- Methods for the production of peptide derivatives
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The invention relates to methods for the preparation of peptides which are a C-terminal amide derivatives by a combination of solid-phase synthesis and post assembly solution phase synthesis. The peptides which are a C-terminal amide derivatives are further converted to peptide acetates. The invention also relates to pure peptide acetates and to protected peptide precursors.
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Page/Page column 17
(2010/11/25)
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- Synthesis and biological activity of some analogs of the gonadotropin releasing hormone
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Twenty one analogs of gonadotropin releasing hormone 2 (GnRH), were synthesized by the solid phase method. The derivatives were 3 (GnRH methyl ester), GnRH N methyl amide, GnRH free acid, 2 (Gn RH N terminal hexapeptide), and also [Ac Ala1], [Ac gly1], [D 1], [Pro1], [Arg2], [Tyr(Me)3], [Ser5], [des Gly6], [Sar6], [des Pro9], [des Gly10, Pro NH29], [des Gly10, Pro NHC2H59], [Tyr11], [Tyr(Me)35], [des His2, des Pro9], [des His2, Sar6], and [Sar6 des Tyr5] GnRH. All analogs were purified at both the protected and the deblocked stage. The final products were characterized by chemical and physical methods and assayed in vitro for both LH and FSH release using rat pituitaries. Those derivatives which showed less than 0.2% of the activity of GnRH itself were further tested for inhibition of gonadotropin release.
- Arnold,Flouret,Morgan,Rippel,White
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p. 314 - 319,315, 316
(2007/10/05)
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