Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H1-receptor agonists

S. Elz; K. Kramer; H.H. Pertz; M. Detert; A.M. ter Laak; R Kuehne; W. Schunack

doi:10.1021/jm991056a

Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H1-receptor agonists

S. Elz
, K. Kramer
, H.H. Pertz
, M. Detert
, A.M. ter Laak
, R Kuehne
, W. Schunack

Research output: Contribution to Journal › Article › Academic › peer-review

Abstract

A new class of histamine analogues characterized by a 3,3-diphenylpropyl substituent at the 2-position of the imidazole nucleus has been prepared outgoing from 4,4-diphenylbutyronitrile (4b) via cyclization of the corresponding methyl imidate 5b with 2-oxo-4-phthalimido-1-butyl acetate or 2-oxo-1,4-butandiol in liquid ammonia, followed by standard reactions. The title compounds displayed partial agonism on contractile H

Original language	English
Pages (from-to)	1071-1084
Journal	Journal of Medicinal Chemistry
Volume	43
Issue number	6
DOIs	https://doi.org/10.1021/jm991056a
Publication status	Published - 2000

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10.1021/jm991056a

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title = "Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H1-receptor agonists",

abstract = "A new class of histamine analogues characterized by a 3,3-diphenylpropyl substituent at the 2-position of the imidazole nucleus has been prepared outgoing from 4,4-diphenylbutyronitrile (4b) via cyclization of the corresponding methyl imidate 5b with 2-oxo-4-phthalimido-1-butyl acetate or 2-oxo-1,4-butandiol in liquid ammonia, followed by standard reactions. The title compounds displayed partial agonism on contractile H",

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AU - Elz, S.

AU - Kramer, K.

AU - Pertz, H.H.

AU - Detert, M.

AU - ter Laak, A.M.

AU - Kuehne, R

AU - Schunack, W.

PY - 2000

Y1 - 2000

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AB - A new class of histamine analogues characterized by a 3,3-diphenylpropyl substituent at the 2-position of the imidazole nucleus has been prepared outgoing from 4,4-diphenylbutyronitrile (4b) via cyclization of the corresponding methyl imidate 5b with 2-oxo-4-phthalimido-1-butyl acetate or 2-oxo-1,4-butandiol in liquid ammonia, followed by standard reactions. The title compounds displayed partial agonism on contractile H

U2 - 10.1021/jm991056a

DO - 10.1021/jm991056a

M3 - Article

SN - 0022-2623

VL - 43

SP - 1071

EP - 1084

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 6

ER -

Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H1-receptor agonists

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