Politechnika Gdanska

Miroslaw Bobrowski

Jerzy Golik

Edward Borowski

Barbara Cybulska

Hanna Wojciechowska

Edward Bordwski

Pawel Kolodziejczyk

Jan Pawlak

Elzbieta Bylec

Wojciech Gruszecki

Jan Zielinski

Malgorzata Gumieniak

Jerzy Gumieniak

Tadeusz Ziminski

Leonard Falkowski

Helena Buluk

Andrzej Rudowski

Maciej Smulkowski

A new class of polyene macrolide antibiotics which exhibit valuable therapeutic properties are obtained by reaction of said antibiotics containing at least one amino group with mono- or oligosaccharides, and/or their derivatives in a suitable solvent. A series of such have been obtained and examined. They all exhibit a high biological activity and form salts which are soluble in water. Said sugar derivatives of antibiotics can be used as antifungal agents, also as substances to reduce the overgrowth of the prostrate gland and cholesterol level in the blood.

Antibiotic derivatives of polyene macrolide group and method of

The subject of this invention are the desalanyltetaine derivatives of the formula 1, wherein R.sup.1 is a hydroxyl group or an arrangement of the formula 2, wherein R.sup.3 is a hydrogen atom or an alkyl, aryl, aralkyl group and X is an acyl or alkyl group, R.sup.2 is a hydrogen atom or an acyl group, and Z is an oxygen atom, hydroxylamine or hydrazine radical or their alkyl, aryl or aralkyl derivatives. The method of the preparation of the derivatives according to the invention consists in treating the desalanyltetaine derivatives of the formula 1, where R.sup.1 and R.sup.2 have the above mentioned significance, and Z is an oxygen atom with hydroxylamine, hydrazine or their derivatives. A modification of the method consists in treating the desalanyltetaine of the formula 1, where R.sup.2 and Z have the above mentioned significance, and R.sup.1 is a hydroxyl group with the chloroethers. Another modification of the method consists in the fact that the desalanyltetaine derivatives of the formula 1 where R.sup.1 and Z have the above mentioned significance and R.sup.2 is a hydrogen atom, are acylized by the proper carboxylic acids derivatives. The advantage of the derivatives according to the invention is a wide spectrum of their activity as well as their low toxity.

Desalanyltetaine derivatives and the method for their preparation

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Miroslaw Bobrowski