
Bioorganic and Medicinal Chemistry p. 2173 - 2183 (1997)
Update date:2022-07-29
Topics:
Gustavsson, Anna-Lena
Larsson, Mattias C.
Hansson, Bill S.
Liljefors, Tommy
The enantiomers of cis- and trans-3-(4-propyl-cyclopent-2-enyl) propyl acetate, which are conformationally constrained analogues of (Z)-5-decenyl acetate (1), a sex pheromone component of the turnip moth, Agrotis segetum, have been synthesized and tested using the elcctrophysiological single-sensillum technique. The analogues mimic a cisoid and transoid conformation of 1, respectively. In addition, the enantiomers of each of the cis- and trans-isomers are conformationally constrained analogues of enantiomeric cisoid and transoid conformations of 1. Thus, the compounds prepared and tested are well suited to investigate the nature of the bioactive conformation of the natural pheromone component 1 and the chiral sense of its interaction with the receptor. Electrophysiological single-sensillum recordings show that the activity of the most active cis-isomer, which has a (1S,4R)-configuration, is more than two orders of magnitude higher than that of the most active trans-isomer. Furthermore, the (1S,4R)-isomer is at least 100 times more active than its enantiomer. These results strongly support a previously proposed cisoid bioactive conformation of 1. Furthermore, the (1S,4R)-configuration of most active stereoisomer identifies the chiral sense of the interaction between the natural pheromone component 1 and its receptor.
View MoreHangzhou Yingshanhua Pigment Chemicals Co.,Ltd.
Contact:+86-0150-58101658
Address:Nanyang Economic DevelopmentZong,Xiaoshan,Hangzhou,China
Shandong Jusage Technology Co.,Ltd.
Contact:86-13406130167
Address:No.20,North Ride No.9 Road, Guangrao Economic Development Zone, Shandong Province
Shangyu Sanhechemicals Co.,LTD.
Contact:86-0571-56696839
Address:Num.2952,Nanhuan Road,Binjiang District,Hangzhou,China
Liao Cheng All Win Chemicals Co.,LTD
Contact:86+0635-2991582
Address:Room 402,Unit 1,No.27 building.Zhong tong shi dai haoyuan,liaocheng city,Shan dong Province.China
Shanghai Xinda Pharmaceuticals Co., Ltd.
Contact:86-21-33692333-8008
Address:999 Linxian Road, Jinshan Industrial Park, Shanghai, China
Doi:10.1248/cpb.45.2085
(1997)Doi:10.1016/S0040-4020(97)10359-3
(1998)Doi:10.1021/jm101299d
(2011)Doi:10.1021/jo035391p
(2004)Doi:10.1016/S0040-4039(97)10647-5
(1998)Doi:10.1016/S0040-4039(97)10734-1
(1998)