Subject(s)
Anti-Bacterial Agents/pharmacology , Biofilms/drug effects , Gram-Positive Bacteria/drug effects , Pyrroles/pharmacology , Staphylococcus/drug effects , Anti-Bacterial Agents/chemical synthesis , Microbial Sensitivity Tests , Pyrroles/chemical synthesis , Pyrroles/chemistry , Structure-Activity Relationship , Vancomycin/pharmacologyABSTRACT
The activity against Gram-positive bacteria of 3,4,5,3',5'-pentabromo-2-(2'-hydroxybenzoyl)pyrrole I, a synthetic anti-bacterial compound related to pyrrolomycins, was tested in vitro using seven reference bacterial strains and Staphylococcus epidermidis and Staphylococcus aureus preformed biofilms. Compound I was active against all strains tested, with minimum inhibitory concentration (MIC) values ranging from 0.002 to 0.097 mg/l and minimum bactericidal concentrations (MBCs) from 0.37 to 12.5 mg/l. Compound I was also active at low concentrations against preformed S. epidermidis and S. aureus biofilms.
Subject(s)
Anti-Bacterial Agents/pharmacology , Biofilms/drug effects , Gram-Positive Bacteria/drug effects , Hydrocarbons, Brominated/pharmacology , Pyrroles/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Drug Resistance, Bacterial , Gentian Violet/metabolism , Gram-Positive Bacteria/growth & development , Humans , Hydrocarbons, Brominated/chemical synthesis , Hydrocarbons, Brominated/chemistry , Microbial Sensitivity Tests , Pyrroles/chemical synthesis , Pyrroles/chemistry , Tetrazolium Salts/metabolism , Thiazoles/metabolismABSTRACT
Copper(II) and platinum(II) complexes of 2-benzoylpyrrole (2-BZPH) were synthesized and characterized with IR, 1H and 13C NMR spectroscopies and coordination geometry with ligands arranged in transoid fashion. The crystal structure of [Cu(II)(2-BZP)2] was determined by X-ray diffraction. Death of complex treated Jurkat cells was measured by flow cytometry. The bis-chelate complexes [Cu(II)(2-BZP)2] and [Pt(II)(2-BZP)2] adopt square-planar coordination geometry with ligands, arranged in transoid fashion. Concentrations of 1-10 microM Platinum(II) complexes reduced cell survival from 100% to 20%, in contrast to the copper(II) complex which caused no cell death at a concentration of 10 microM. While the Pt(II) complexes may have damaged DNA to induce cell death, treatment with the Cu(II) complex did not induce Jurkat cell death.
Subject(s)
Antineoplastic Agents/chemical synthesis , Copper/chemistry , Organometallic Compounds/chemical synthesis , Platinum/chemistry , Pyrroles/chemical synthesis , Pyrroles/toxicity , Antineoplastic Agents/chemistry , Antineoplastic Agents/toxicity , Cell Death/drug effects , Cell Survival , Crystallography, X-Ray , Dose-Response Relationship, Drug , Flow Cytometry , Formazans/pharmacology , Humans , Hydrogen Bonding , Indicators and Reagents/pharmacology , Jurkat Cells , Ligands , Magnetic Resonance Spectroscopy , Molecular Conformation , Molecular Structure , Organometallic Compounds/chemistry , Organometallic Compounds/toxicity , Pyrroles/chemistry , Spectrophotometry, InfraredABSTRACT
Nine naturally-occurring 2,2':5',2"-terthiophenes were quantitatively evaluated for their in vitro photoinduced growth inhibitory activity against three bacterial strains. All the compounds proved active towards Staphylococcus aureus. As regards Escherichia coli, the unsubstituted 2,2':5'2"-terthiophene (MIC = 0.62 microgram/ml at 4j/cm2 fluence), was found to be the only compound active. None of the compounds tested displayed activity on Pseudomonas aeruginosa at the highest concentration tested.
Subject(s)
Anti-Bacterial Agents/pharmacology , Thiophenes/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/radiation effects , Escherichia coli/drug effects , Light , Microbial Sensitivity Tests , Molecular Structure , Plants, Medicinal , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects , Structure-Activity Relationship , Thiophenes/chemistry , Thiophenes/radiation effectsSubject(s)
Anti-Bacterial Agents/pharmacology , Bromine/pharmacology , Pyrroles/pharmacology , Staphylococcus aureus/drug effects , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Bromine/chemistry , Humans , Methicillin Resistance , Microbial Sensitivity Tests , Pyrroles/chemical synthesis , Pyrroles/chemistryABSTRACT
The synthesis of 1-phenyl-5,8-dimethyl-1,4,5,6,7,8-hexahydro-pyrazolo[3,4-e][1,4] diazepin-4,7-dione and of 1-phenyl-3,5,8-trimethyl-1,4,5,6,7,8-hexahydro-pyrazolo[3,4-e] [1,4]diazepin-4,7-dione is described. These compounds exhibit activity on CNS in animals.
