Ceskoslovenska Akademie Ved

Alena Machova

Tomislav Barth

Karel Jost

Linda Servitova

Frantisek Brtnik

Michal Lebl

Ivan Krejci

Jana Skopkova

Jirina Slaninova

Bela Kupkova

Petr Simek

Jirina Slantinova

Pavel Hrbas

The invention pertains to analogs of neurohypophysial hormones evidencing inhibition effects of the chemical formula I ##STR1## where A is CH.sub.3 CO or H, V is a residue of penicilamine or cysteine, B is CH.sub.3 or H, X is a residue of isoleucine or phenylalanine, Y is a residue of penicilamine or cysteine, and Z is a residue of leucine or lysine. These analogues evidence inhibition effects towards certain biological activities of neurohypophysial hormones.

Analogs of neurohypophysial hormones with inhibition effects

Analogs of neurohypophysial hormones with inhibition properties are described. The hormones are of the formula ##STR1## wherein in all chiral amino acids are of the L-series and the aromatic amino acid in the position 2, indicated with an asterisk, is of the D-series, and where R.sup.1 and R.sup.2 are hydrogen or a methyl group, R.sup.3 is hydrogen, an amino group, or a triglycylamine grouping, R.sup.4 is hydrogen, a methyl, ethyl or ethoxy group, R.sup.5 is S--CH.sub.2 or S--S group, X.sup.1 is a residue of isoleucine or phenylalanine, X.sup.2 is a residue of leucine or lysine, and X.sup.3 is a glycinamide residue or a hydroxyl group. These compounds exhibit inhibition effects towards the uterotonic and pressor activity of natural hormones. The common structural feature of all these analogues is the presence of an aromatic hydrophobic D-amino acid in the position 2.

Analogs of neurohypophysial hormones

Vasopressin analogs of the formula ##STR1## wherein R.sup.1 is H, R.sup.2 is CH.sub.2 S and R.sup.3 is D-Arg,

Analogs of vasopressin

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Prague, Czechia

Alena Machova