Journal of Medicinal Chemistry p. 2570 - 2579 (1991)
Update date:2022-08-04
Topics:
Francis, John E.
Webb, Randy L.
Ghai, Geetha R.
Hutchison, Alan J.
Moskal, Michael A.
et al.
A wide variety of 2-substituted aminoadenosines were prepared for comparison with the moderately A2 receptor selective adenosine agonist 2-anilinoadenosine (CV-1808).High selectivity combined with significant affinity at the A2 receptor in rat membranes was observed for those amines bearing a two-carbon chain to which was attached an aryl, heteroaryl, or alicyclic moiety. 2-(2-Phenethylamino)adenosine (3d), a 14-fold A2 selective compound, was modified by introduction of a variety of substituents in the benzene ring and the side chain.Some of these changes led to improved A2 affinity and increased selectivity.Replacement of the phenyl moiety by cyclohexenyl produced a 210-fold selective agonist 3ag (CGS 22989) whereas the cyclohexanyl analogue 3af (CGS 22492) was 530-fold selective at the A2 site.These compounds showed hypotensive activity in rat models over a range of doses without the bradycardia observed with less selective agonists.
View MoreShanghai Taibao Pharmaceutical Technology Co., Ltd
Contact:021-52217366
Address:shanghai
QINGDAO ON-BILLION INDUSTRAIL CO.,LTD
website:http://www.obn.com.cn
Contact:+86-15005320811 +86-532-80681989
Address:F35 Parkson Mansion No.44-60 Zhongshan Rd.
Contact:+91 9963263336
Address:Plot#146A, IDA Mallapur, Hyderabad - 500072
Shanghai Haoyuan Chemexpress Co., Ltd.
Contact:86-21-51870955;58998985;58999585
Address:Room 601, No. 2 BLD, NO. 720, Cailun Road, Zhangjiang, Shanghai, China
Contact:15973022782
Address:7-5-6218,Incubation Centre,Guandong Industry Park, East Lake High-Tech Development Zone,Wuhan City.
Doi:10.1016/j.saa.2019.117645
(2020)Doi:10.3390/molecules15063887
(2010)Doi:10.1016/j.saa.2014.09.124
(2015)Doi:10.1039/c0cc00297f
(2010)Doi:10.1021/es702671v
(2008)Doi:10.1016/j.crci.2013.08.007
(2014)