Discovery of a series of potent, orally active α,α- disubstituted piperidine NK1 antagonists

Dong Xiao; Cheng Wang; Anandan Palani; Hon Chung Tsui; Gregory Reichard; Sunil Paliwal; Neng Yang Shih; Robert Aslanian; Ruth Duffy; Jean Lachowicz; Geoffrey Varty; Cynthia Morgan; Fei Liu; Amin Nomeir

doi:10.1016/j.bmcl.2010.08.059

Discovery of a series of potent, orally active α,α- disubstituted piperidine NK₁ antagonists

Dong Xiao
, Cheng Wang
, Anandan Palani
, Hon Chung Tsui
, Gregory Reichard
, Sunil Paliwal
, Neng Yang Shih
, Robert Aslanian
, Ruth Duffy
, Jean Lachowicz
, Geoffrey Varty
, Cynthia Morgan
, Fei Liu
, Amin Nomeir

Department of Chemistry and Chemical Biology

Merck

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

Modification of prototype NK₁ antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK₁ antagonists.

Original language	English
Pages (from-to)	6313-6315
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	21
DOIs	https://doi.org/10.1016/j.bmcl.2010.08.059
State	Published - 1 Nov 2010

Keywords

Dibasic amine metabolite
NK antagonist

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10.1016/j.bmcl.2010.08.059

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Xiao, D., Wang, C., Palani, A., Tsui, H. C., Reichard, G., Paliwal, S., Shih, N. Y., Aslanian, R., Duffy, R., Lachowicz, J., Varty, G., Morgan, C., Liu, F., & Nomeir, A. (2010). Discovery of a series of potent, orally active α,α- disubstituted piperidine NK₁ antagonists. Bioorganic and Medicinal Chemistry Letters, 20(21), 6313-6315. https://doi.org/10.1016/j.bmcl.2010.08.059

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title = "Discovery of a series of potent, orally active α,α- disubstituted piperidine NK1 antagonists",

abstract = "Modification of prototype NK1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK1 antagonists.",

keywords = "Dibasic amine metabolite, NK antagonist",

author = "Dong Xiao and Cheng Wang and Anandan Palani and Tsui, \{Hon Chung\} and Gregory Reichard and Sunil Paliwal and Shih, \{Neng Yang\} and Robert Aslanian and Ruth Duffy and Jean Lachowicz and Geoffrey Varty and Cynthia Morgan and Fei Liu and Amin Nomeir",

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doi = "10.1016/j.bmcl.2010.08.059",

language = "English",

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pages = "6313--6315",

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Xiao, D, Wang, C, Palani, A, Tsui, HC, Reichard, G, Paliwal, S, Shih, NY, Aslanian, R, Duffy, R, Lachowicz, J, Varty, G, Morgan, C, Liu, F & Nomeir, A 2010, 'Discovery of a series of potent, orally active α,α- disubstituted piperidine NK₁ antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 21, pp. 6313-6315. https://doi.org/10.1016/j.bmcl.2010.08.059

TY - JOUR

T1 - Discovery of a series of potent, orally active α,α- disubstituted piperidine NK1 antagonists

AU - Xiao, Dong

AU - Wang, Cheng

AU - Palani, Anandan

AU - Tsui, Hon Chung

AU - Reichard, Gregory

AU - Paliwal, Sunil

AU - Shih, Neng Yang

AU - Aslanian, Robert

AU - Duffy, Ruth

AU - Lachowicz, Jean

AU - Varty, Geoffrey

AU - Morgan, Cynthia

AU - Liu, Fei

AU - Nomeir, Amin

PY - 2010/11/1

Y1 - 2010/11/1

N2 - Modification of prototype NK1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK1 antagonists.

AB - Modification of prototype NK1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK1 antagonists.

KW - Dibasic amine metabolite

KW - NK antagonist

UR - https://www.scopus.com/pages/publications/77957872554

UR - https://www.scopus.com/pages/publications/77957872554#tab=citedBy

U2 - 10.1016/j.bmcl.2010.08.059

DO - 10.1016/j.bmcl.2010.08.059

M3 - Article

C2 - 20846861

AN - SCOPUS:77957872554

SN - 0960-894X

VL - 20

SP - 6313

EP - 6315

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 21

ER -

Discovery of a series of potent, orally active α,α- disubstituted piperidine NK₁ antagonists

Abstract

Keywords

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