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 - http://www.scopus.com/inward/record.url?scp=77957872554&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=77957872554&partnerID=8YFLogxK
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 -