Tiamulin is a semi–synthetic analogue of pleuromutilin in which the hydroxyacetyl side chain is replaced with a larger diethylaminoethylthioacetyl moiety, providing greater hydrophobicity and an ionisable group for salt formation and greater water solubility. Tiamulin is a potent and highly selective antibiotic active against a range of Gram positive bacteria, with no cross resistance to existing antibiotic classes due to its unique mode of action. Like pleuromutilin, it inhibits protein synthesis by binding to domain V of 23S rRNA.
정의
ChEBI: A carbotricyclic compound that is pleuromutilin in which the hydroxyacetate group is replaced by a 2-{[2-(diethylamino)ethyl]sulfanyl}acetate group. An antibacterial drug, tiamulin is used in veterinary medicine (generally as its hydrogen fumarate salt) fo
the treatment of swine dysentery caused by Serpulina hyodysenteriae.
Safety Profile
Poison by
intramuscular and intravenous routes.
Moderately toxic by ingestion and
subcutaneous routes. When heated to
decomposition it emits toxic fumes of SOx
and NOx. See also MERCAPTANS.
Synthesis
Tiamulin was synthesized by Sandoz Co. in 1973, starting from pleuromutilin produced by Pleurotus mutilus.
