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[ CAS No. 206361-99-1 ] {[proInfo.proName]}

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Chemical Structure| 206361-99-1
Chemical Structure| 206361-99-1
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Nour M. Alkashef ; Mohamed N. Seleem ; DOI: PubMed ID:

Abstract: Cryptococcosis is a fungal infection that is becoming increasingly prevalent worldwide, particularly among individuals with compromised immune systems, such as HIV patients. Amphotericin B (AmB) is the first-line treatment mainly combined with flucytosine. The scarcity and the prohibitive cost of this regimen urge the use of fluconazole as an alternative, leading to increased rates of treatment failure and relapses. Therefore, there is a critical need for efficient and cost-effective therapy to enhance the efficacy of AmB. In this study, we evaluated the efficacy of the HIV protease inhibitors (PIs) to synergize the activity of AmB in the treatment of cryptococcosis. Five PIs (ritonavir, atazanavir, saquinavir, lopinavir, and nelfinavir) were found to synergistically potentiate the killing activity of AmB against Cryptococcus strains with ?FICI ranging between 0.09 and 0.5 against 20 clinical isolates. This synergistic activity was further confirmed in a time-kill assay, where different AmB/PIs combinations exhibited fungicidal activity within 24 hrs. Additionally, PIs in combination with AmB exhibited an extended post-antifungal effect on treated cryptococcal cells for approximately 10 hrs compared to 4 hours with AmB alone. This promising activity against cryptococcal cells did not exhibit increased cytotoxicity towards treated kidney cells, ruling out the risk of drug combination-induced nephrotoxicity. Finally, we evaluated the efficacy of AmB/PIs combinations in the Caenorhabditis elegans model of cryptococcosis, where these combinations significantly reduced the fungal burden of the treated nematodes by approximately 2.44 Log10 CFU (92.4%) compared to the untreated worms and 1.40 Log10 ((39.4%) compared to AmB alone. The cost-effectiveness and accessibility of PIs in resource-limited geographical areas compared to other antifungal agents, such as flucytosine, make them an appealing choice for combination therapy.

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Johnston, Nikki ; Samuels, Tina L. ; Goetz, Christopher J. , et al. DOI: PubMed ID:

Abstract: Objective: More than 20% of the US population suffers from laryngopharyngeal reflux. Although dietary/lifestyle modifications and alginates provide benefit to some, there is no gold standard medical therapy. Increasing evidence suggests that pepsin is partly, if not wholly, responsible for damage and inflammation caused by laryngopharyngeal reflux. A treatment specifically targeting pepsin would be amenable to local, inhaled delivery, and could prove effective for endoscopic signs and symptoms associated with nonacid reflux. The aim herein was to identify small molecule inhibitors of pepsin and test their efficacy to prevent pepsin-mediated laryngeal damage in vivo. Methods: Drug and pepsin binding and inhibition were screened by high-throughput assays and crystallography. A mouse model of laryngopharyngeal reflux (mechanical laryngeal injury once weekly for 2 weeks and pH 7 solvent/pepsin instillation 3 days/week for 4 weeks) was provided inhibitor by gavage or aerosol (fosamprenavir or darunavir; 5 days/week for 4 weeks; n = 3). Larynges were collected for histopathologic analysis. Results: HIV protease inhibitors amprenavir, ritonavir, saquinavir, and darunavir bound and inhibited pepsin with IC50 in the low micromolar range. Gavage and aerosol fosamprenavir prevented pepsin-mediated laryngeal damage (i.e., reactive epithelia, increased intraepithelial inflammatory cells, and cell apoptosis). Darunavir gavage elicited mild reactivity and no discernable protection; aerosol protected against apoptosis. Conclusions: Fosamprenavir and darunavir, FDA-approved therapies for HIV/AIDS, bind and inhibit pepsin, abrogating pepsin-mediated laryngeal damage in a laryngopharyngeal reflux mouse model. These drugs target a foreign virus, making them ideal to repurpose. Reformulation for local inhaled delivery could further improve outcomes and limit side effects.

Keywords: Laryngopharyngeal reflux ; LPR ; pepsin ; fosamprenavir ; darunavir

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Chufan Andrew Jin ; DOI:

Abstract: Reactive species that are employed as electrophiles in functionalization of substrates are typically prepared from native functionality such as alcohols and carboxylic acids. The addition of a pre-functionalization step of native substrates can reduce the efficiency of syntheses. These pre-functionalization reactions along with the functionalization reactions themselves proceed through polar mechanisms, limiting the scope of both functionalization and pre-functionalization reactions. Reported herein are preliminary efforts in the development of a deoxy-functionalization protocol for secondary and tertiary alcohols. The reported protocol proceeds through a derived Barton-McCombie deoxygenation mediated by a super silyl radical. Transfer of a thiocarbonate activating group to the silyl radical generates carbon radical which can be trapped out with an external sulfonyl trap, generating sulfonyl radical, which may then react with an allylic silane allowing for turnover of the radical chain.

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Product Details of [ 206361-99-1 ]

CAS No. :206361-99-1 MDL No. :MFCD09260006
Formula : C27H37N3O7S Boiling Point : -
Linear Structure Formula :- InChI Key :CJBJHOAVZSMMDJ-HEXNFIEUSA-N
M.W : 547.66 Pubchem ID :213039
Synonyms :
UIC-94017;TMC114
Chemical Name :(3R,3aS,6aR)-Hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate

Calculated chemistry of [ 206361-99-1 ]      Expand+

Physicochemical Properties

Num. heavy atoms : 38
Num. arom. heavy atoms : 12
Fraction Csp3 : 0.52
Num. rotatable bonds : 13
Num. H-bond acceptors : 8.0
Num. H-bond donors : 3.0
Molar Refractivity : 142.2
TPSA : 148.8 ?2

Pharmacokinetics

GI absorption : Low
BBB permeant : No
P-gp substrate : Yes
CYP1A2 inhibitor : No
CYP2C19 inhibitor : No
CYP2C9 inhibitor : No
CYP2D6 inhibitor : No
CYP3A4 inhibitor : Yes
Log Kp (skin permeation) : -7.55 cm/s

Lipophilicity

Log Po/w (iLOGP) : 3.3
Log Po/w (XLOGP3) : 2.94
Log Po/w (WLOGP) : 3.46
Log Po/w (MLOGP) : 1.18
Log Po/w (SILICOS-IT) : 1.46
Consensus Log Po/w : 2.47

Druglikeness

Lipinski : 1.0
Ghose : None
Veber : 2.0
Egan : 1.0
Muegge : 0.0
Bioavailability Score : 0.55

Water Solubility

Log S (ESOL) : -4.46
Solubility : 0.0188 mg/ml ; 0.0000344 mol/l
Class : Moderately soluble
Log S (Ali) : -5.73
Solubility : 0.00103 mg/ml ; 0.00000188 mol/l
Class : Moderately soluble
Log S (SILICOS-IT) : -5.33
Solubility : 0.00255 mg/ml ; 0.00000466 mol/l
Class : Moderately soluble

Medicinal Chemistry

PAINS : 0.0 alert
Brenk : 1.0 alert
Leadlikeness : 2.0
Synthetic accessibility : 5.67

Safety of [ 206361-99-1 ]

Signal Word:Warning Class:N/A
Precautionary Statements:P261-P305+P351+P338 UN#:N/A
Hazard Statements:H302-H315-H319-H335 Packing Group:N/A
GHS Pictogram:
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