Substituted Benzylidene-3-Oxo-3,4-Dihydro-2H-Benzo[b][1,4]thiazine-6-Carboxylic Acid Analogs as Dynamin GTPase Inhibitors.
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DOI: 10.1002/cmdc.202500377
Abstract: Screening identified 2‐hydroxy‐3‐oxo‐3,4‐dihydro‐2H‐benzo[b][1,4]oxazine‐6‐carboxylic acid (1) as a 55 µM dynaminGTPase inhibitor. Synthesis of three 1‐based libraries shows no potency enhancement. However, S‐isostere‐based 3‐oxo‐3,4‐dihydro‐2H‐benzo[b][1,4]thiazine‐6‐carboxylic acid (16) gives rise to Libraries 4–6. Library 4 retains the C6‐ester of… read more here.
Keywords: carboxylic acid; benzo thiazine; oxo dihydro; dihydro benzo ... See more keywords
Synthesis of 1,2,3-triazole-piperazin-benzo[b][1,4]thiazine 1,1-dioxides: antibacterial, hemolytic and in silico TLR4 protein inhibitory activities
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DOI: 10.1039/d3ra07509e
Abstract: In this study, we designed and synthesized a number of novel 1,2,3-triazole-piperazin-benzo[b][1,4]thiazine 1,1-dioxide derivatives and investigated their in vitro antibacterial and hemolytic activity. When compared to the lead chemical, dicloxacillin, the majority of the compounds… read more here.
Keywords: piperazin benzo; benzo thiazine; antibacterial hemolytic; triazole piperazin ... See more keywords
Derivatives of benzo-1,4-thiazine-3-carboxylic acid and the corresponding amino acid conjugates
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DOI: 10.3762/bjoc.18.124
Abstract: Herein, we present the synthesis and utilization of derivatives of 4H-benzo[b][1,4]thiazine-3-carboxylic acid. These benzothiazine compounds were assembled via the coupling of aminothiols and bromopyruvates. Oxidative dimerization of these starting materials was also observed and the… read more here.
Keywords: carboxylic acid; derivatives benzo; thiazine carboxylic; acid ... See more keywords