Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents

J M Elliott; M A Cascieri; G Chicchi; S Davies; F J Kelleher; M Kurtz; T Ladduwahetty; R T Lewis; A M MacLeod; K J Merchant; S Sadowski; G I Stevenson

doi:10.1016/s0960-894x(98)00320-5

Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1845-50. doi: 10.1016/s0960-894x(98)00320-5.

Authors

J M Elliott¹, M A Cascieri, G Chicchi, S Davies, F J Kelleher, M Kurtz, T Ladduwahetty, R T Lewis, A M MacLeod, K J Merchant, S Sadowski, G I Stevenson

Affiliation

¹ Merck Sharp and Dohme Research Laboratories, Neuroscience Research Center, Harlow, Essex, U.K. [email protected]

PMID: 9873445
DOI: 10.1016/s0960-894x(98)00320-5

Abstract

A series of novel serine derived NK1 antagonists is described. The effect of variations in the N-benzyl, O-benzyl and serine groups are used to define the elements which are necessary for binding.

MeSH terms

Neurokinin-1 Receptor Antagonists*
Piperidines / chemistry
Piperidines / pharmacology*
Serine / chemistry*
Stereoisomerism
Structure-Activity Relationship

Substances

Neurokinin-1 Receptor Antagonists
Piperidines
Serine