Molecules · 2017 · 36 citations · 21 references
PharmacyMedicinal ChemistryPharmacologyAntimicrobial PharmacologyDrug DesignDrug DiscoveryAntibacterial AgentsAntibacterial PharmacologyAntibacterial PharmacotherapyAntibacterial TherapyAntibiotic ResistanceMultidrug ResistanceAntibacterial Drug DevelopmentGram-negative Bacterial InfectionsGram-positive Bacterial InfectionsMinimum Inhibitory Concentration DeterminationMycobacterium Tuberculosis InfectionPhenotypic Drug Susceptibility TestingPotency RelationshipTuberculosis Drug Development
A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for 7) show potency against Mycobacterium tuberculosis (MTB) H37Rv (minimum inhibitory concentration (MIC): <0.5 μM), which is better than the parent drug CPFX, and comparable to moxifloxacin and isoniazid, some of the tested Gram-positive strains (MIC: 0.06–4 μg/mL), and most Gram-negative strains (MIC: ≤0.03–4 μg/mL).
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Isatin hybrids and their anti-tuberculosis activity
Zhi Xu, Shu Zhang, Chuan Gao et al. · Chinese Chemical Letters · 2016 · 258 citations
Megan J. Robinson, Barbara A. Martin, Thomas D. Gootz et al. · Journal of Biological Chemistry · 1991 · 145 citations · Full text