European Journal of Medicinal Chemistry p. 419 - 425 (2018)
Update date:2022-08-10
Topics:
Zhu, Wanping
Liu, Xia
Wang, Yuji
Tong, Yeling
Hu, Yongzhou
A series of novel α-terpineol derivatives were designed and synthesized through structural derivatization of the tertiary hydroxyl moiety or reduction of the double bond. Of the resulting compounds, eight compounds enhanced relaxation of airway smooth muscle (ASM) compared to the α-terpineol precursor, and four compounds (4a, 4d, 4e, and 4i)were superior or comparable to aminophylline at a concentration of 0.75 mmol/L. Assays for 3′-5′-Cyclic adenosine monophpsphate (cAMP) activation revealed that some representative α-terpineol derivatives in this series were capable of upregulating the level of cAMP in ASM cells. Further in vivo investigation using the asthmatic rat model, illustrated that treatment with the compounds 4a and 4e resulted in significantly lowered lung resistance (RL) and enhanced dynamic lung compliance (Cldyn), two important parameters for lung fuction. Moreover, treatment with 4e downregulated the levels of both IL-4 and IL-17. Due to its several favorable physiological functions, including ASM relaxation activity, cAMP activation capability, and in vivo anti-asthmatic efficacy, 4e is a promising remedy for bronchial asthma, meriting extensive development.
View MoreJiangxi Hito Chemical Co., Ltd.
Contact:+86-792-3170318
Address:No. 6, Tianhong Ave., Xinghuo Industry Park, Yongxiu, Jiujiang, Jiangxi, China
Jinan Jiaquan Chemical Co.,Ltd
Contact:+86-531-62318366
Address:Room 502 of Yidonghuayuan No.601 Huaxin Road Licheng District Jinan China
Meryer (Shanghai) Chemical Technology Co., Ltd.
website:http://www.meryer.com/cn/index/
Contact:+86-755-86170518
Address:Minhang,Shanghai, China
Contact:+86-0760-85282375
Address:zhongjing road,zhongshan torch hi-tech industrial development zone
Geen Chemical Technology Co., Ltd
Contact:86-769-21660847
Address:1408, Yingfeng Commercial Center, Nancheng District
Doi:10.1039/c5cy01607j
(2016)Doi:10.1021/jo01076a042
(1960)Doi:10.1007/BF01920719
(1996)Doi:10.1007/s11164-018-3351-y
(2018)Doi:10.1081/SCC-120034174
(2004)Doi:10.1021/jo0108111
(2001)