53712-77-9Relevant academic research and scientific papers
ANTI-FUNGAL TREATMENT
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Paragraph 00117, (2018/03/25)
Provided are compounds, methods, and pharmaceutical compositions useful for treatment of fungal infections, e.g., aspergillosis, candidiasis, cryptococcosis, histoplasmosis, and the like. For example, the pharmaceutical composition may include a pharmaceutically acceptable carrier or excipient, and a compound represented by Ar— C(=NR1)NR2— A---X— Y— Het2 and pharmaceutically acceptable salts thereof. Ar may be an optionally substituted aryl or nitrogen- containing heteroaryl. R1 and R2 may independently be H, optionally substituted C1-C6 aikyi, or optionally substituted C3-C6 cyeloalkyi. A may be a bond or an optionally substituted linking moiety comprising 1, 2, or 3 rings. Each ring in the optionally substituted linking moiety may independently be one of: aryl, cyeloalkyi, heterocycloalkyl, and heteroaryl. X may be O, S, amide, or a bond. Y may be optionally substituted C1-C10 alkyi or optionally substituted C2-C10 alkenyl. Het2 may be an optionally substituted five-membered nitrogen-containing heteroaromatic ring comprising 1, 2, or 3 ring heteroatoms.
Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using
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Page/Page column 56, (2015/09/23)
Substituted 1,4,7-triazacyclononane-N,N′,N″-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N′,N″,N′″-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.
4-alkyloxyimino derivatives of uridine-5′-triphosphate: Distal modification of potent agonists as a strategy for molecular probes of P2Y 2, P2Y4, and P2Y6 receptors
Jayasekara, P. Suresh,Barrett, Matthew O.,Ball, Christopher B.,Brown, Kyle A.,Hammes, Eva,Balasubramanian, Ramachandran,Harden, T. Kendall,Jacobson, Kenneth A.
, p. 3874 - 3883 (2014/05/20)
Extended N4-(3-arylpropyl)oxy derivatives of uridine-5′-triphosphate were synthesized and potently stimulated phospholipase C stimulation in astrocytoma cells expressing G protein-coupled human (h) P2Y receptors (P2YRs) activated by UTP (P2Y2/4R) or UDP (P2Y6R). The potent P2Y4R-selective N4-(3- phenylpropyl)oxy agonist was phenyl ring-substituted or replaced with terminal heterocyclic or naphthyl rings with retention of P2YR potency. This broad tolerance for steric bulk in a distal region was not observed for dinucleoside tetraphosphate agonists with both nucleobases substituted. The potent N 4-(3-(4-methoxyphenyl)-propyl)oxy analogue 19 (EC50: P2Y2R, 47 nM; P2Y4R, 23 nM) was functionalized for chain extension using click tethering of fluorophores as prosthetic groups. The BODIPY 630/650 conjugate 28 (MRS4162) exhibited EC50 values of 70, 66, and 23 nM at the hP2Y2/4/6Rs, respectively, and specifically labeled cells expressing the P2Y6R. Thus, an extended N4-(3- arylpropyl)oxy group accessed a structurally permissive region on three G q-coupled P2YRs, and potency and selectivity were modulated by distal structural changes. This freedom of substitution was utilized to design of a pan-agonist fluorescent probe of a subset of uracil nucleotide-activated hP2YRs.
A highly effective bifunctional ligand for radioimmunotherapy applications
Chong, Hyun-Soon,Song, Hyun A.,Kang, Chi Soo,Le, Thien,Sun, Xiang,Dadwal, Mamta,Lee, Hyunbeom,Lan, Xiaoli,Chen, Yunwei,Dai, Anzhi
supporting information; experimental part, p. 5584 - 5586 (2011/06/21)
A novel bifunctional ligand (3p-C-NETA) for antibody-targeted radioimmunotherapy (RIT) of β-emitting radioisotopes 90Y and 177Lu was efficiently synthesized via an unexpected regiospecific ring opening of an aziridinium ion. 3p-C-NET
SIGMA-1 RECEPTOR LIGANDS AND METHODS OF USE
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Page/Page column 41-42, (2010/07/10)
The invention provides compounds of formula I and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.
Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors
Hajipour, Abdol R.,Fontanilla, Dominique,Chu, Uyen B.,Arbabian, Marty,Ruoho, Arnold E.
experimental part, p. 4397 - 4404 (2010/09/12)
The sigma-1 receptor is a unique non-opioid, non-PCP binding site that has been implicated in many different pathophysiological conditions including psychosis, drug addiction, retinal degeneration and cancer. Based on the structure of fenpropimorph, a hig
Ionic liquids on demand in continuous flow
Wilms, Daniel,Klos, Johannes,Kilbinger, Andreas F. M.,Loewe, Holger,Frey, Holger
scheme or table, p. 961 - 964 (2010/04/22)
We report on the development of an alternative protocol for the facile, solvent-free synthesis of various novel imidazolium-based ionic liquids (ILs) that affords highly pure products without the necessity of subsequent purification steps. The continuous
PHENYLALKYL AND PYRIDYLALKYL PIPERAZINE DERIVATIVES
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Page 66-67, (2010/02/07)
This invention relates to compounds of the formula (1) wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page 213, (2010/02/06)
The present invention provides a novel benzazepine derivative represented by formula : wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.
Photochemical synthesis of aldehydes in the solid phase
Blankespoor, Ronald L.,DeVries, Tim,Hansen, Eric,Kallemeyn, Jeffrey M.,Klooster, Aaron M.,Mulder, Jason A.,Smart, Robert P.,Vander Griend, Douglas A.
, p. 2677 - 2681 (2007/10/03)
A substituted anthraquinone (AQ), previously shown to photochemically generate benzaldehyde in methanol solution, was attached to a commercially available resin via an 11 carbon tether and an amide bond. Photolysis of the polymer-bound AQ with visible or 350 nm UV light resulted in the formation of benzaldehyde in yields of 50-55% as determined by HPLC. The phenolic positions in the polymer were then alkylated using benzyl bromide and 1-iodo-3-(4-nitrophenyl)propane in a coupling reaction with K2CO3 as a base and a solution-phase proton shuttle. Photolysis of these alkylated polymers resulted in the formation of benzaldehyde (54-89%) and 3-(4-nitrophenyl)-propanal (58-67%). The yields of both aldehydes dropped considerably with subsequent realkylation and photolysis, and the polymer beads began to show signs of deterioration. This is the first time that aldehydes have been made photochemically on a solid-supported phase.
