HETEROCYCLES 46. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF THIAZOLO[3,2-b][1,2,4]TRIAZOLES BEARING BENZENESULFONAMIDE MOIETY

被引：7

作者：

Cristina, Anamaria ^{[1
,2
]}

Leonte, Denisa ^{[1
]}

Vlase, Laurian ^{[3
]}

Bencze, Laszlo Csaba ^{[4
]}

Imre, Silvia ^{[5
]}

Apan, Bogdan ^{[6
]}

Mogosan, Cristina ^{[2
]}

Zaharia, Valentin ^{[1
]}

机构：

[1] Iuliu Hatieganu Univ Med & Pharm, Dept Organ Chem, 41 Victor Babes St, Cluj Napoca 400012, Romania

[2] Iuliu Hatieganu Univ Med & Pharm, Dept Pharmacol Physiol & Pathophysiol, 6 Louis Pasteur St, Cluj Napoca 400349, Romania

[3] Iuliu Hatieganu Univ Med & Pharm, Dept Pharmaceut Technol & Biopharmaceut, 41 Victor Babes St, Cluj Napoca 400012, Romania

[4] Babes Bolyai Univ, Fac Chem & Chem Engn, Biocatalysis & Biotransformat Res Grp, 11 Arany Janos St, Cluj Napoca 400028, Romania

[5] Univ Med & Pharm Tirgu Mures, Dept Analyt Chem & Drug Anal, 38 Gheorghe Marinescu St, Targu Mures 540139, Romania

[6] Iuliu Hatieganu Univ Med & Pharm, Dept Pharmacol Toxicol & Clin Pharmacol, 23 Gheorghe Marinescu St, Cluj Napoca 400337, Romania

来源：

FARMACIA | 2018年 / 66卷 / 05期

关键词：

thiazolo[3,2-b][1,2,4]triazole; anti-inflammatory activity; antinociceptive activity; ulcerogenic activity; POLYHETEROCYCLIC COMPOUNDS; ANTIINFLAMMATORY AGENTS; SELECTIVE-INHIBITION; ANALGESIC ACTIVITY; CARRAGEENAN; INFLAMMATION; DERIVATIVES; RAT; DRUGS; EDEMA;

D O I：

10.31925/farmacia.2018.5.20

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In order to synthesize novel anti-inflammatory and analgesic compounds with reduced ulcerogenic risk, a series of thiazolo[3,2-b][1,2,4]triazoles (6a-6d) and their corresponding acyclic intermediates (5a-5d) bearing benzenesulfonamide moiety were obtained and characterized by spectral analysis (H-1 NMR, C-13 NMR, IR and MS). All synthesized compounds were evaluated in vivo for their anti-inflammatory and antinociceptive activities in a rat model of acute inflammation induced by lambda-carrageenan. The compounds 5b, 5c and 6d showed significant anti-inflammatory activity when compared to negative control group, but they did not show superior anti-inflammatory activity when compared to diclofenac, as reference drug. The compounds were also screened for antinociceptive activity in a model of inflammatory hyperalgesia and compounds 5a, 5b, 5c, 6a, 6d presented a significant increase of nociceptive threshold in the inflamed paw. Moreover, compounds 5c, 6a, 6b, 6c and 6d did not show any significant ulcerogenic activity.

引用

页码：883 / 893

页数：11

共 44 条

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