Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives

Heuisul Park; Kyeongsik Min; Hyo-Shin Kwak; Ki Dong Koo; Dongchul Lim; Sang-Won Seo; Jae-Ung Choi; Bettina Platt; Deog-Young Choi

doi:10.1016/j.bmcl.2008.03.081

Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives

Heuisul Park, Kyeongsik Min, Hyo-Shin Kwak, Ki Dong Koo, Dongchul Lim, Sang-Won Seo, Jae-Ung Choi, Bettina Platt, Deog-Young Choi

Medical Sciences

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23 Citations (Scopus)

Abstract

We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modi. cation of P3, P1, and P2' and combination of SAR display a > 100-fold increase in potency with good cellular activity (IC50 = 0.15 mu M) relative to the previously reported compound 3. (C) 2008 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	2900-2904
Number of pages	5
Journal	Bioorganic & Medicinal Chemistry
Volume	18
Issue number	9
Early online date	8 Apr 2008
DOIs	https://doi.org/10.1016/j.bmcl.2008.03.081
Publication status	Published - 1 May 2008

Keywords

Alzheimer's disease
BACE-1
cyclic urea
beta-secretase
Alzheimers-disease
design

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10.1016/j.bmcl.2008.03.081

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title = "Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives",

abstract = "We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modi. cation of P3, P1, and P2' and combination of SAR display a > 100-fold increase in potency with good cellular activity (IC50 = 0.15 mu M) relative to the previously reported compound 3. (C) 2008 Elsevier Ltd. All rights reserved.",

keywords = "Alzheimer's disease, BACE-1, cyclic urea, beta-secretase , Alzheimers-disease, design",

author = "Heuisul Park and Kyeongsik Min and Hyo-Shin Kwak and Koo, {Ki Dong} and Dongchul Lim and Sang-Won Seo and Jae-Ung Choi and Bettina Platt and Deog-Young Choi",

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T1 - Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives

AU - Park, Heuisul

AU - Min, Kyeongsik

AU - Kwak, Hyo-Shin

AU - Koo, Ki Dong

AU - Lim, Dongchul

AU - Seo, Sang-Won

AU - Choi, Jae-Ung

AU - Platt, Bettina

AU - Choi, Deog-Young

PY - 2008/5/1

Y1 - 2008/5/1

N2 - We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modi. cation of P3, P1, and P2' and combination of SAR display a > 100-fold increase in potency with good cellular activity (IC50 = 0.15 mu M) relative to the previously reported compound 3. (C) 2008 Elsevier Ltd. All rights reserved.

AB - We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modi. cation of P3, P1, and P2' and combination of SAR display a > 100-fold increase in potency with good cellular activity (IC50 = 0.15 mu M) relative to the previously reported compound 3. (C) 2008 Elsevier Ltd. All rights reserved.

KW - Alzheimer's disease

KW - BACE-1

KW - cyclic urea

KW - beta-secretase

KW - Alzheimers-disease

KW - design

U2 - 10.1016/j.bmcl.2008.03.081

DO - 10.1016/j.bmcl.2008.03.081

M3 - Article

SN - 0968-0896

VL - 18

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JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 9

ER -

Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives

Abstract

Keywords

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