PNU 100480 Chemical Properties

Melting point:

186-187°C

Boiling point:

609.0±55.0 °C(Predicted)

Density 

1.321±0.06 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: soluble20mg/mL, clear

pka

15.53±0.46(Predicted)

form 

powder

color 

white to beige

optical activity

[α]/D -8 to -12°, c = 1 in chloroform-d

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

Safety Statements 

45

PNU 100480 Usage And Synthesis

Description

PNU 100480 is an oxazolidinone antibiotic that is active against multidrug resistant tuberculosis. It inhibits the growth of M. tuberculosis replicating and nonreplicating strains (MIC = ~400 ng/ml for both) and of clinical isolates that are susceptible or resistant to a combination of isoniazid , rifampin (rifampicin; ), ethambutol , and streptomycin (; MICs = ≤0.0625-0.5 mg/L). It also inhibits the growth of P. insidiosum and P. aphanidermatum clinical isolates (MICs = 4-64 μg/ml). PNU 100480 (100 mg/kg per day) decreases the number of colony forming units (CFU) in the lung in a mouse model of systemic nonreplicating M. tuberculosis infection.

Uses

Sutezolid is an oxazolidinone antibacterial agent analog. Sutezolid is a promising antimycobacterial agent (tuberculostatic).

Biochem/physiol Actions

Sutezolid (PNU 100480) is an oxazolidinone antimicrobial. Sutezolid inhibits protein synthesis by inhibiting bacterial mRNA translation. Sutezolid is being investigated for the treatment of multiple drug–resistant and extensively drug-resistant tuberculosis. The compound is a less toxic and more potent derivative of linezolid.

in vivo

IC 50

Oxazolidinone

References

[1] J W C ALFFENAAR. Susceptibility of clinical Mycobacterium tuberculosis isolates to a potentially less toxic derivate of linezolid, PNU-100480.[J]. Antimicrobial Agents and Chemotherapy, 2011, 55 3: 1287-1289. DOI: 10.1128/aac.01297-10
[2] MING ZHANG. In vitro and in vivo activities of three oxazolidinones against nonreplicating Mycobacterium tuberculosis.[J]. Antimicrobial Agents and Chemotherapy, 2014: 3217-3223. DOI: 10.1128/aac.02410-14
[3] ERICO S LORETO. In Vitro Activities of Miltefosine and Antibacterial Agents from the Macrolide, Oxazolidinone, and Pleuromutilin Classes against Pythium insidiosum and Pythium aphanidermatum.[J]. Antimicrobial Agents and Chemotherapy, 2018, 62 3. DOI: 10.1128/aac.01678-17

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