Journal of Medicinal Chemistry p. 1394 - 1398 (1985)
Update date:2022-07-29
Topics:
Alhaider, Abdulqader A.
Abbdelkader, M. Atef
Lien, Eric J.
This work represents the design, synthesis, and pharmacological testing of 4-phenylquinoline derivatives as potential antidepressants.Various modifications of substituents at the 2-position of the quinoline ring were tried, and two main series of derivatives were synthesized.In the first series, an open (dialkylamino)alkyl chain is linked to the 2-position of the quinoline ring by isosteres.The second approach involved the synthesis of a novel analogue of trazodone with a 4-phenylquinoline grouping replacing the chlorophenyl group of trazodone.The potential antidepressant activity of these new compounds has been demonstrated by their antagonism to the reserpine-induced hypothermia in mice.Both length of the side chain and isosteric displacements within the side chain affect the value of the ED50 obtained.Compounds having three atoms separating the terminal nitrogen from the quinoline ring were found to be more active than those with four atoms.The 2-thia derivatives were devoid of antidepressant activity.Replacement of the open side chain at the 2-position of the quinoline ring by piperazine or substituted piperazines resulted in new compounds that are slightly more potent than imipramine.
View MoreContact:+(852) 301-98033
Address:Flat C, 23/F, Lucky Plaza, 315-321 Lockhart Road, Wan Chai, Hong Kong
website:http://www.mingchem.com/en/index
Contact:0519-85170101-802
Address:Fifth Floor,B of Beihua Buliding,520 Road of Science and Education City,Changwu middle road NO.801,Wujin District,Changzhou,Jiangsu province
Nanjing Fayekong Chemcial Co.,Ltd(expird)
Contact:86-25-58813444
Address:Rm 1503, Unit 1, Building 5, Zijinnanyuan, Nanjing, Jiangsu, China
Valiant Fine Chemicals Co., Ltd.
Contact:+86 535 6101878/6374484
Address:11 Wuzhishan Rd.,YTETDZ,Yantai,264006,Shandong,China
Yangling Ciyuan biotech Co., Ltd.
Contact:86-15802970736
Address:2-1804, International Park Mansion, No.2, South Fengdeng Road, Lianhu District
Doi:10.1016/S0040-4039(00)61920-2
(1985)Doi:10.1016/S0040-4039(00)85961-4
(1983)Doi:10.1039/jr9490002035
(1949)Doi:10.1021/ja01548a033
(1958)Doi:10.1002/jps.2600740817
(1985)Doi:10.1039/c7gc02838e
(2017)