推荐产品
SMILES字符串
CCC1=NC(N)=NC(N)=C1C2=CC=C(Cl)C=C2
InChI
1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)
InChI key
WKSAUQYGYAYLPV-UHFFFAOYSA-N
基因信息
human ... CYP2C9(1559) , DHFRP1(573971)
rat ... Dhfr(24312)
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Warning
危险声明
危险分类
Acute Tox. 4 Oral
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
法规信息
新产品
Journal of medicinal chemistry, 54(14), 5116-5130 (2011-06-08)
Starting from a hit series from a GNF compound library collection and based on a cell-based proliferation assay of Plasmodium falciparum, a novel imidazolopiperazine scaffold was optimized. SAR for this series of compounds is discussed, focusing on optimization of cellular
Antimicrobial agents and chemotherapy, 54(6), 2603-2610 (2010-03-31)
Drug resistance against dihydrofolate reductase (DHFR) inhibitors-such as pyrimethamine (PM)-has now spread to almost all regions where malaria is endemic, rendering antifolate-based malaria treatments highly ineffective. We have previously shown that the di-amino quinazoline QN254 [5-chloro-N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine] is active against the
Journal of medicinal chemistry, 54(11), 3935-3949 (2011-04-27)
Malaria is one of the leading causes of severe infectious disease worldwide; yet, our ability to maintain effective therapy to combat the illness is continually challenged by the emergence of drug resistance. We previously reported identification of a new class
Antimicrobial agents and chemotherapy, 54(9), 3927-3932 (2010-06-23)
Plasmodium vivax resistance to antifolates is prevalent throughout Australasia and is caused by point mutations within the parasite dihydrofolate reductase (DHFR)-thymidylate synthase. Several unique mutations have been reported in P. vivax DHFR, and their roles in resistance to classic and
Journal of medicinal chemistry, 54(13), 4581-4589 (2011-06-08)
A novel class of antimalarial pyrido[1,2-a]benzimidazoles were synthesized and evaluated for antiplasmodial activity and cytotoxicity following hits identified from screening commercially available compound collections. The most active of these, TDR86919 (4c), showed improved in vitro activity vs the drug-resistant K1
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