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[ CAS No. 527-72-0 ] {[proInfo.proName]}

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Chemical Structure| 527-72-0
Chemical Structure| 527-72-0
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Product Citations

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Ramirez, Eduardo ; Min, Sehong ; Ganegamage, Susantha K. , et al. DOI: PubMed ID:

Abstract: Alzheimer's disease (AD) is a multifactorial, chronic neurodegenerative disease characterized by the presence of extracellular beta-amyloid (Abeta) plaques, intraneuronal neurofibrillary tangles (NFTs), activated microglial cells, and an inflammatory state (involving reactive oxygen species production) in the brain. NFTs are comprised of misfolded and hyperphosphorylated forms of the microtubule-binding protein tau. Interestingly, the trimeric form of the 2N4R splice isoform of tau has been found to be more toxic than the trimeric 1N4R isoform in neuron precursor cells. Few drug discovery programs have focused on specific tau isoforms. The present drug discovery project is centered on the anti-aggregation effect of a series of seventeen 4- or 5-aminoindole carboxamides on the 2N4R isoform of tau. The selection of the best compounds was performed using alpha-synuclein (alpha-syn). The anti-oligomer and -fibril activities of newly synthesized aminoindole carboxamide derivatives were evaluated with biophys. methods, such as thioflavin T fluorescence assays, photo-induced crosslinking of unmodified proteins, and transmission electron microscopy. To evaluate the reduction of inclusions and cytoprotective effects, M17D neuroblastoma cells expressing inclusion-forming alpha-syn were treated with the best amide representatives. The 4-aminoindole carboxamide derivatives exhibited a better anti-fibrillar activity compared to their 5-aminoindole counterparts. The amide derivatives 2, 8, and 17 exerted anti-oligomer and anti-fibril activities on alpha-syn and the 2N4R isoform of tau. At a concentration of 40 μM, compound 8 reduced inclusion formation in M17D neuroblastoma cells expressing inclusion-prone alphaSynuclein3K::YFP. Our results demonstrate the potential of 4-aminoindole carboxamide derivatives with regard to inhibiting the oligomer formation of alpha-syn and tau (2N4R isoform) for further optimization prior to pre-clin. studies.

Keywords: Alzheimer's disease ; Amide ; Alpha-synuclein ; Fibril ; Oligomer

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Rao, Youliang ; Wang, Ting-Yu ; Qin, Chao , et al. DOI: PubMed ID:

Abstract: The newly emerged SARS-CoV-2 caused a global pandemic with astonishing mortality and morbidity. The mechanisms underpinning its highly infectious nature remain poorly understood. We report here that SARS-CoV-2 exploits cellular CTP synthetase 1 (CTPS1) to promote CTP synthesis and suppress interferon (IFN) induction. Screening a SARS-CoV-2 expression library identified ORF7b and ORF8 that suppressed IFN induction via inducing the deamidation of interferon regulatory factor 3 (IRF3). Deamidated IRF3 fails to bind the promoters of classic IRF3-responsible genes, thus muting IFN induction. Conversely, a shRNA-mediated screen focused on cellular glutamine amidotransferases corroborated that CTPS1 deamidates IRF3 to inhibit IFN induction. Functionally, ORF7b and ORF8 activate CTPS1 to promote de novo CTP synthesis while shutting down IFN induction. De novo synthesis of small-molecule inhibitors of CTPS1 enabled CTP depletion and IFN induction in SARS-CoV-2 infection, thus impeding SARS-CoV-2 replication. Our work uncovers a strategy that a viral pathogen couples immune evasion to metabolic activation to fuel viral replication. Inhibition of the cellular CTPS1 offers an attractive means for developing antiviral therapy that would be resistant to SARS-CoV-2 mutation.

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Product Details of [ 527-72-0 ]

CAS No. :527-72-0 MDL No. :MFCD00005437
Formula : C5H4O2S Boiling Point : -
Linear Structure Formula :- InChI Key :QERYCTSHXKAMIS-UHFFFAOYSA-N
M.W : 128.15 Pubchem ID :10700
Synonyms :

Calculated chemistry of [ 527-72-0 ]      Expand+

Physicochemical Properties

Num. heavy atoms : 8
Num. arom. heavy atoms : 5
Fraction Csp3 : 0.0
Num. rotatable bonds : 1
Num. H-bond acceptors : 2.0
Num. H-bond donors : 1.0
Molar Refractivity : 31.28
TPSA : 65.54 ?2

Pharmacokinetics

GI absorption : High
BBB permeant : Yes
P-gp substrate : No
CYP1A2 inhibitor : No
CYP2C19 inhibitor : No
CYP2C9 inhibitor : No
CYP2D6 inhibitor : No
CYP3A4 inhibitor : No
Log Kp (skin permeation) : -5.97 cm/s

Lipophilicity

Log Po/w (iLOGP) : 1.08
Log Po/w (XLOGP3) : 1.57
Log Po/w (WLOGP) : 1.45
Log Po/w (MLOGP) : 0.52
Log Po/w (SILICOS-IT) : 1.94
Consensus Log Po/w : 1.31

Druglikeness

Lipinski : 0.0
Ghose : None
Veber : 0.0
Egan : 0.0
Muegge : 1.0
Bioavailability Score : 0.56

Water Solubility

Log S (ESOL) : -2.02
Solubility : 1.22 mg/ml ; 0.00955 mol/l
Class : Soluble
Log S (Ali) : -2.56
Solubility : 0.356 mg/ml ; 0.00278 mol/l
Class : Soluble
Log S (SILICOS-IT) : -1.0
Solubility : 12.8 mg/ml ; 0.0998 mol/l
Class : Soluble

Medicinal Chemistry

PAINS : 0.0 alert
Brenk : 0.0 alert
Leadlikeness : 1.0
Synthetic accessibility : 1.72

Safety of [ 527-72-0 ]

Signal Word:Warning Class:N/A
Precautionary Statements:P261-P305+P351+P338 UN#:N/A
Hazard Statements:H315-H319-H335 Packing Group:N/A
GHS Pictogram:

Application In Synthesis of [ 527-72-0 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Upstream synthesis route of [ 527-72-0 ]
  • Downstream synthetic route of [ 527-72-0 ]

[ 527-72-0 ] Synthesis Path-Upstream   1~2

  • 1
  • [ 527-72-0 ]
  • [ 75-65-0 ]
  • [ 56267-50-6 ]
YieldReaction ConditionsOperation in experiment
69% for 5 h; Heating / reflux A solution of thiophene2-carboxylic acid (1.00 g, 7.8 mmol), diphenylphosphoryl azide (2.15 g, 7.80 mmol) and triethylamine (1.1 mL, 7.8 mmol) in tert-butanol (20 mL) was heated at reflux for 5 hours, at which time thin layer chromatography (DCM/Hexanes) indicates the reaction is complete. The reaction mixture was cooled to room temperature, poured into water and extracted with diethyl ether (3.x.). The combined ether extracts were washed with brine, dried over anhydrous sodium sulfate, and then concentrated to afford a beige solid. Purification by column chromatography (SiO2, DCM/Hexanes) afforded compound 113 as a white solid 1.07 g (69percent). 1H-NMR (400 MHz, DMSO-d6)δ 6.87(dd, 1H), 6.77 (m, 1H), 6.5 (dd, 1H), 1.46 (s, 9H).
69% for 5 h; Heating / reflux Example 113; A solution of thiophene2-carboxylic acid (1.00 g, 7.8 mmol), diphenylphosphoryl azide (2.15 g, 7.80 mmol) and triethylamine (1.1 mL, 7.8 mmol) in tert-butanol (20 mL) was heated at reflux for 5 hours, at which time thin layer chromatography (DCM/Hexanes) indicates the reaction is complete. The reaction mixture was cooled to room temperature, poured into water and extracted with diethyl ether (3.x.). The combined ether extracts were washed with brine, dried over anhydrous sodium sulfate, and then concentrated to afford a beige solid. Purification by column chromatography (SiO2, DCM/Hexanes) afforded compound 113 as a white solid 1.07 g (69percent). 1H-NMR (400 MHz, DMSO-d6)δ 6.87 (dd, 1H), 6.77 (m, 1H), 6.5 (dd, 1H), 1.46 (s, 9H).
50% at 90℃; for 4 h; To a solution of thiophenecarboxylic acid (0.5 g, 3.90 mmol) in tBuOH (10 ml) was added Et3N (0.571 ml, 4.10 mmol) and DPPA (0.883 ml, 4.10 mmol). The solution was heated at 90 °C for 4 hours. The reaction mixture was cooled to RT and the solvent was removed in vacuo. The residue was treated with benzene and then the solution was washed with 5percent citric acid, and sat'd NaHCO3. Solid was filtered off and the filtrate was washed with brine. The organic layer was dried (MgSO4), concentrated in vacuo and the residue was purified by silica gel column chromatography (EtOAc/hexanes) to obtain tert-butyl thiophen-2-ylcarbamate (0.39 g, 50percent yield). 1H NMR (400 MHz, DMSO-d6): δ 10.4 (brs, 1H), 6.84 (dd, J = 1.6, and 5.2 Hz, 1H), 6.75 (dd, J = 4.0, and 5.6 Hz, 1H), 6.48 (dd, J= 1.6, and 4.0 Hz, 2H), 1.45 (s, 9H); MS (ESI) m/z: 222.0 (M+22+H+).
Reference： [1] Journal of Medicinal Chemistry, 1991, vol. 34, # 5, p. 1594 - 1605
[2] Patent: US2007/105864, 2007, A1, . Location in patent: Page/Page column 151
[3] Patent: US2007/117804, 2007, A1, . Location in patent: Page/Page column 77
[4] Journal of Medicinal Chemistry, 2002, vol. 45, # 20, p. 4513 - 4523
[5] Journal of Medicinal Chemistry, 2007, vol. 50, # 20, p. 4898 - 4908
[6] Patent: WO2010/51373, 2010, A1, . Location in patent: Page/Page column 100
[7] Bioorganic and Medicinal Chemistry Letters, 2006, vol. 16, # 21, p. 5567 - 5571
  • 2
  • [ 527-72-0 ]
  • [ 112887-68-0 ]
Reference： [1] Patent: CN107616976, 2018, A,
[2] Patent: CN107616976, 2018, A,
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