Design,synthesis and biological evaluation of oxazolidinone-quinolone hybrids |
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Authors: | Hubschwerlen Christian Specklin Jean Luc Sigwalt Christine Schroeder Susanne Locher Hans H |
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Institution: | Morphochem AG, Schwarzwaldallee 215, CH-4058 Basel, Switzerland. christian.hubschwerlen@morphochem.ch |
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Abstract: | Oxazolidinone-quinolone hybrids that combine the pharmacophores of a quinolone and an oxazolidinone were synthesised and shown to be active against a variety of resistant and susceptible Gram-positive and fastidious Gram-negative organisms. The best compounds in this series overcome all types of resistance in relevant clinical Gram-positive pathogens. The nature of the spacer greatly influences the antibacterial activity. The dual mode of action could be demonstrated for compounds having a piperazinyl spacer. Antibacterial activity was higher at acidic pH. |
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