Bulletin of the Korean Chemical Society · 2010 · 11 citations · 26 references
PharmacyChemistryMedicinal ChemistryDrug DiscoveryOrganic ChemistryStructure-activity RelationshipsHeterocyclic ChemistryStructure-activity Relationship AnalysisAntibiotic DiscoveryAntimicrobial Compound ScreeningEscherichia ColiNovel Antibacterial Agents
A series of N(2)-benzothiazolyl substituted tetrahydroindazoles has been synthesized via cyclic <TEX>${\beta}$</TEX> keto esters. Optimum reaction condition was found as acidic toluene and effect of higher acidity towards substituted hydrazines in situ was described. Synthesized compounds have been achieved as single isomer and characterized by using 1D and 2D NMR spectral reports. Antimicrobial screening was carried out for the synthesized compounds along with a series of N(2)-pyridyl tetrahydroindazoles.1 The results of the in vitro antimicrobial screening studies revealed that compounds 13, 16 against Staphylococcus aureus, 11 against Escherichia coli, 10-12, 16 against Pseudomonas aeruginosa and 12 against Klebsiella pneumoniae recorded almost two-fold better activity compared to the standard drug used.
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Michaël Génin, Carolyn Biles, Barb J. Keiser et al. · Journal of Medicinal Chemistry · 2000 · 378 citations · Full text
3,4-Diphenyl-1H-pyrazole-1-propanamine antidepressants
Denis M. Bailey, Philip E. Hansen, Allan G. Hlavac et al. · Journal of Medicinal Chemistry · 1985 · 306 citations