RESUMEN
A 33-year-old male patient with fever, splenomegaly, pancytopenia and lymphocytosis was admitted to the Department of Hematology in Rijeka. Laboratory findings, bone marrow aspiration and biopsy excluded hemoblastosis and aplastic anemia. To exclude primary splenic lymphoma we performed splenic aspiration where Leishmania amastigotes were found. No cases of visceral leishmaniasis have been previously described in the Northern Adriatic region. Considering epidemiology, a contraction of the disease in the Velebit mountain range could be possible despite the current non-endemic status of the region.
Asunto(s)
Leishmaniasis Visceral/epidemiología , Adulto , Croacia/epidemiología , Humanos , Leishmaniasis Visceral/diagnóstico , MasculinoRESUMEN
A series of the novel oleandomycin 9-oximes has been prepared and characterized by spectroscopic data and X-ray analysis. The antibacterial in vitro activities of the oximes (6-10) were compared with that of oleandomycin (1). Among the novel derivatives the most active compound was 8(R)-methyloleandomycin-9-oxime (9) in contrast ot its 8(S)-isomer (10) which possessed only low potency. Some preliminary pharmacokinetic data of 9 confirmed its activity. Compound 9 has been advanced to further biological study.
Asunto(s)
Oleandomicina/química , Oleandomicina/farmacología , Animales , Bacterias/efectos de los fármacos , Cristalografía , Técnicas In Vitro , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Oleandomicina/análogos & derivados , Oleandomicina/farmacocinética , Ratas , Distribución TisularRESUMEN
The novel 9a,11-cyclic carbamates (13-15) of 9-deoxo-9a-aza-9a-homoerythromycin A (4) have been prepared and characterized by 1H-1H and 1H-13C 2D NMR spectroscopy. When compared to azithromycin (1) or its 6-O-methyl derivative (2), the new bicyclic 15-membered azalides exhibited substantially decreased antibacterial activities in vitro.
Asunto(s)
Azitromicina/análogos & derivados , Bacterias/efectos de los fármacos , Eritromicina/análogos & derivados , Azitromicina/química , Azitromicina/farmacología , Eritromicina/química , Eritromicina/farmacología , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Relación Estructura-ActividadRESUMEN
A series of O-methylazithromycin derivatives have been synthesized and their antibacterial activities were compared with those of azithromycin (1). O-Methylation of 1 proceeded stepwise by the two main pathways beginning at the C-6 and C-11 hydroxyl groups, individually. Among O-methyl derivatives, 6-O-methylazithromycin A (11) was slightly less active than 1. The methylation of the secondary hydroxyl group at the C-11 position resulted surprisingly in an increase of their in vitro activity. The antibacterial activities of novel azalides decreased with increasing the number of the methyl groups introduced.