77409-99-5Relevant academic research and scientific papers
A novel water soluble axially substituted silicon(IV) phthalocyanine bearing quaternized 4-(4-pyridinyl)phenol groups: Synthesis, characterization, photophysicochemical properties and BSA/DNA binding behavior
Al-Raqa, Shaya Y.,Durmu?, Mahmut,Kaya, Esra Nur,Khezami, Khaoula
, (2021)
The novel axially bis[4-(4-pyridinyl)phenol] substituted silicon(IV) phthalocyanine (3) and its quaternized derivative (3Q) were designed and synthesized. These phthalocyanines were fully characterized by elemental analysis and different spectroscopic met
3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations
Tang, Jing,Liu, Feng,Nagy, Eva,Miller, Lena,Kirby, Karen A.,Wilson, Daniel J.,Wu, Bulan,Sarafianos, Stefan G.,Parniak, Michael A.,Wang, Zhengqiang
, p. 2648 - 2659 (2016/04/10)
Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) remains an unvalidated antiviral target. A major challenge of specifically targeting HIV RNase H arises from the general lack of selectivity over RT polymerase (pol) and integrase (IN) strand transfer (ST) inhibitions. We report herein the synthesis and biochemical evaluations of three novel 3-hydroxypyrimidine-2,4-dione (HPD) subtypes carefully designed to achieve selective RNase H inhibition. Biochemical studies showed the two subtypes with an N-1 methyl group (9 and 10) inhibited RNase H in low micromolar range without siginificantly inhibiting RT polymerase, whereas the N-1 unsubstituted subtype 11 inhibited RNase H in submicromolar range and RT polymerase in low micromolar range. Subtype 11 also exhibited substantially reduced inhibition in the HIV-1 INST assay and no significant cytotoxicity in the cell viability assay, suggesting that it may be amenable to further structure-activity relationship (SAR) for identifying RNase H inhibitors with antiviral activity.
APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
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Page/Page column 117, (2010/07/04)
Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
Spin-crossover and liquid crystal properties in 2D cyanide-bridged Fe II-MI/II metalorganic frameworks
Seredyuk,Gaspar,Ksenofontov,Galyametdinov,Verdaguer,Villain,Guetlich
scheme or table, p. 10022 - 10031 (2011/01/10)
Novel two-dimensional heterometallic Fe(II)-M(NiII, Pd II, PtII, AgI, and AuI) cyanide-bridged metalorganic frameworks exhibiting spin-crossover and liquid crystal properties, formulated as {FeL2
REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 122, (2009/07/10)
Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using t
Vesicular monoamine transporter substrate/inhibitor activity of MPTP/MPP+ derivatives: A structure-activity study
Wimalasena, D. Shyamali,Perera, Rohan P.,Heyen, Bruce J.,Balasooriya, Inoka S.,Wimalasena, Kandatege
, p. 760 - 768 (2008/09/19)
The active metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), N-methyl-4-phenylpyridinium (MPP+), selectively destroys the dopaminergic neurons and induces the symptoms of Parkinson's disease. Inhibition of mitochondrial complex
Syntheses of sterically hindered pyridinium phenoxides as model compounds in nonlinear optics
Diemer, Vincent,Chaumeil, Helene,Defoin, Albert,Fort, Alain,Boeglin, Alex,Carre, Christiane
, p. 2727 - 2738 (2007/10/03)
Noncentrosymmetric molecules with a π-conjugated system and, among them, push-pull molecules such as pyridinium phenoxide, are a promising new class of materials for applications in optoelectronics due to their nonlinear optical (NLO) properties. Modelling studies have indicated that an increase in the twist angle between the two aromatic rings leads to an enhancement of the NLO properties. In order to confirm this feature experimentally, it was necessary to prepare a series of new hindered pyridinium phenoxides. Their efficient syntheses by Suzuki cross-coupling reactions are described herein. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
Synthesis of 4-[N-methyl-4-pyridinio]-phenolate (POMP) and negative solvatochromism of this model molecule in view of nonlinear optical applications
Diemer, Vincent,Chaumeil, Hélène,Defoin, Albert,Jacques, Patrice,Carré, Christiane
, p. 4737 - 4740 (2007/10/03)
4-[N-Methyl-4-pyridinio]-phenolate or [4-(phenyloxido)-N-methylpyridinium, POMP] has been synthesized via Suzuki cross-coupling reaction. POMP undergoes a strong negative solvatochromism (blue shift) as the solvent polarity increases and behaves qualitati
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 16, (2010/02/05)
Compounds represented by formula I: wherein R2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K
Robichaud, Jo?l,Oballa, Renata,Prasit, Peppi,Falgueyret, Jean-Pierre,Percival, M. David,Wesolowski, Gregg,Rodan, Sevgi B.,Kimmel, Donald,Johnson, Colena,Bryant, Cliff,Venkatraman, Shankar,Setti, Eduardo,Mendonca, Rohan,Palmer, James T.
, p. 3709 - 3727 (2007/10/03)
A novel series of nonpeptidic biaryl compounds was identified as potent and reversible inhibitors of cathepsin K. The P2-P3 amide bond of a known amino acetonitrile dipeptide 1 was replaced with a phenyl ring, thereby giving rise to this biaryl series that retained potency vs cathepsin K and showed an improved selectivity profile against other cathepsins. Structural modification within this series resulted in the identification of compound (R)-2, a potent human cathepsin K inhibitor (IC50 = 3 nM) that is selective versus cathepsins B (IC50 = 3950 nM), L (IC50 = 3725 nM), and S (IC50 = 2010 nM). In an in vitro assay involving rabbit osteoclasts and bovine bone, compound (R)-2 inhibited bone resorption with an IC 50 of 95 nM. It was shown that, unlike some peptidic nitrile inhibitors of cysteine proteases, the nitrile moiety of (R)-2 is not converted to the corresponding amide 3 by cathepsin K. This indicates that this class of nonpeptidic nitrile inhibitors is unlikely to be hydrolyzed by cysteine proteases. Furthermore, the inhibition of cathepsin K by compound (R)-2 was shown to be fully reversible and not observably time-dependent. To demonstrate the efficacy of compound (R)-2 in vivo, it was administered to ovariectomized (OVX) rhesus monkeys at 20 mg/kg, po once daily for 8 days, and a urinary marker of bone turnover, N-telopeptide of type I collagen (uNTx), was measured. During the eight-day dosing period, the mean reduction by compound (R)-2 in uNTx was 80% (p 0.001). This demonstrates that inhibition of cathepsin K leads to an inhibition of this bone resorption marker in OVX rhesus monkeys and strongly suggests that inhibition of cathepsin K is a viable therapeutic approach for the treatment of osteoporosis.
