100 mg/kg were injected as IP and paw edema was determined. The results showed that some of the compounds have good activity compared to the references drug, indomethacin. For analgesic activity, the test compounds were studied using the in Tail-flick test model in 50 and 100 mg/kg as IP injections. Their analgesic activities were determined after 30 min via latency time assay. Statistical analysis showed that all test compounds have antinociceptive activity in the range of 24% -47% as compared to the control with a dose of 50 mg/kg. However, all tested compounds have analgesic activity lower than the standard drug, morphine.
引用
收藏
页码:69 / 76
页数:8
相关论文
共 23 条
[1]   Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity [J].
Abdel-Megeed, Ashraf M. ;
Abdel-Rahman, Hamdy A. ;
Alkaramany, Gamal-Eldien S. ;
El-Gendy, Mahmoud A. .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (01) :117-123
[2]  
Alam MJ, 2013, LETT DRUG DES DISCOV, V10, P776
[3]   Synthesis, cyclooxygenase inhibitory effects, and molecular modeling study of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and-2-alkylsulfonyl-1H-imidazole derivatives [J].
Assadieskandar, Amir ;
Amirhamzeh, Amirali ;
Salehi, Marjan ;
Ozadali, Keriman ;
Ostad, Seyed Nasser ;
Shafiee, Abbas ;
Amini, Mohsen .
BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 21 (08) :2355-2362
[4]   Design, Synthesis and Molecular Docking Study of Some Substituted 4,5-dihydro-2H-indazole Derivatives as Potential Anti-inflammatory Agents [J].
Badr, Mona H. ;
Elbayaa, Rasha Y. ;
El-Ashmawy, Ibrahim M. .
MEDICINAL CHEMISTRY, 2013, 9 (05) :718-730
[5]   6-Chloro-7-methyl-3′, 4′-dimethoxyflavone - a Potent Selective COX-2 Inhibitor [J].
Bashir, Rafia ;
Javed, Kalim ;
Yaseen, Shafiya ;
Ovais, Syed ;
Rathore, Pooja ;
Hamid, Hinna ;
Alam, M. S. ;
Samim, Mohammed ;
Singh, Surender ;
Nair, Vinod .
MEDICINAL CHEMISTRY, 2013, 9 (04) :617-623
[6]   Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors [J].
Ghodsi, Razieh ;
Zarghi, Afshin ;
Daraei, Bahram ;
Hedayati, Mehdi .
BIOORGANIC & MEDICINAL CHEMISTRY, 2010, 18 (03) :1029-1033
[7]   COMPOUNDS RELATED TO THIOSEMICARBAZIDE .2. 1-BENZOYLTHIOSEMICARBAZIDES [J].
HOGGARTH, E .
JOURNAL OF THE CHEMICAL SOCIETY, 1949, (MAY) :1163-1167
[8]   Design and synthesis of niflumic acid-based N-acylhydrazone derivatives as novel anti-inflammatory and analgesic agents [J].
Kheradmand, Amin ;
Navidpour, Latifeh ;
Shafaroodi, Hamed ;
Saeedi-Motahar, Ghazaleh ;
Shafiee, Abbas .
MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (05) :2411-2420
[9]   Anti-inflammatory activity of 2,5-dihydroxycyclohepta-2,4,6-trienone in rats [J].
Koc, Feride ;
Cadirci, Elif ;
Albayrak, Abdulmecit ;
Halici, Zekai ;
Hacimuftuoglu, Ahmet ;
Suleyman, Halis .
MEDICINAL CHEMISTRY RESEARCH, 2010, 19 (01) :84-93
[10]   Estimation of antmociceptive and anti-inflammatory activity on Geranium pratense subsp finitimum and its phenolic compounds [J].
Kuepeli, Esra ;
Tatli, I. Irem ;
Akdemir, Zeliha S. ;
Yesilada, Erdem .
JOURNAL OF ETHNOPHARMACOLOGY, 2007, 114 (02) :234-240