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Chemical Structure| 72-80-0 Chemical Structure| 72-80-0

Structure of Chlorquinaldol
CAS No.: 72-80-0

Chemical Structure| 72-80-0

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Chlorquinaldol is a halogenated hydroxyquinoline mainly applied topically in infected skin conditions and in vaginal infections.

Synonyms: Chloquinan

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Product Citations

Product Citations

Abouelkhair, Ahmed A ; Seleem, Mohamed N ;

Abstract: Clostridioides difficile is an enteric pathogen that can cause a range of illnesses from mild diarrhea to pseudomembranous colitis and even death. This pathogen often takes advantage of microbial dysbiosis provoked by antibiotic use. With the increasing incidence and severity of infections, coupled with high recurrence rates, there is an urgent need to identify innovative therapies that can preserve the healthy state of the gut microbiota. In this study, we screened a microbial metabolite library against C. difficile. From a collection of 527 metabolites, we identified 18 compounds with no previously identified antimicrobial activity and metabolites that exhibited potent activity against C. difficile growth. Of these 18 hits, five drugs and three metabolites displayed the most potent anti-C. difficile activity and were subsequently assessed against 20 clinical isolates of C. difficile. These potent agents included ecteinascidin 770 (minimum inhibitory concentration against 50% of isolates [MIC50] ≤0.06 µg/mL); derivatives, such as broxyquinoline and choloroquinaldol (MIC50 = 0.125 µg/mL); ionomycin calcium salt, carbadox, and (MIC50 = 1 µg/mL); and and milbemycin oxime (MIC50 = 4 µg/mL). Unlike vancomy_x005f_x0002_cin and , which are the standard-of-care anti-C. difficile antibiotics, most of these metabolites showed robust bactericidal activity within 2-8 h with minimal impact on the growth of representative members of the normal gut microbiota. These results suggest that the drugs and microbial metabolite scaffolds may offer alternative avenues to address unmet needs in C. difficile disease prevention and treatment.

Keywords: screening ; microbiota ; MIC ; microbial metabolites ; Clostridioides difficile

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Product Details of Chlorquinaldol

CAS No. :72-80-0
Formula : C10H7Cl2NO
M.W : 228.07
SMILES Code : OC1=C2N=C(C)C=CC2=C(Cl)C=C1Cl
Synonyms :
Chloquinan
MDL No. :MFCD00023984
InChI Key :GPTXWRGISTZRIO-UHFFFAOYSA-N
Pubchem ID :6301

Safety of Chlorquinaldol

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NIH/3T3 cells 2.11 μM (IC50) 72 h To evaluate the inhibitory effect of Chlorquinaldol on NIH/3T3 cell proliferation. Results showed that Chlorquinaldol had a stronger inhibitory effect on activated NIH/3T3 cells. ACS Cent Sci. 2024 Aug 28;10(9):1789-1802.
MRC5 cells 7.15 μM (IC50) 72 h To evaluate the inhibitory effect of Chlorquinaldol on MRC5 cell proliferation. Results showed that Chlorquinaldol had a stronger inhibitory effect on activated MRC5 cells. ACS Cent Sci. 2024 Aug 28;10(9):1789-1802.
NIH/3T3 cells 10 μM 24 h To evaluate the inhibitory effect of Chlorquinaldol on TGFβ1-stimulated fibroblast proliferation. Results showed that Chlorquinaldol significantly reduced TGFβ1-stimulated fibroblast proliferation. ACS Cent Sci. 2024 Aug 28;10(9):1789-1802.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Bleomycin-induced pulmonary fibrosis model Intraperitoneal injection 2, 4, and 8 mg/kg Every 48 hours for 20 days To evaluate the preventive effect of Chlorquinaldol on bleomycin-induced pulmonary fibrosis. Results showed that Chlorquinaldol significantly improved the survival rate of mice, reduced collagen deposition and inflammatory responses in lung tissues. ACS Cent Sci. 2024 Aug 28;10(9):1789-1802.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01153958 Vaginosis, Bacterial Phase 4 Terminated - China ... More >> Peking University People's Hospital Beijing, China Second Hospital of West China Medical School, Sichuan University Chengdu, China Obstetrics & Gynaecology Hospital of Fudan University Shanghai, China Peking University Shenzhen Hospital Shenzhen, China Wuhan Union Hospital of China Wuhan, China Less <<
NCT01153958 - Terminated - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.38mL

0.88mL

0.44mL

21.92mL

4.38mL

2.19mL

43.85mL

8.77mL

4.38mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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