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.