ARKIVOC · 2007 · 282 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyAntimicrobial PharmacologyDrug DiscoveryStructure-activity RelationshipsHit-to-lead OptimizationLead Compound DesignLead DiscoveryStructure-activity Relationship AnalysisTuberculosis PharmacotherapyMinimum Inhibitory Concentration DeterminationMycobacterium Tuberculosis InfectionNitro CompoundsTuberculosis Drug DevelopmentTuberculosis Drug Resistance
Several nicotinic and isoniazid derivatives, most of them containing nitro groups were synthesized by our group, and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37 Rv using the Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in mg/mL. The compound 11d exhibited the best result (1.2 g/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of multi-drug resistant tuberculosis.