Journal of Medicinal Chemistry p. 349 - 368 (2020)
Update date:2022-08-15
Topics:
Martínez-Gualda, Belén
Sun, Liang
Martí-Marí, Olaia
Noppen, Sam
Abdelnabi, Rana
Bator, Carol M.
Quesada, Ernesto
Delang, Leen
Mirabelli, Carmen
Lee, Hyunwook
Schols, Dominique
Neyts, Johan
Hafenstein, Susan
Camarasa, María-José
Gago, Federico
San-Félix, Ana
Currently, there are only three FDA-approved drugs that inhibit human immunodeficiency virus (HIV) entry-fusion into host cells. The situation is even worse for enterovirus EV71 infection for which no antiviral therapies are available. We describe here the discovery of potent entry dual inhibitors of HIV and EV71. These compounds contain in their structure three or four tryptophan (Trp) residues linked to a central scaffold. Critical for anti-HIV/EV71 activity is the presence of extra phenyl rings, bearing one or two carboxylates, at the C2 position of the indole ring of each Trp residue. The most potent derivatives, 22 and 30, inhibit early steps of the replicative cycles of HIV-1 and EV-A71 by interacting with their respective viral surfaces (glycoprotein gp120 of HIV and the fivefold axis of the EV-A71 capsid). The high potency, low toxicity, facile chemical synthesis, and great opportunities for chemical optimization make them useful prototypes for future medicinal chemistry studies.
View MoreZibo Fuxi'er Chemical Co.,Ltd (Shanxian Fuxi'er Chemical Co.,Ltd)
Contact:+86-533-2091422
Address:Eastern 4 on the 3th Road ,Liangxiang Industrial Park, Zibo city ,Shandong,China
website:http://www.herbpurify.com
Contact:0086-028-85249238
Address:Room709-C1,Incubator Building, Tianfu Life Science Park No.88,Keyuan Road,Gaoxin district,Chengdu City,Sichuan Prov,China
website:http://www.win-winchemical.com
Contact:0086-577-64498589
Address:6F,No.396 Xingping Road,Longwan Industrial Zone
Compro Shijiazhuang Fine Chemical Co., Ltd
Contact:0086-311-89689838
Address:Economic and Technological Development Zone of Shijiazhuang,Hebei
Hebei Think-Do Environment Co., Ltd
website:http://www.thinkdo-environment.com
Contact:0311-86510809
Address:No 6, Shilian Middle Street, Circular Chemical Industry Park
Doi:10.1007/BF00899590
(1956)Doi:10.1039/c5ra26549e
(2016)Doi:10.1016/j.ejmech.2020.112966
(2021)Doi:10.1055/s-2008-1067168
(2008)Doi:10.1016/S0031-9422(00)85909-9
(1969)Doi:10.1021/ol070537i
(2007)