ABSTRACT
A set of arylpiperazine derivatives with imide fragments, 1-(1H-pyrrol-1-ylmethyl)-10-oxa-4-azatricyclo[5.2.1.0(2,6)-]dec-8-ene-3,5-dione connected by propyl and butyl linkers, were synthesized and tested for the potential anxiolytic and antidepressant activities. Compounds 3a and 3b demonstrated antidepressant activity in the forced swimming tests in mice and were devoid of neurotoxic effects. (chimney test in mice).
Subject(s)
Anti-Anxiety Agents/chemical synthesis , Antidepressive Agents/chemical synthesis , Piperazines/chemical synthesis , Animals , Anti-Anxiety Agents/chemistry , Anti-Anxiety Agents/pharmacology , Antidepressive Agents/chemistry , Antidepressive Agents/pharmacology , Male , Mice , Motor Activity/drug effects , Piperazines/chemistry , Piperazines/pharmacologyABSTRACT
A new quaternary ammonium compound, bis-[2-hydroxy-3-(1,7,8,9,10-pentamethyl-3,5-dioxo-4-aza-tricyclo[5.2.1.0(2,6)]dec-8-en-4-yloxy)-propyl]-dimethyl-ammonium chloride (4), was synthesized. The compound was investigated for antibacterial activity, including Gram-positive cocci and Gram-negative rods, and antifungal activity. Compound 4 showed significant inhibition against Staphylococcus aureus. Research was carried out over 4 standard strains and 40 hospital strains. Elementary analysis and/or MS, (1)H NMR and (13)C NMR spectra confirmed the identity of the products. The molecular structure of 3 was determined by an X-ray analysis.
Subject(s)
Ammonium Chloride/chemical synthesis , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Ammonium Chloride/chemistry , Ammonium Chloride/pharmacology , Anti-Bacterial Agents/chemistry , Culture Media , Magnetic Resonance Spectroscopy , Mass Spectrometry , Microbial Sensitivity Tests , Models, Molecular , Molecular StructureABSTRACT
The structural analysis of deacetylcephalothin [systematic name: (6R,7R)-3-hydroxymethyl-8-oxo-7-(2-thiophen-2-ylacetylamino)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid], C(14)H(14)N(2)O(5)S(2), shows that the geometry of the central bicyclic moiety is close to the geometry exhibited by other biologically active cephalosporin antibiotics. The molecules are arranged in a helical chain running parallel to the 2(1) axis via a strong O-H...O hydrogen bond. The main helices are zipped together via N-H...O interactions, forming infinite layers. The supramolecular architecture is stabilized by O-H...S and C-H...O hydrogen bonds.
Subject(s)
Cephalothin/analogs & derivatives , Cephalothin/chemistry , Hydrogen Bonding , X-Ray DiffractionABSTRACT
Two binuclear bis(tricarbonyliron) title complexes with N(2)Fe(2) tetrahedral cores, 1 and 2, respectively, which show different molecular folding resulting from the appearance (in 1), and absence (in 2) of the N-N sigma-bond, were compared in terms of mass spectral fragmentation routes. A multipath fragmentation noted for the molecule 1 revealing internal stress contrasts with the single-route fragmentation of 2. The fragmentation paths resulting from the admixtures were defined and analyzed from the fragment ion B/E and parent ion B(2)/E linked scan spectra.
