Potent antiinflammatory 3-thiazole-4(5)-acetic acids of 1,2-benzisothiazole

Sharma, Pawan K.; Sawhney, S. N.

doi:10.1016/s0960-894x(97)00449-6

Cited by 34 publications

(10 citation statements)

References 12 publications

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“…These results have further promoted our interest to design and synthesize some new products derived from thiazolo[3,2-b]-1,2,4-triazoles and evaluate their anti-inflammatory and analgesic activities. 1974; Sharma and Sawhney, 1997). For example, fenclozic acid (III, I.C.I.…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of some thiazolotriazolyl esters as anti-inflammatory and analgesic agents

et al. 2010

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In order to develop potent analgesic/antiinflammatory compounds with reduced ulcerogenic risk, a series of thiazolotriazolyl-carboxylic and acetic acid esters were synthesized and characterized by spectral and elementary analysis. All synthesized compounds were screened for in vivo anti-inflammatory activities in mice by carregeenan-induced paw edema model. The compounds showing 20% reduction in paw edema were also evaluated for their analgesic activities by acetic acid-induced writhing test and the gastric ulceration risk by determining the lipid peroxidation level in stomachs. Among the compounds tested, compounds 1, 4, 6, 7, 8, 1a, 2a, 3a, 4a, 7a, 2b, and 8b showed moderate-to-good anti-inflammatory activity at various doses in any of the measurement intervals. Compounds 7a, 2b, and 8b were the most actives of the series in analgesic activity test. Moreover, compounds 1, 4, and 8 were found to be safe in stomach in respect of free radical production.

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Section: Introductionmentioning

confidence: 99%

Design and synthesis of some thiazolotriazolyl esters as anti-inflammatory and analgesic agents

et al. 2010

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“…Since there was a lower abundance of the angiogenic marker, we studied the microvessel density Benzisothiazole derivative reported to have many potent pharmacological effects such as antimicrobial, antibacterial, anti-inflammatory, local anesthetic and psychotropic activity [15], [16], [17], [18]. In our previous study, the drug-like property of the compound-g using bioinformatics tool has been showed [19].…”

Section: Calceinmentioning

confidence: 99%

Untitled

2019

RJLBPCS

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Benzisothiazole derivative is known to have potential pharmacological activities such as anti-bacterial, anti-microbial, anti-inflammation and local anesthetic, etc. Here we have studied the anti-tumor activity of novel derivative of benzisothiazole using Ehrlich Ascites solid tumor in mice and its pro-apoptotic property in vitro. Our earlier study showed that 10µM of the compound-g is most effective in inhibiting cancer cells growth and proliferation, so we used the same concentration for this work. Ehrlich ascites solid tumor-bearing mice treated with compoundg showed reduced tumor size and weight by a 3 and 27 fold, respectively. The compound-g upon treatment decreases the endothelial cell proliferation marker CD31 and angiogenic molecule VEGF receptor VEGFR2 along with the proliferation biomarker Ki67. H&E staining showed a three-fold decrease in microvessel density (MVD) count. Cancer biomarker Ki67 was also found to be effectively inhibited by the compound-g in tumor sample as compared to the untreated group.

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“…Thiazole moiety is the key pharmacophore for the synthesis of several biological important molecules. Thiazole containing derivatives plays an important role in biological activity of many compounds such as antimicrobial activity [1,2], anti-inflammatory [3], antitumor activities [4], antiarrhythmic and anticoagulant activities [5]. We also knows that imine derivatives possess potent activities including antibacterial [6,7], antifungal [8,9] and antitubercular [10] activities.…”

Section: Introductionmentioning

confidence: 99%