High Quality Pharmaceutical Pleuromutilin Pleuromulin CAS: 125-65-5

Superiority:

English name: Pleuromulin

CAS Number: 125-65-5

Molecular formula: C22H34O5

Molecular weight: 378.5

EINECS Number: 204-747-5

Melting point: 170-1710C

Specific rotation: D24+20°(c=3inabsethanol)

Boiling point: 482.8±45.0°C (Predicted)

Density: 1.15±0.1g/cm3(Predicted)

Storage conditions: -20°C Freezer

Solubility: DMSO:>10mg/mL(warmed)

Acidity coefficient: (pKa) 12.91±0.10 (Predicted)

Form: powder

Color: white to beige

Pleuromutilin is a broad-spectrum diterpene antibiotic produced by Pleurotus mutilus, and it is the precursor of semi-synthetic derivatives of pleuromutilin drugs. Pleuromutilin antibiotics are a large family of novel antibiotics with good antibacterial activity and resistance to drug resistance, which can effectively inhibit most gram-positive bacteria, mycoplasma and some gram-negative bacteria. Pleuromutilin antibiotics are mainly composed of tricyclic diterpenoids, and the most basic structure is an eight-membered ring. The carbonyl group on the five-membered ring and the hydroxyl group on C-11 in the molecular structure are the necessary functional groups for the basic activity of this class of antibiotics.

Pleuromutilin is a broad-spectrum diterpene antibiotic produced by Pleurotus. It can inhibit the protein synthesis of bacteria, so as to achieve the effect of inhibiting the growth of bacteria. It works differently than other types of antibiotics. in terms of mechanism of action. Pleuromutilin antibiotics mainly act on the ribosome level of bacterial cells. It inhibits the synthesis of bacterial proteins by inhibiting the activity of peptide acyltransferase, thereby achieving a broad-spectrum antibacterial effect. Pleuromutilin drugs are composed of three rings to form the main skeleton, and the basic structure of the group is an eight-membered ring; the carbonyl group on the five-membered ring and the hydroxyl group on C-11 are groups necessary for activity. -14 is chemically modified to greatly improve its bacteriostatic activity and bioavailability. Since C-14 of pleuromutilin drugs contains a free hydroxyl group, they have no activity; by modifying the C-14 position, derivatives with enhanced antibacterial activity against bacteria and mycoplasma can be obtained. In addition, the antibacterial activity of the compound with a neutral group or an acidic group connected to the side chain at the C-14 position is extremely low, and the activity of connecting two basic side chains is also low; The activity of derivatives is decisively improved, for example, the drug Tiamulin fumarate contains thioether side chains. However, if the sulfur atom in the thioether group is replaced by an oxygen atom, the activity of the pleuromutilin drugs can be drastically decreased. Adding other basic substituents, such as guanidino groups or primary amines, to the C-14 side chain can not achieve the activity level of derivatives containing thioether groups, and is easily hydrolyzed and inactivated in vivo. Therefore, acylation of the C-14 position of pleuromutilin compounds can significantly reduce the minimum inhibitory concentration and improve the antibacterial activity.

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