Synthesis, anti-inflammatory and analgesic activity of 2-[4-(substituted benzylideneamino)-5-(substituted phenoxymethyl)-4H-1,2,4-triazol-3-yl thio] acetic acid derivatives

AbstractThe title compounds 3a–l have been synthesized by the reaction of thiocarbohydrazide with substituted phenoxy acetic acid to obtained substituted 1,2,4-triazoles (1). Compound 1 was treated with various substituted aromatic aldehydes which results in 4-(substituted benzylideneamino)-5-(substituted phenoxymethyl)-2H-1,2,4-triazol-3(4H)-thiones (2a–g), further 2a–g is converted to 2-[4-(substituted benzylideneamino)-5-(substituted phenoxymethyl)-4H-1,2,4-triazol-3-yl thio] acetic acid (3a–l) derivatives by the reaction with chloroacetic acid. All the newly synthesized compounds were evaluated for in vivo anti-inflammatory and analgesic activities. Among the series 2-[4-(2,4-dichlorobenzylideneamino)-5-(phenoxymethyl)-4H-1,2,4-triazol-3-yl thio] acetic acid (3d), 2-[4-(4-dichlorobenzylideneamino)-5-(phenoxymethyl)-4H-1,2,4-triazol-3-yl thio] acetic acid (3e), 2-[4-(2,4-dichlorobenzylideneamino)-5-[(2,4-dichlorophenoxy)methyl]-4H-1,2,4-triazol-3-yl thio] acetic acid (3j) and 2-[5-[(2,4-dichlorophenoxy)methyl)]-4-(4-chlorobenzylideneamino)-4H-1,2,4-triazol-3-yl thio] acetic acid (3k) showed significant anti-inflammatory activity with P<0.001 (63.4%, 62.0%, 64.1% and 62.5% edema inhibition, respectively), as compared to the standard drug diclofenac (67.0%) after third hour respectively and also compounds 3j, 3k exhibited significant analgesic activity with P<0.001 (55.9% and 54.9% protection, respectively) and less ulcerogenic activity as compared with standard drug aspirin (57.8%)

DNA-Based Food Authentication Techniques : Differentiation of Tetraploid and Hexaploid Wheat

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Synthesis and Antimicrobial Activity of 2-[4-(Substituted Benzylidenamino)-5-(Substituted Phenoxymethyl)-4H-1,2,4-Triazol-3-yl thio] Acetic Acid Derivatives

2-[4-(substituted benzylidenamino)-5-(substituted phenoxymethyl)-4H-1,2,4-triazol-3-yl thio] acetic acid (3a-j) derivatives have been synthesized by the reaction between 4-(substituted benzylidenamino)-5-(substituted phenoxymethyl)-2H-1,2,4-triazol-3(4H)-thiones (2a-j) and chloroacetic acid containing catalytic amount of pyridine. All these compounds were screened for antimicrobial activity. The compounds 3h and 3j exhibited good antifungal activity against A. niger, C. Neoformans, and A. fumigatus at MIC of 0.25 μg/ml compared to standard drug fluconazole at MIC of 1 μg/mL

Clinical characteristics of eosinophilic COPD versus COPD patients with a history of asthma

Abstract Eosinophilic COPD appears to be a distinct patient subgroup with an increased corticosteroid response. Eosinophilic COPD has been labelled as part of the asthma COPD overlap syndrome (ACOS). We compared the clinical characteristics of eosinophilic COPD patients (without any clinical history of asthma) and COPD patients with a childhood history of asthma. COPD patients with asthma were characterised by more allergies and more exacerbations, but less eosinophilic inflammation. While terms such as “ACOS” are used to “lump” patients together, we report distinct differences between eosinophilic COPD and COPD patients with asthma, and propose that these groups should be split rather than lumped