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Evaluation of Biological Activity of Derivatives of 1,3,4-Thiadiazole, 1,3,4-Oxadiazole and 1,2,4-Triazole
Endocrine, Metabolic & Immune Disorders - Drug Targets ( IF 2.0 ) Pub Date : 2021-05-01 , DOI: 10.2174/1871530320999200729164926
Gaurav M. Doshi 1 , Mayuresh U. Bansode 2 , Rakesh R. Somani 3
Affiliation  

Objective: 1,3,4-thiadiazole (A), 1,3,4-oxadiazole (B) and 1,2,4-triazole (C) derivatives have been known for their immense pharmacotherapeutic potential. The current research article attempts to further explore and understand the probable biochemical mechanism related to antiinflammatory activity of derivatives.

Methods: The screened A, B and C derivatives were investigated for both in-vitro (Erythrocyte Membrane stabilization activity, Proteinase enzyme inhibitory activities) and in-vivo correlation using acute and chronic anti-inflammatory potential by carrageenan induced rats paw edema and cotton pellet granuloma methods, respectively. The activity was studied after interpreting acute toxicity studies results.

Results: In vitro studies in the case of Erythrocyte Membrane stability and Proteinase enzyme inhibitory activities exhibited by A, B, and C at 100 ppm were found to be 48.89%, 51.08% and 50.08% and 66.78%, 76.91% and 57.41%, respectively. The maximum toxic dose was found to be 2000 mg/kg. The derivatives were studied for two-dose levels viz; Lower (100 mg/kg) and higher dose (200 mg/kg). In rat paw edema, maximum decrease was obtained for A (50.05%), B (50.05%) and C (51.06%) at lower and higher dose at 68.76%, 55.61%, and 65.26%, respectively for effect up to 24 h. In the chronic model of cotton pellet granuloma viz; higher and lower doses of A, B and C exhibited 38.15%, 33.19% and 30.25 % and 19.45%, 18.55% and 17.55 %, respectively.

Conclusion: The studied models depicted that derivatives A, B and C have the probable potential as anti-inflammatory agents. Further studies need to be undertaken to explore their potential in the different therapeutic areas.



中文翻译:

1,3,4-噻二唑,1,3,4-恶二唑和1,2,4-三唑衍生物的生物活性评价

目的:1,3,4-噻二唑(A),1,3,4-恶二唑(B)和1,2,4-三唑(C)衍生物具有巨大的药物治疗潜力。当前的研究文章试图进一步探索和理解与衍生物的抗炎活性有关的可能的生化机制。

方法:利用角叉菜胶诱导的大鼠爪水肿和棉花颗粒,利用筛选出的急性,慢性消炎潜力,对筛选出的A,B和C衍生物的体外(红细胞膜稳定活性,蛋白酶抑制酶活性)和体内相关性进行研究。肉芽肿的方法分别。在解释了急性毒性研究结果之后,对活性进行了研究。

结果:A,B和C在100 ppm时对红细胞膜稳定性和蛋白酶抑制活性的体外研究发现分别为48.89%,51.08%和50.08%和66.78%,76.91%和57.41%,分别。发现最大毒性剂量为2000 mg / kg。研究了衍生物的两个剂量水平。较低(100 mg / kg)和较高剂量(200 mg / kg)。在大鼠足水肿中,分别以68.76%,55.61%和65.26%的低剂量和高剂量分别对A(50.05%),B(50.05%)和C(51.06%)产生最大的降低作用,直至24小时。在棉花颗粒肉芽肿的慢性模型中,即;较高和较低剂量的A,B和C分别显示38.15%,33.19%和30.25%和19.45%,18.55%和17.55%。

结论:所研究的模型描述了衍生物A,B和C可能具有抗炎药的潜力。需要进行进一步的研究以探索其在不同治疗领域中的潜力。

更新日期:2021-05-06
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