Pharmaceuticals ergot alkaloids

An extremely important aspect in pharmaceutical research is the determination of drug optical purity. The most frequently applied technique for chiral separations in CZE remains the so-called dynamic mode where resolution of enantiomers is carried out by adding a chiral selector directly into the BGE for in situ formation of diastereomeric derivatives. Various additives, such as cyclodextrins (CD), chiral crown ethers, proteins, antibiotics, bile salts, chiral micelles, and ergot alkaloids, are reported as chiral selectors in the literature, but CDs are by far the selectors most widely used in chiral CE. 

The primary aim of this chapter is to demonstrate different strategies, chemical and chemo-enzymatic, for the preparation of glycosides of pharmaceutically active and broadly used compounds - ergot alkaloids. New glycosides prepared recently have interesting immunomodulatory, neuroactive and cytostatic activity. 

HPLC ANALYSIS ERGOT ALKALOIDS IN PHARMACEUTICAL PREPARATIONS ... 

Ogunlana, O.E., Ramstad, E., Tyler, V.E. Effects of Some Substances on Ergot Alkaloid Production Journal of Pharmaceutical Sciences (1969) 58 (1) 143-... 

Alkaloids are always compounds isolated from nature. However, there are many examples of alkaloid derivatives with a high profile which may be confused and sometimes classified as alkaloids. For example, Lyserg Saure Diathylamid (LSD) (LSD-25) is prepared by the amidation of lysergic acid, itself derived from the ergot alkaloids. Methamphetamine is prepared by the reduction of (-)-ephedrine, and heroin is prepared by the acetylation of morphine, and there are many derivatives of alkaloids which are pharmaceutical products. These semisynthetic compounds can be classed as alkaloid derivatives. 

TLC has been applied to studies of chemical reactions of ergot alkaloids [90, 223] the configuration of lysergic acid [224] biogenesis of the ergot alkaloids [79, 80, 140] pharmaceutical preparations [68]. 

Therapeutically Significant Ergot Alkaloids and Those as Potential Pharmaceuticals... 

Semisynthetic Modifications of Natural Ergot Alkaloids Yield Significant Pharmaceuticals... 

This group includes simple lysergic acid amides and peptide ergot alkaloids. Most of these substances are directly used in pharmaceutical preparations. However, reports referring to their biotransformation are scarce. 

Takeda Pharmaceutical Industries (1956) Water-soluble ergot alkaloid, elymoclavine. GB pat. 757 696. 

All the therapeutically used ergot alkaloids and their derivatives are described in the following part of the chapter. The main qualitative requirements of actual world leading pharmacopoeias (Enr. Ph. 1997, USP 23 and JP XIII), in which the substances have been incorporated and the names of pharmaceutical specialities with ergot alkaloids (Negwer, 1994) are presented here. 

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