COMPOUNDS AND METHODS FOR THE TREATMENT OF MICROBIAL INFECTIONS
Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I): In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
1 . A compound having formula (I):
or a derivative thereof,
wherein R 1 , R 2 , and R 3 are independently or jointly selected from the group consisting of: H; I; OH; CN; (C 1-4 )alkyl; (C 2-4 )alkenyl, wherein a double bond is optionally located at any position in the alkenyl carbon chain; alkynyl; aralkyl; alkaryl; halogenated alkyl; aryl; heterocyclyl; cycloalkyl; cycloalkenyl; cycloalkynyl; hydroxyalkyl; aminoalkyl; acylamino; thiol; thioalkyl; alkoxy; alkoxyalkyl; aryloxy; arylalkoxy; acyloxy; carbamoyl; trifluoromethyl; phenoxy; benzyloxy; phosphonic acid; phosphate ester; sulfonic acid (—SO 3 H); sulfonate ester; sulfonamide; carbamate; alkyltriphenylphosphonium; ketone (═O); ether (—OR 4 ); ester (—COOR 5 and —OC(═O)R 5 ); and R 1 is not methyl at a C-2 position or a C-4 position in a cyclic group when R 2 and R 3 are both H,
wherein R 1 , R 2 , and R 3 are not jointly H; R 3 is not methyl when R 1 and R 2 are both H; R 1 and R 2 are not jointly —OMe,
wherein R 1 , R 2 are optionally bonded together to form a four-, five-, or six-membered heterocyclyl, cycloalkenyl, or cycloalkyl, and wherein R 1 and R 2 are not bonded together to form
wherein R 4 and R 5 are independently or jointly selected from the group consisting of: a (C 1-4 )alkyl; (C 2-4 )alkenyl, wherein a double bond is optionally located at any position in the alkenyl carbon chain; and alkynyl, and wherein R 4 is not methyl at a C-4 position in a cyclic group when R 2 and R 3 are both H, and
wherein the combinations of substituents are selected for the resulting compound to exhibit effectiveness in reducing virulence of bacteria.
2 . The compound of claim 1 , wherein R 3 is H or methyl.
3 . The compound of claim 1 , wherein the bacteria that the compound of claim 1 exhibits effectiveness in reducing virulence comprise Staphylococci sp.
4 . The compound of claim 1 , wherein the bacteria that the compound of claim 1 exhibits effectiveness in reducing virulence comprise Staphylococcus aureus.
5 . The compound of claim 1 , wherein the said reducing virulence of bacteria by the compounds and/or derivatives thereof comprises inhibiting biosynthesis of staphyloxanthin in said bacteria.
6 . A composition for preventing and/or treating bacterial infections and/or related diseases or conditions, comprising an effective amount of the compound according to claim 1 , or the derivative thereof, and a pharmaceutically acceptable carrier.
7 . The composition of claim 6 , wherein the said bacterial infections comprise staphylococcal infections.