Search results for "Pyrimidine"

Six-Membered Rings, and Their Fused Derivatives

2015

In vivo and in vitro anti-leishmanial activities of 4-nitro-N-pyrimidin- and N-pyrazin-2-ylbenzenesulfonamides, and N2-(4-nitrophenyl)-N1-propylglyci…

2009

A series of compounds containing the nitrobenzene and sulfonamido moieties were synthesized and their leishmanicidal effect was assessed in vitro against Leishmania infantum promastigotes. Among the compounds evaluated, the p-nitrobenzenesulfonamides 4Aa and 4Ba, and the p-nitroaniline 5 showed significant activity with a good selectivity index. In a Balb/c mice model of L. Infantum, administration of compounds 4Aa, 4Ba or 5 (5 mg/kg/day for 10 days, injected ip route) led to a clear-cut parasite burden reduction (ca. 99%). In an attempt to elucidate their mechanism of action, the DNA interaction of 4Aa and 5 was investigated by means of viscosity studies, thermal denaturation and nuclease …

Annelated pyrrolo-pyrimidines from amino-cyanopyrroles and BMMAs as leads for new DNA-interactive ring systems.

2005

The efficient one-pot synthesis of several new tricyclic systems of type 1 and 2, obtained from the reaction of substituted 2-amino-3-cyanopyrroles and 3-amino-4-cyanopyrroles with BMMAs, is reported. The duration and yields of the reaction strongly depend on the reactivity of the starting pyrrole and on the size of the ring to be formed. Mechanist features of the reaction were investigated and proposed by studying also the reactivity of a 3-aminopyrrole-2,4-dicyano substituted. The method reported represents the first example of the use of BMMA reagents in combination with pyrrole derivatives and allows an easy and versatile entry to a large number of hitherto unknown pyrrolo-pyrimidines f…

A two-dimensional magnetic architecture with bridging polynitrile and 2,2′-bipyrimidine ligands

2004

cited By 7; International audience; A new polymeric, two-dimensional compound [Co2(bpym)(dcne) 4 (H2O)2] (1) (dcne = [(CN)2CC(O) OEt)]- = 2,2-dicyano-1-ethoxyethenolate anion and bpym = 2,2'-bipyrimidine) has been synthesized and characterized by X-ray crystallography. The structure is monoclinic space group P21/a and consists of two-dimensional networks of octahedrally coordinated Co(II) ions, bridged by bis-bidentate 2,2'-bipyrimidine and μ2-dcne anions. Magnetic measurements revealed a broad maximum in the xm vs T plot at 20 K which is characteristic of antiferromagnetic exchange between the high spin cobalt(II) centres. © EDP Sciences.

Synthesis, spectroscopic characterization and in vitro antimicrobial activity of diorganotin(IV) dichloride adducts with [1,2,4]triazolo-[1,5-a]pyrim…

2006

Abstract The heterocyclic ligands [1,2,4]triazolo-[1,5-a]pyrimidine (tp) and 5,7-dimethyl-[1,2,4]triazolo-[1,5-a]pyrimidine (dmtp), react with diorganotin dichlorides giving the addition compounds Me2SnCl2(tp)2, Et2SnCl2(tp)2, Me2SnCl2(dmtp)2, Et2SnCl2(dmtp)2, Bu2SnCl2(dmtp), Ph2SnCl2(dmtp). The organotin:ligand stoichiometry goes from 1:2 to 1:1 by increasing the steric hindrance of the organic groups bound to tin. The compounds have been characterized by means of infrared, 119Sn Mossbauer and 1H AND 13C NMR spectroscopy. The ligands presumably coordinate to tin classically through the nitrogen atom at the position 3. The 1:1 complexes adopt trigonal bipyramidal structures, with the organi…

Lipid-Altering Efficacy of Ezetimibe/Simvastatin 10/20 mg Compared to Rosuvastatin 10 mg in High-Risk Patients with and without Type 2 Diabetes Melli…

2010

AIMS: This post hoc analysis compared the effects of switching to ezetimibe/simvastatin 10/20 mg (EZE/SIMVA) or rosuvastatin 10 mg (ROSUVA) in uncontrolled high-risk hypercholesterolemic patients with/without type 2 diabetes mellitus (T2DM) despite statin monotherapy. METHODS: Patients (n = 618) at high risk for coronary vascular disease with elevated LDL-C ≥100 and ≤190 mg/dL despite use of statins were randomized 1:1 to double-blind EZE/SIMVA 10/20 mg or ROSUVA 10 mg for 6 weeks. Patients were classified as having T2DM based on ≥1 of the following: diagnosis of T2DM, antidiabetic medication, or FPG ≥126 mg/dL. This analysis evaluated percent changes from baseline in lipids among patients …

CCDC 696703: Experimental Crystal Structure Determination

2009

Related Article: D.Visinescu, L.M.Toma, O.Fabelo, C.Ruiz-Perez, F.Lloret, M.Julve|2009|Polyhedron|28|851|doi:10.1016/j.poly.2008.12.032

1,2-Methyl shift in the reaction of 4,7-dihydro-4,5-dimethyl-7-phenyl-(1,2,4)-triazolo[1,5-a]pyrimidine with tosyl azide

2000

The reaction of the heterocyclic enamine 1 with tosyl azide (2) leads to the tosylimino derivative 4 of 1,2,4-triazolo[1,5-a]pyrimidine. The extrusion of nitrogen from the primary adduct 3 is followed by a 1,2-shift of a methyl group. The structure determination of 4 is based on 1H and 13C nmr spectra including NOE measurements.

Synthetic and theoretical studies of novel ring closure and ring opening reactions

2006

Ring closure and ring opening reactions are in many cases useful synthetic procedures in organic chemistry. They allow the preparation of complex molecules with high stereoselectivity and good yields. Mechanistic and theoretical studies have been carried out on the transformation of 2-aminopyrimidines into imidazo[1,2-c]pyrimidines and guanidines, respectively, through ring closure and ring opening reactions, as well as the transamidation reactions through the ring closure and ring opening of guanidine derivatives, which constitute novel synthetic methods. Sepulveda Arques, Jose, Jose.Sepulveda@uv.es

CCDC 696698: Experimental Crystal Structure Determination

2009

Related Article: D.Visinescu, L.M.Toma, O.Fabelo, C.Ruiz-Perez, F.Lloret, M.Julve|2009|Polyhedron|28|851|doi:10.1016/j.poly.2008.12.032