Glycosyl derivatives of NK2 tachykinin receptor antagonists

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Abstract

The influence of glycosylation on the structure-activity relationship of the tachykinin antagonist MEN 10376 and of its minimal active fragment MEN 10414 was investigated. The antagonist activity was preserved only when β-d-glucosylated Tyr, Ser and Asn were added to the N-terminal position of MEN 10376, while the modification of the side chain of the Tyr2 induced a dramatic decrease in affinity.

The syntheses and the activity on RPA and HT of some glycopeptides of NK2 tachykinin receptor antagonists are reported.

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