Design, synthesis and biological evaluation of antipicornaviral pyrrole-containing peptidomimetics.

A series of new peptidomimetics based on the tripeptide sequence Z-Leu-Phe-Gln-OH were synthesized, with ten of these including the alpha-nitrogen atom of the N-terminal amino acid incorporated into the pyrrole cycle. The synthesized compounds were tested for antiviral activity by agar-diffusion plaque inhibition test against Coxsackievirus B1 replication in FL cell. Four of the products were observed to possess an antiviral activity, which was proven to be significant for one product. N-terminal pyrrole moiety and C-terminal free carboxyl function are available in all active compounds. On the other hand, their corresponding -OBzl and -Obu t esters are inactive.

[Suppression of hyperprolactinemia in pituitary microadenoma with cabergoline (Dostinex)].

First choice therapy of microprolactinoma is drug treatment with dopamine agonists. Cabergoline is widely accepted in clinical practice as a first line therapy for tumor-induced pituitary hyperprolactinemia. This study assessed serum prolactin levels, tumor size and adverse events in 22 women treated with cabergoline for one year (mean age 43.5 +/- 6.6 years). Serum prolactin levels changed from a baseline mean of 1417 +/- 347 UI/L to 489 +/- 102 UI/L at study end (in the normal range). Tumor size reduction to tumor disappearance was found in 18 women (from a mean of 7.2 mm to 5.5 mm), and was absent in 4 participants. Adverse events were reported in 2 women. In conclusion, the excellent therapeutic efficacy and the lack of adverse events with Cabergoline promotes its use as a first line therapy of hyperprolactinemia due to pituitary microadenoma.

[Treatment of obesity with a very low-energy dietetic regimen--the endocrine parallels]. / Lechenie na zatlustiavaneto s mnogo niskoenergien dietichen rezhim--endokrinni paraleli.

25 patients with various degree of obesity treated with a very low-caloric diet (Dresden diet) were followed up dynamically. By an average clinical stay of 22 days a satisfactory reduction of the body mass with mean 6.6 kg was achieved at mean reduction of the body mass index from 34 to 31. The blood sugar level, immunoreactive insulin in the course of the oral glucose tolerance test, the 24 h rhythm of the plasma cortisol and the aldosterone level at rest and in orthostatic position at the beginning and the end of the dietetic treatment were followed up. The results achieved are discussed in relation to the reduction of the body mass.