Antimalarial Activities of New Guanidylimidazole and Guanidylimidazoline Derivatives
摘要:
A series of new guanidylimidazole derivatives was prepared and evaluated in mice and Rhesus monkeys infected with malarial sporozoites. The majority of the new compounds showed poor metabolic stability and weak in vitro activities in three clones of Plasmodium falciparum. Compounds 8a, 8h, 9a, 16a, and 16e cured the mice infected with sporozoites of P. berghei at 160 and 320 mg/kg/day x 3 po. Compounds 8a showed better causal prophylactic activity than primaquine, tafenoquine, and Malarone in the Rhesus test. In the radical curative test, 8a cured one monkey and delayed relapse of another for 74 days at 30 mg/kg/day x 7 by im. By oral dosing, 8a delayed relapse 81 days for one and 32 days for other vs 11-12 days for control monkeys treated with 10 mg/kg of chloroquine by po alone. Compound 8h, which showed superior activity to 8a in mouse test, delayed the relapse of treated monkeys for 21-26 days at 30 mg/kg/day x 7 by oral.
HYBRID BLOCK COPOLYMER MICELLES WITH MIXED STEREOCHEMISTRY FOR ENCAPSULATION OF HYDROPHOBIC AGENTS
申请人:SILL Kevin N.
公开号:US20080274173A1
公开(公告)日:2008-11-06
The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.
本发明涉及聚合物化学领域,更具体地说是涉及多嵌段共聚物以及包含该共聚物的胶束。
OUAST, H.;NAHR, U., CHEM. BER., 1984, 117, N 8, 2761-2778
作者:OUAST, H.、NAHR, U.
DOI:——
日期:——
Covalent modification of metal surfaces
申请人:Breitenkamp Kurt
公开号:US20080035243A1
公开(公告)日:2008-02-14
The present invention provides modified metal surfaces, methods of preparing the same, and intermediates thereto. These materials are useful in a variety of applications including biomaterials.
ENCAPSULATED AMYLOID-BETA PEPTIDES
申请人:Breitenkamp Kurt
公开号:US20080274965A1
公开(公告)日:2008-11-06
The present invention relates to the field of polymer chemistry and more particularly to encapsulated peptides and uses thereof.
ENCAPSULATED CONTRAST AGENTS
申请人:Skaff Habib
公开号:US20090092554A1
公开(公告)日:2009-04-09
The present invention relates to the field of polymer chemistry and more particularly to encapsulated contrast agents and methods for using the same.