Journal of Medicinal Chemistry p. 2403 - 2409 (1986)
Update date:2022-09-26
Topics:
Peet, Norton P.
Baugh, Larry E.
Sunder, Shyam
Lewis, Jon E.
Matthews, Emily H.
et al.
Syntheses for 3-(1H-tetrazol-5-yl)-4(3H)-quinazolinone sodium salt monohydrate (9; MDL 427) and the related formamido compound, 2-(formylamino)-N-1H-tetrazol-5-ylbenzamide (10), are described.Both compounds are active in the rat passive cutaneous anaphylaxis and passive peritoneal anaphylaxis tests.A 94:6 equilibrium mixture of 9 and ionized 10, respectively, forms in aqueous buffer systems at a pH-dependent rate.In addition, analogues of 3-(1H-tetrazol-5-yl)-4(3H)-quinazolinone (8) bearing substituents on the benzene ring, substituents at the 2-position, and heteroaryl groups at the 3-position other than tetrazole were prepared.These analogue sets demonstrated that an accessible electrophilic center and an acidic functionality were requirements for good antiallergic activity.
View MoreContact:+(852) 301-98033
Address:Flat C, 23/F, Lucky Plaza, 315-321 Lockhart Road, Wan Chai, Hong Kong
Contact:410-273-7300; 800-221-3953
Address:4609 Richlynn Dr., PO Box 369, Belcamp, MD, 21017-0369, USA
Engineering Research Center of Pesticide, Heilongjiang Province
Contact:+86-451-86609001
Address:No.74 of Xuefu Road, Nangang District,
website:http://www.guarson.com
Contact:+86-523-88059600,+86-13805268803
Address:Room B1006,Yafang Building,Jiangyan Avenue,Jiangyan District, Taizhou City,Jiangsu,China
Tianjin Ingenochem Technology Co.,Ltd
Contact:+86-22-23677060
Address:Hitech Green Industry Park K2-9-602, Nankai district
Doi:10.1007/BF00953932
(1985)Doi:10.1016/j.tet.2019.06.035
(2019)Doi:10.1021/ja00374a047
(1982)Doi:10.1002/ejoc.200701224
(2008)Doi:10.1246/bcsj.73.2283
(2000)Doi:10.1002/ardp.201300255
(2014)
