Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof

#The invention relates to novel peptaibol antibiotics, called cephaibols, which are synthesized from Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium, a process for the isolation of the cephaibols from the culture medium and their purification, and the use of the cephaibols as pharmacologically active compounds, in particular for the control of parasites.

#Parasitoses are widespread and cause a wide spectrum of pathological effects in humans and animals, which range from slight physiological disturbances to severe, even fatal disorders. Nowadays, many intensively researched parasite disorders are known which threaten the health and the life of humans, their pets, and farm animals.

#Globally, the weakening of the immune system is to be increasingly found in millions of humans. This group of people is so massively affected by opportunistic parasites that, annually, millions of deaths are mourned. In the age of long-distance travel, even in non-third world countries, which normally have a high standard of hygiene, exotic parasites have to be expected. This has its origins in the fact that there is an ever increasing trend to go on trekking trips under local hygiene conditions and that—because of the supposed safety in one's own country—there is a loss of the feeling/knowledge about hygiene dangers in other countries. In addition to the protection of human health, protection of animals from the suffering and pain caused by parasitoses is required either by a cure or, if possible, by prevention. Economic reasons especially come to bear in farm animal husbandry, where, owing to unfavorable conditions for the keeping and feeding of animals (e.g., in certain forms of mass animal husbandry), parasitic disorders occur which contribute to a quantitative loss (reduction in yield of meat, number of eggs, racing pace) or a qualitative loss (quality of meat and wool). The great damage that is caused by parasitoses in humans and animals makes their control desirable, if not indispensable, in the interests of health and economy.

#In the following, the invention is described in detail, in particular in its preferred embodiments.

#Compounds of the formula I or II are also designated as peptide active compounds or cephaibols.

#In the following sequences, AcPhe is N-acetylphenylalanine, Aib is α-aminoisobutyric acid, Ala is alanine, Iva is isovaline, Hyp is hydroxyproline, Phe-ol is phenylalaninol, Phe-al is phenylalaninal, Phe is phenylalanine, Gly is glycine, Leu is leucine, Gin is glutamine, Pro is proline, lie is isoleucine, Thr is threonine and Ser is serine.