Synthesis and pharmaceutical properties of N-acyloxymethyl prodrugs of Allop with potential anti-trypanosomal activity.

We report herein the synthesis, and the physicochemical and pharmacokinetic properties of N-acyloxymethyl prodrugs of allopurinol (Allop) (2a-f). Allop is a compound with activity against Trypanosoma cruzi, a causative agent of Chagas disease. Its pathology leads to a huge number of infections and deaths per year, because in addition to many sufferers only having limited access to health services only an inefficient chemotherapy is available. Relevant pharmaceutical properties (pKa, stability, solubility, lipophilicity, in vitro permeability, binding protein, xanthine oxidase binding) were also determined. The results obtained showed that derivatives behave as prodrugs of Allop, since they exhibit improved physicochemical and pharmacokinetic properties relative to their precursor. This behavior turns these compounds into active reservoirs of Allop, and reduces its unfavorable characteristics, so 2a-f compounds are excellent candidates for the treatment of Chagas disease. This work is therefore an important contribution leading to the suppression of Chagas disease.

Preparative chromatography for obtaining pure samples of rosaniline, magenta II, and new fuchsine.

A simple low pressure liquid chromatographic method is reported that can separate the basic fuchsine homologues, rosaniline, magenta II and new fuchsine from an impure commercial dye. The chromatographic purity of the separated dyes is > 90%. All homologues were obtained in multi-milligram amounts per chromatographic run; precise yields depend on the composition of the starting material and potentially may be greater. This is a useful preparative procedure for generating chromatographically pure samples of basic fuchsine homologues, especially those that cannot be obtained in pure form by direct synthesis.

[Occurrence of pregnancy after microsurgical treatment of sterile patients with tubo-ovarian adhesive diseases]. / Frecuencia de embarazos después de tratamiento microquirúrgico en pacientes estériles por enfermedad adherencial tuboovárica.

In the last years, the adherence adnexal disease has been increased due to pelvic infections. This may cause infertility problems depending, of the nature, extension and localization inside the pelvis. In this paper we inform the results obtained in 70 patients with adnexal adhesions to whom it was performed a salpingo-ovariolysis with microsurgery technology, with the purpose of promote the fertility. All the patients received pre, trans and postoperative support (Heparin, steroids and antimicrobials). The minimal time of postoperative observation was at least 6 months. In 27 (Group I) of the 70 cases (38.6%), the adherences were avascular (IA & IIA based on Hulka's classification); and in the 43 patients of the group II (61.4%), the lesions were dense and vascular (IB & IIB). In group I, 15 pregnancies were obtained (55.6%), 13 at term, 1 miscarriage and 1 ectopic pregnancy; in the group II we documented 9 pregnancies (20.9%), 5 at term, 4 miscarriage (I trimester).

[Lesions of the fallopian tube following tube occlusion]. / Lesiones de la trompa de Falopio posteriores a oclusión tubárica.

This is a study using light microscopy and electronic microscopy of Fallopian tube subjected to sterilization; and compare it with a control group. A total of 60 samples from patients with different surgical procedures, whose age was from 20 to 40 years; they were amenorrheic, without antecedents of pelvic inflammatory disease nor endometriosis. Among the control group, there were lesions as isthsmical nodular salpingitis in 30.7%. There was chronic salpingitis in 15.3%; follicular salpingitis in 23%, and polyps in 15%. In the group with OTB antecedents, endosalpingiosis was found in 20%; follicular salpingitis in 30% and chronic salpingitis in the remaining 50%. By means of electronic, ultrastructural microscopy, were seen lesions at myosalpinx level, that is, alterations in myofilaments, formation, much fibrosis and descilliation in the adjacent to OTB. It may be concluded that these findings, never seen before, may condition an alteration of tubal motility in patients subjected to rechannelization procedures, that condition an alteration in gametes transportation, avoiding fecundation or a greater incidence ectopic pregnancy incidence.