Pharmaceutical raw materials powder Pleuromulin

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Pleuromulin Powder Usage and Synthesis.

Pleurin truncatus is a broad-spectrum diterpene antibiotic produced by Pleurus. It can inhibit the protein synthesis of bacteria, thus achieving the effect of inhibiting bacterial growth. It works in a different way than other types of antibiotics. In the mechanism of action. Truncated pleurotins mainly act on the ribosome level of bacterial cells, and inhibit the synthesis of bacterial proteins by inhibiting the activity of peptidyl transferase, so as to achieve a broad spectrum antibacterial effect. The main skeleton of truncated pleurotins is composed of three rings, and the basic structure of the group is eight membered rings. The carbonyl group on the five-membered ring and the hydroxyl group on C-11 are the necessary groups for activity, and most foreign studies are to chemically modify C-14, so as to greatly improve its antibacterial activity and bioavailability.

Use of Pleuromulin.

The main skeleton of truncated pleurotins is composed of three rings, and the basic structure of the group is eight membered rings. The carbonyl group on the five-membered ring and the hydroxyl group on C-11 are the necessary groups for activity, and most foreign studies are to chemically modify C-14, so as to greatly improve its antibacterial activity and bioavailability. Because C-14 of the truncated pleurin drugs contains free hydroxyl groups, it is not active; By modifying C-14, the derivatives with enhanced antibacterial activity against bacteria and mycoplasma can be obtained.

In addition, the antibacterial activity of C-14 side chain connecting neutral or acidic groups was very low, and the activity of connecting two basic side chains was also low. The thioether-based side chain linked to an alkaline center, for example, contains thioether-based side chains in the drug Tymycin fumarate. However, if the sulfur atom in the thioether group is replaced by the oxygen atom, the activity of the truncated pleurin drugs can be sharply decreased. Other alkaline substituents, such as guanidine or primary amine, linked to C-14 side cannot reach the activity level of thioether-containing group derivatives, and are easily hydrolyzed and inactivated in vivo. Therefore, acylation of C-14 site of truncated pleurin compounds can significantly reduce the minimum antibacterial concentration and increase antibacterial activity.

Pleuromulin