87700-75-2Relevant academic research and scientific papers
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA)
Venkatraj, Muthusamy,Messagie, Jonas,Joossens, Jurgen,Lambeir, Anne-Marie,Haemers, Achiel,Van Der Veken, Pieter,Augustyns, Koen
, p. 1557 - 1568 (2012/04/17)
Recent drug discovery programs targeting urokinase plasminogen activator (uPA) have resulted in nonpeptidic inhibitors consisting of amidine or guanidine functional groups attached to aromatic or heteroaromatic scaffolds. There is a general problem of poor oral bioavailability of these charged inhibitors. In this paper, we report the synthesis and evaluation of a series of naphthamide and naphthalene sulfonamides as uPA inhibitors containing non-basic groups as substitute for amidine or guanidine groups.
Kinetics of Reaction of Substituted Naphthoyl Chlorides with Aniline
Ananthakrishnanadar, P.,Varghesedharumaraj, G.
, p. 506 - 507 (2007/10/02)
Rate constants for the reactions of aniline with 6- and 3-substituted 2-naphthoyl chlorides and 6- and 4-substituted 1-naphthoyl chlorides have been measured at several temperatures in benzene solution.The Hammett equation applies very well in all these cases.The p values for the reaction with 6-substituted 2-naphthoyl chlorides are 1.38, 1.31 and 1.26 at 30, 35 and 40 deg C respectively and those for the reaction with 6- and 4-substituted 1-naphthoyl chlorides are 1.28, 1.24 and 1.19 at 30, 35 and 40 deg C respectively.The reaction of 3-substituted 2-naphthoyl chlo-rides also adheres to the Hammett equation with ?p constants, giving a p value of 1.55 at 30 deg C.
