- Discovery of substituted (2‐aminooxazol‐4‐yl)isoxazole‐3‐ carboxylic acids as inhibitors of bacterial serine acetyltransferase in the quest for novel potential antibacterial adjuvants
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Many bacteria and actinomycetales use L‐cysteine biosynthesis to increase their tolerance to antibacterial treatment and establish a long‐lasting infection. In turn, this might lead to the onset of antimicrobial resistance that currently represents one of
- Magalh?es, Joana,Franko, Nina,Raboni, Samanta,Annunziato, Giannamaria,Tammela, P?ivi,Bruno, Agostino,Bettati, Stefano,Armao, Stefano,Spadini, Costanza,Cabassi, Clotilde Silvia,Mozzarelli, Andrea,Pieroni, Marco,Campanini, Barbara,Costantino, Gabriele
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- Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery
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Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the growth of actively replicating, nonreplicating persistent, and resistant Mycobacterium tuberculosis strains. Clues from the structure-activity relationships lining up the antitubercular activity were exploited for the rational design of improved analogues. Two compounds, namely N-phenyl-5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 7a and N-(pyridin-2-yl)-5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 8a, were found to show high inhibitory activity toward susceptible M. tuberculosis strains, with an MIC90 of 0.125-0.25 μg/mL (0.33-0.66 μM) and 0.06-0.125 μg/mL (0.16-0.32 μM), respectively. Moreover, they maintained good activity also toward resistant strains, and they were selective over other bacterial species and eukaryotic cells, metabolically stable, and apparently not susceptible to the action of efflux pumps.
- Azzali, Elisa,Machado, Diana,Kaushik, Amit,Vacondio, Federica,Flisi, Sara,Cabassi, Clotilde Silvia,Lamichhane, Gyanu,Viveiros, Miguel,Costantino, Gabriele,Pieroni, Marco
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supporting information
p. 7108 - 7122
(2017/09/07)
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- Synthesis and pharmacological characterization of new analogs of broxaterol
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A series of isoxazole derivatives structurally related to broxaterol 1 has been prepared and tested for their potency to β1 and β2 adrenergic receptors. At variance with broxaterol, none of the tested compounds displayed agonistic activity. The 3-isopropenyl derivative 5f is the most potent antagonist both in the trachea and atria preparations.
- De Amici,Conti,Dallanoce,Kassi,Castellano,Stefancich,De Micheli
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- N-(4-isoxazolylthiazol-2-yl)oxamic acid derivatives as potent orally active antianaphylactic agents
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A series of N-(4-isoxazolylthiazol-2-yl)oxamic acid derivatives was synthesized and tested on the passive cutaneous anaphylaxis (PCA) model in rats to verify its potential antianaphylactic activity. These compounds were prepared by reaction of an appropri
- Chiarino,Grancini,Frigeni,Biasini,Carenzi
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p. 600 - 605
(2007/10/02)
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- Synthesis of New Isoxazole Aminoalcohols
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The preparation of new 1-isoxazolyl-2-amino-1-ethanol derivatives is described starting from the corresponding 1-isoxazolylethanones.It is also reported the synthesis of 1-(5-isoxazolyloxy)-3-amino-2-propanol compounds starting from the corresponding 5-ha
- Chiarino, D.,Fantucci, M.,Sala, A.,Veneziani, C.
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p. 337 - 342
(2007/10/02)
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