138107-19-4Relevant academic research and scientific papers
Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation
Singh, Amandeep,Rani, Anu,Gut, Jiri,Rosenthal, Philip J.,Kumar, Vipan
, p. 590 - 595 (2017)
A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41 to 2.38?μ
4-Aminoquinoline-ferrocenyl-chalcone conjugates: Synthesis and anti-plasmodial evaluation
Singh, Amandeep,Gut, Jiri,Rosenthal, Philip J.,Kumar, Vipan
, p. 269 - 277 (2017)
A series of aliphatic and aromatic substituted 1H-1,2,3-triazole-tethered 4-amino-quinoline-ferrocenylchalcone conjugates has been synthesized and evaluated for anti-plasmodial activity. The conjugates with flexible aliphatic (aminoethanol or aminopropano
Design, synthesis, and anti-proliferative evaluation of 1: H -1,2,3-triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates in estrogen responsive and triple negative breast cancer cells
Awolade, Paul,Cele, Nosipho,Gu, Liang,Kaur, Mandeep,Kumar, Vipan,Pillay, Ruvesh Pascal,Sharma, Bharvi,Singh, Parvesh
, p. 11137 - 11147 (2020/07/15)
A series of 1H-1,2,3 triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates were synthesized and in vitro evaluated against estrogen responsive (MCF-7) and triple negative (MDA-MB-231) breast cancer cells. Comparative analysis reve
Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease
Cheng, Maojun,Guo, Jie,Jiang, Neng,Li, Qing,Liang, Ningsheng,Liu, Jing,Nong, Xiaojie,Pang, Chengyun,Qin, Yuelian,Tang, Chunli,Tang, Weizhong,Xie, Sai-Sai,Zhang, Zhipeng
, (2020/07/10)
A series of rasagiline-clorgyline hybrids was designed, synthesized and investigated in vitro for their inhibition of monoamine oxidase and amyloid-β aggregation. Most of compounds were found to be selective and highly potent hMAO-B inhibitors showing IC50 values in the nanomolar, and exhibited a moderate inhibition of amyloid-β aggregation. 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one (6j) was the most interesting compound identified in this research, endowed with higher hMAO-B potency (IC50 = 4 nM) and selectivity (SI > 25000) compared to the reference selective inhibitor rasagiline (IC50 = 141 nM, SI > 355), and exhibited good inhibitory activity against Aβ1-42 aggregation (40.78percent, 25 μM). Kinetic and molecular modeling studies revealed that 6j was a competitive reversible inhibitor for hMAO-B. Moreover, compound 6j displayed low toxicity and good neuroprotective effects in SH-SY5Y cell assay, and could penetrate the blood-brain barrier according to the parallel artificial membrane permeability assay. Pharmacokinetics assay revealed that compound 6j possessed good pharmacokinetic profiles after intravenous and oral administrations. Overall, these results highlighted that compound 6j was an effective and promising multitarget agent against Alzheimer's disease.
Application of propynylamine derivative in pharmacy
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Paragraph 0046-0048, (2020/06/22)
The invention discloses application of a propynylamine derivative in pharmacy. Shown by tests of the applicant, the derivative can selectively inhibit MAO-B, is remarkable in activity and can be usedfor preparing MAO-B inhibitors and drugs for preventing
Propargylamine derivative and synthesis method thereof
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Paragraph 0037-0041, (2020/06/16)
The invention discloses a series of propargylamine derivatives and a synthesis method thereof. The synthesis method of the derivative mainly comprises the following steps: (1) putting any one of the structures shown in the following formulas (A)-(E) and e
Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands
Szczepańska, Katarzyna,Karcz, Tadeusz,Siwek,Kuder, Kamil J.,Latacz, Gniewomir,Bednarski,Szafarz, Ma?gorzata,Hagenow, Stefanie,Lubelska, Annamaria,Olejarz-Maciej, Agnieszka,Sobolewski, Micha?,Mika,Kotańska, Magdalena,Stark, Holger,Kie?-Kononowicz, Katarzyna
supporting information, (2019/07/31)
A novel series of 4-pyridylpiperazine derivatives with varying alkyl linker length and eastern part substituents proved to be potent histamine H3 receptor (hH3R) ligands in the nanomolar concentration range. While paying attention to
Efficacy of novel phenoxyalkyl pyridinium oximes as brain-penetrating reactivators of cholinesterase inhibited by surrogates of sarin and VX
Chambers, Janice E.,Chambers, Howard W.,Funck, Kristen E.,Meek, Edward C.,Pringle, Ronald B.,Ross, Matthew K.
, p. 154 - 159 (2016/12/06)
Pyridinium oximes are strong nucleophiles and many are effective reactivators of organophosphate-inhibited cholinesterase (ChE). However, the current oxime reactivators are ineffective at crossing the blood-brain barrier and reactivating brain ChE in the intact organism. Our laboratories have developed a series of substituted phenoxyalkyl pyridinium oximes (US patent 9,227,937 B2) with the goal of identifying reactivators effective in crossing the blood-brain barrier. The first 35 of the series were found to have similar in?vitro efficacy as reactivators of ChE inhibited by a sarin surrogate (phthalimidyl isopropyl methylphosphonate, PIMP) or a VX surrogate (nitrophenyl ethyl methylphosphonate, NEMP) in bovine brain preparations as previously observed in rat brain preparations. A number of these novel oximes have shown the ability to decrease the level of ChE inhibition in the brains of rats treated with a high sublethal dosage of either a sarin surrogate (nitrophenyl isopropyl methylphosphonate, NIMP) or the VX surrogate NEMP. Levels of reactivation at 2?h after oxime administration were up to 35% while the currently approved therapeutic, 2-PAM, yielded no reduction in brain ChE inhibition. In addition, there was evidence of attenuation of seizure-like behavior with several of the more effective novel oximes, but not 2-PAM. Therefore these novel oximes have demonstrated an ability to reactivate inhibited ChE in brain preparations from two species and in?vivo data support their ability to enter the brain and provide a therapeutic action. These novel oximes have the potential to be developed into improved antidotes for nerve agent therapy.
Generation of metallomesogens using common ligands functionalised with liquid-crystalline moieties
Shashikala, Indudhara S.,Bruce, Duncan W.
, p. 1128 - 1131 (2008/09/18)
Functionalisation of 2,2′-bipyridine or acetylacetone with an alkyleneoxycyanobiphenyl group induces liquid-crystalline properties in simple metal complexes. The Royal Society of Chemistry.
Multiple 1,2,3-Thiadiazoles
Al-Smadi, Mousa,Hanold, Norbert,Meier, Herbert
, p. 605 - 611 (2007/10/03)
A series of compounds 3a-d,i-n with two or three 1,2,3-thiadiazole rings, useful for photocrosslinking processes, was prepared from the di- or triketones 1a-d,i-n via the corresponding hydrazones 2a-d,i-n by applying the Hurd-Mori method. A special synthe
