170993-41-6Relevant academic research and scientific papers
Synthesis and structure-activity relationships of novel fused ring analogues of Q203 as antitubercular agents
Kang, Sunhee,Kim, Young Mi,Jeon, Heekyung,Park, Sejin,Seo, Min Jung,Lee, Saeyeon,Park, Dongsik,Nam, Jiyeon,Lee, Seokwoo,Nam, Kiyean,Kim, Sanghee,Kim, Jaeseung
, p. 420 - 427 (2017/05/22)
A set of fused ring analogues of a new antitubercular agent, Q203, was designed and synthesized. To reduce the lipophilicity of Q203 caused by linearly extended side chains, shorter and heteroatoms containing fused rings were introduced into the side chain region. Antitubercular activity was tested against H37Rv-GFP replicating in liquid broth culture medium (extracellular) and within macrophages (intracellular). Many analogues showed potent extracellular activities as well as intracellular activities without cytotoxicity. Among them, compounds 18–21 displayed significant antitubercular activities with favorable metabolic stabilities. Representative compound 21 exhibited excellent in?vivo pharmacokinetic values at high drug exposure levels in the plasma, which makes this compound promising candidate for a new antitubercular drug.
NITROGENOUS CYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
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, (2008/06/13)
The present invention provides a novel compound having a superior calcium antagonism, in particular, a neuron-selective calcium antagonism. Namely, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, Ar indicates an optionally substituted 5- to 14-membered aromatic ring etc.; the ring A indicates any one ring selected from a piperazine, a homopiperazine, a piperidine and the like; the ring B indicates an optionally substituted C3-14 hydrocarbon ring etc.; E indicates a single bond, a group represented by the formula -CO-, etc.; X indicates a single bond, an oxygen atom etc.; R1 indicates a hydrogen atom, a halogen atom, a hydroxyl group etc.; and D1, D2, W1 and W2 are the same as or different from each other and each represents a single bond or an optionally substituted C1-6 alkylene chain.
