118499-85-7Relevant academic research and scientific papers
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes
Patrick, Donald A.,Bakunov, Stanislav A.,Bakunova, Svetlana M.,Suresh Kumar,Chen, Heidi,Jones, Susan Kilgore,Wenzler, Tanja,Barzcz, Todd,Werbovetz, Karl A.,Brun, Reto,Tidwell, Richard R.
experimental part, p. 3543 - 3551 (2009/12/04)
A series of 37 dicationically substituted bis(phenoxymethyl)benzene bis(phenoxymethyl)naphthalene, and bis(benzyloxy)naphthalene analogues of pentamidine was prepared and evaluated for antiprotozoal activities and cytotoxicity in in vitro. 1,3-Bis(4-amidinophenoxymethyl)benzene (1) was the most active against Trypanosoma brucei rhodesiense (IC50 = 2.1 nM). 1,3-Bis[4-(N-isopropylamidino)phenoxymethyl]benzene (2) was most active against Plasmodium falciparum (IC50 = 3.6 nM) and displayed a selectivity index more than 50 times greater than that of pentamidine. Several other compounds displayed lower antiplasmodial IC50 values and higher selectivity indices relative to pentamidine. 1,4-Bis(4-amidinophenoxymethyl)benzene (14) was the most active against Leishmania donovani (IC50 = 1.3 μM). Compound 2 displayed the greatest activity against T. b. rhodesiense in vivo, curing three of four infected mice dosed intraperitoneally at 5 mg/kg × 4 days.
Antiparasitic Agents: Part VI - Synthesis of 1,2-, 1,3,- and 1,4-Bis(4-substituted aryloxy)benzenes and their Biological Activities
Chauhan, P. M. S.,Niyer, R.,Bhakuni, D. S.,Shankhdhar, V.,Guru, P.Y.,Sen, A. B.
, p. 38 - 42 (2007/10/02)
Several 1,2-, 1,3-, 1,4-bis(4-amidinophenoxy)benzenes (8-10); 1,2-, 1,3-, 1,4-bis(4-amidinobenzyloxy)benzenes (14-16) and 1,2-, 1,3-, 1,4-bis(4-amidinophenoxymethyl)benzenes (26-28) and the corresponding amidoximes (17-19), (29-31) and 33 have been synthe
