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[ CAS No. 2243-83-6 ] {[proInfo.proName]}

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Chemical Structure| 2243-83-6
Chemical Structure| 2243-83-6
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Product Citations

Product Citations      Expand+

Faisal Aziz ; Kanamata Reddy ; Virneliz Fernandez Vega , et al. DOI:

Abstract: The suppressor of T cell receptor signaling (Sts) proteins are negative regulators of immune signaling. Genetic inactivation of these proteins leads to significant resistance to infection. From a 590,000 compound high-throughput screen, we identified the 2-(1H)-quinolinone derivative, , as a putative inhibitor of Sts activity. , and a small library of derivatives, are competitive, selective inhibitors of Sts-1 with IC50 values from low to submicromolar. SAR analysis indicates that the , the acid, and the moieties are all essential for activity. A crystal structure confirmed the SAR and reveals key interactions between this class of compound and the . Although has poor cell permeability, we demonstrated that a liposomal preparation can inactivate the activity of Sts-1 in cells. These studies demonstrate that Sts-1 enzyme activity can be pharmacologically inactivated and provide foundational tools and insights for the development of immune-enhancing therapies that target the Sts proteins.

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Kim, Ho Young ; Lee, Ji Youn ; Hsieh, Chia-Ju , et al. DOI: PubMed ID:

Abstract: Previous studies have confirmed that the binding of D3?receptor antagonists is competitively inhibited by endogenous dopamine despite excellent binding affinity for D3?receptors. This result urges the development of an alternative scaffold that is capable of competing with dopamine for binding to the D3?receptor. Herein, an SAR study was conducted on metoclopramide that incorporated a flexible scaffold for interaction with the secondary binding site of the D3?receptor. The alteration of benzamide substituents and secondary binding fragments with aryl carboxamides resulted in excellent D3?receptor affinities (Ki = 0.8–13.2 nM) with subtype selectivity to the D2?receptor ranging from 22- to 180-fold. The β-arrestin recruitment assay revealed that?21c?with 4-(pyridine-4-yl)benzamide can compete well against dopamine with the highest potency (IC50?= 1.3 nM). Computational studies demonstrated that the high potency of?21c?and its analogs was the result of interactions with the secondary binding site of the D3?receptor. These compounds also displayed minimal effects for other GPCRs except moderate affinity for 5-HT3?receptors and TSPO. The results of this study revealed that a new class of selective D3?receptor antagonists should be useful in behavioral pharmacology studies and as lead compounds for PET radiotracer development.

Keywords: D3 receptor antagonists ; metoclopramide ; bitopic ligand ; β-arrestin recruitment assay ; computational chemistry

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Product Details of [ 2243-83-6 ]

CAS No. :2243-83-6 MDL No. :MFCD00004093
Formula : C11H7ClO Boiling Point : -
Linear Structure Formula :- InChI Key :XNLBCXGRQWUJLU-UHFFFAOYSA-N
M.W : 190.63 Pubchem ID :75246
Synonyms :

Calculated chemistry of [ 2243-83-6 ]      Expand+

Physicochemical Properties

Num. heavy atoms : 13
Num. arom. heavy atoms : 10
Fraction Csp3 : 0.0
Num. rotatable bonds : 1
Num. H-bond acceptors : 1.0
Num. H-bond donors : 0.0
Molar Refractivity : 54.13
TPSA : 17.07 ?2

Pharmacokinetics

GI absorption : High
BBB permeant : Yes
P-gp substrate : No
CYP1A2 inhibitor : Yes
CYP2C19 inhibitor : Yes
CYP2C9 inhibitor : No
CYP2D6 inhibitor : No
CYP3A4 inhibitor : No
Log Kp (skin permeation) : -4.44 cm/s

Lipophilicity

Log Po/w (iLOGP) : 2.13
Log Po/w (XLOGP3) : 4.26
Log Po/w (WLOGP) : 3.22
Log Po/w (MLOGP) : 3.03
Log Po/w (SILICOS-IT) : 3.47
Consensus Log Po/w : 3.22

Druglikeness

Lipinski : 0.0
Ghose : None
Veber : 0.0
Egan : 0.0
Muegge : 2.0
Bioavailability Score : 0.55

Water Solubility

Log S (ESOL) : -4.21
Solubility : 0.0118 mg/ml ; 0.0000618 mol/l
Class : Moderately soluble
Log S (Ali) : -4.33
Solubility : 0.00891 mg/ml ; 0.0000467 mol/l
Class : Moderately soluble
Log S (SILICOS-IT) : -4.64
Solubility : 0.00437 mg/ml ; 0.0000229 mol/l
Class : Moderately soluble

Medicinal Chemistry

PAINS : 0.0 alert
Brenk : 1.0 alert
Leadlikeness : 2.0
Synthetic accessibility : 1.03

Safety of [ 2243-83-6 ]

Signal Word:Danger Class:8
Precautionary Statements:P280-P305+P351+P338-P310 UN#:3261
Hazard Statements:H314 Packing Group:Ⅱ
GHS Pictogram:

Application In Synthesis of [ 2243-83-6 ]

* 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.

  • Downstream synthetic route of [ 2243-83-6 ]

[ 2243-83-6 ] Synthesis Path-Downstream   1~3

  • 1
  • [ 2243-82-5 ]
  • [ 2243-83-6 ]
  • [ 149484-66-2 ]
  • 2
  • [ 2243-83-6 ]
  • ammonium carbonate [ No CAS ]
  • [ 2243-82-5 ]
  • 3
  • [ 2243-83-6 ]
  • [ 2243-82-5 ]
YieldReaction ConditionsOperation in experiment
100% With ammonia; In methanol; 2-Naphthoyl chloride (2.21 g, 11.6 mmol) was dissolved in a MeOH/NH3 solution (2 M, 20 mL) and was allowed to stir overnight. Volatiles were removed and the resulting white solid was triturated with EtOAc. The solid was filtered and washed with cold EtOAc to yield a white solid which was used without further purification (1.98 g, 100percent yield). m.p. 191-192° C. 1H NMR (CDCl3) delta 8.39 (s, 1H, ArH) , 7.90 (4H, ArH), 7.57 (m, 2H, ArH). 13C NMR (CDCl3) delta 169.3, 135.0, 132.6, 130.5, 129.0, 128.6, 128.1, 127.9, 127.8, 126.9, 123.7. IR (nujol) vmax cm-1: 3400, 3210, 1650, 1628, 1512, 1510.
52% With ammonia; In tetrahydrofuran; water; at 20℃; for 4h;Cooling with ice; A solution of 2-naphthoyl chloride (5.70 g, 29.9 mmol) in tetrahydrofuran (60 ml) was added dropwise to a mixture of 28 percentaqueous ammonia (20 ml) and tetrahydrofuran (30 ml) with stirring under ice cooling, and the mixture was stirred at room temperature for 4 hrs. The solvent was distilled off under reduced pressure, and water was added to the residue. The precipitates were collected by filtration and dried to give 2-carbamoylnaphthalene (2.68 g, 52 percent) as a colorless solid. IR (Nujol): 3378, 3194, 1685, 1655 cm-1; APCI-MS m/z: 172 [M+H]+.
52% With ammonium hydroxide; In tetrahydrofuran; at 20℃; for 4h;Cooling with ice; (Preparation 1) [0083] 1) A solution of 2-naphthoyl chloride (5.70 g, 29.9 mmol) in tetrahydrofuran (60 ml) was added dropwise to a mixture of 28percent aqueous ammonia (20 ml) and tetrahydrofuran (30 ml) with stirring under ice cooling, and the mixture was stirred at room temperature for 4 hrs. The solvent was distilled off under reduced pressure, and water was added to the residue. The precipitates were collected by filtration and dried to give 2-carbamoylnaphthalene (2.68 g, 52percent) as a colorless solid. IR (Nujol) : 3378, 3194, 1685, 1655 cm-1; APCI-MS m/z: 172 [M+H]+.
With ammonia; In dichloromethane; water; at 0℃; for 1h; To a solution of 2-naphthoic acid (25 g, 0.145 mol) in MC (200ml), oxalyl chloride (38 ml, 0.4356 mol) and a catalytic amount of DMF wereadded and stirred at room temperature for 2hrs. After the solvent wasevaporated, the crude acyl chloride was diluted with MC (200 ml), to which asolution of ammonium hydroxide in water (160 ml) was dropwise added at anice bath temperature. After stirring for 1 hr, the precipitated product wascollected by suction filtration, triturated in hexane and dried to obtain the titlecompound, which was used next step without further purification.
With ammonia; In tetrahydrofuran; at 0 - 20℃; for 5.5h; A solution of Naphthalene-2-carbonyl chloride obtained from Step A was dissolved in THF (30 mL) and this was cooled down to O0C. Ammonia gas was passed for approximately 1.5 hrs through the solution and the reaction was stirred at room temperature under a closed system for 4 hrs. A white solid precipitate was observed in the reaction mixture. The reaction mixture was dissolved in ethyl acetate and washed using water followed by brine solution. The organic layer was separated and dried over sodium sulphate and the volatiles were evaporated off in vacuo to afford the crude product.The crude product was purified by column chromatography using neutral silica gel of 60- 120 mesh size. A gradient of 50-60 percent ethyl acetate in hexane was used for elution of the title compound (0.8 g).
With ammonium hydroxide; In dichloromethane; at 20℃; Procedure for the synthesis of amides 2Amides 2 were prepared by reaction of naphtoic acids 1 (lmmol) commercially available with 2 mL of S0C12 and 0.5 mL of Et3 . The mixture was refluxed for 30 minutes and acyl chloride was dissolved in CH2C12 and was added to a solution of NH40H. The mixture was shaken at room temperature for 4-24 h. The alkaline layer was extracted with CH2C12 and organic layers were combined and dried over Na2SC>4 and concentrated. In some cases, the amide precipitated before separation of the two layers and was isolated by filtration. The amides were purified by column chromatography in the elution conditions reported in the experimental data for each example reported.
With ammonium hydroxide; In dichloromethane; water; at 20℃; for 4h; General procedure: Amides 7a?e were prepared from the corresponding commercially available carboxylic acids (1?mmol) 6a?e treated with an excess of SOCl2 (7?mmol) in presence of Et3N (0.1?mmol) under reflux for 1?h. The corresponding acylchloride was added to a mixture (45?mL) of ? NH4OH (28percent), ? H2O and CH2Cl2 (1:1:1). The mixture was stirred at room temperature for 4?h. Insoluble amides 7a?d were separated by filtration while the amide ? 7e was obtained removing the solvent under vacuo. The crude was washed with H2O (20?mL) and extracted with AcOEt (3?×?20?mL).
With ammonium hydroxide; In tetrahydrofuran; at 20℃; for 2h; General procedure: To a solution of an appropriate substituted carboxylic acid (10 mmol) in CHCl3 (50 mL) was added thionyl chloride (3.6 mL, 50 mmol), dropwise over 10 min. The resulting solution was refluxed for 8 h and then concentrated in vacuo. The residual light brown oil was dissolved in THF (50 mL), diluted with a solution of 30percent NH4OH (6 mL), and stirred at room temperature for an additional 2 h. At that point, saturated aqueous NaHCO3 (10 mL) was added and the reaction mixture was extracted with EtOAc (3 × 30 mL). The combined organic layer was washed with brine (50 mL), dried over anhydrous Na2SO4, and concentrated in vacuo. The crude amide was carried directly to the next step without further purification.
With ammonium hydroxide; In dichloromethane; at 20℃; General procedure: Amides 2 were prepared by reaction of naphtoic acids 1 (1 mmol) commercially available with 2 mL of SOCl2 and 0.5 mL of Et3N. The mixture was refluxed for 30 minutes and acyl chloride was dissolved in CH2Cl2 and was added to a solution of NH4OH. The mixture was shaken at room temperature for 4-24 h. The alkaline layer was extracted with CH2Cl2 and organic layers were combined and dried over Na2SO4 and concentrated. In some cases, the amide precipitated before separation of the two layers and was isolated by filtration. The amides were purified by column chromatography in the elution conditions reported in the experimental data for each example reported.

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