Synthesis, Biological Evaluation, and Structure–Activity Relationships of N-Benzoyl-2-hydroxybenzamides as Agents Active against P. falciparum (K1 strain), Trypanosomes, and Leishmania
摘要:
In our efforts to identify novel chemical scaffolds for the development of new antiprotozoal drugs, a compound library was screened against Toxoplasma gondii tachyzoites with activity discovered for N-(4-ethylbenzoyl)-2-hydroxybenzamide la against T. gondii as described elsewhere. Synthesis of a compound set was guided by T. gondii SAR with 1r found to be superior for T. gondii, also active against Thai and Sierra Leone strains of Plasmodium falciparum, and with superior ADMET properties as described elsewhere. Herein, synthesis methods and details of the chemical analysis of the compounds in this series are described. Further, this series of N-benzoyl-2-hydroxybenzamides was repurposed for testing against four other protozoan parasites: Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and P. falciparum (K1 isolate). Structure-activity analyses led to the identification of compounds in this set with excellent antileishmanial activity (compound 1d). Overall, compound 1r was the best and had activity 21-fold superior to that of the standard antimalarial drug chloroquine against the K1 P. falciparum isolate.
POLYCARBONATE RESIN COMPOSITION CONTAINING TRIAZINE COMPOUND AND MOLDED ARTICLE USING THE SAME
申请人:Kitagawa Takashi
公开号:US20110077331A1
公开(公告)日:2011-03-31
A polycarbonate resin composition comprising a compound represented by the following formula (1):
wherein each of R
1a
, R
1b
, R
1c
, R
1d
and R
1e
independently represents a hydrogen atom or a monovalent substituent provided that OH is excluded, at least one of the substituents represents a substituent having a Hammett's σp value of 0.3 or more, and the substituents may be combined each other to form a ring; and each of R
1g
, R
1h
, R
1i
, R
1j
, R
1k
, R
1m
, R
1n
and R
1p
independently represents a hydrogen atom or a monovalent substituent, and the substituents may be combined each other to form a ring.
POLYESTER RESIN COMPOSITION
申请人:Watanabe Yukie
公开号:US20120301696A1
公开(公告)日:2012-11-29
To provide a polyester resin composition being able to maintain a long-wavelength ultraviolet-blocking effect for a long period of time, ensuring high solubility for a solvent, and having excellent light resistance.
A polyester resin composition comprising a compound represented by the following formula (1) and a polyester resin:
wherein each of R
1a
, R
1b
, R
1c
, R
1d
and R
1e
independently represents a hydrogen atom or a monovalent substituent excluding OH, at least one of the substituents represents a substituent having a positive Hammett's σp value, and the substituents may combine with each other to form a ring; and each of R
1g
, R
1h
, R
1i
, R
1j
, R
1k
, R
1m
, R
1n
and R
1p
independently represents a hydrogen atom or a monovalent substituent, and the substituents may combine with each other to form a ring.