Anti-mycobacterial drugs
AssigneeThe Florida International University Board of Trustees
InventorsJoong Ho Moon, Michelle Miranda
Life of this patent
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Abstract
The subject invention provides oligo(carbamoylated guanidine)s (OCGs) having fast and selective mycobactericidal effects via disruption of the mycobacterial membrane potential. OCGs also potentiates bedaquiline, an oxidative phosphorylation-targeting anti-TB drug. The combination of OCG and anti-TB drug can be used as an effective therapy for treating tuberculosis.
Claims20
A method of treating a bacterial infection in a subject, the method comprising administering an effective amount of a pharmaceutical composition comprising an oligo(carbamoylated guanidine) (OCG) comprising a general structure of:
- wherein
- n is an integer from 3 to 50;
- X is an alkylene;
- a heteroatom interrupted alkylene;
- an arylene;
- a heteroarylene;
- or a combination thereof;
- Y is an alkylene;
- a heteroatom interrupted alkylene;
- an arylene;
- a heteroarylene;
- or a combination thereof;
- wherein the heteroatom interrupted alkylene and the heteroarylene have one or more heteroatoms selected from the group consisting of O, S, and N;
- and
- R1 and R2 are each independently H;
- substituted or unsubstituted linear, branched, or cyclic alkyl;
- one or more heteroatom interrupted substituted or unsubstituted linear branched or cyclic alkyl;
- unsubstituted or substituted aryl;
- unsubstituted or substituted heteroarylene;
- or a combination thereof;
- or R1 and R2 are combined as an alkylene or heteroatom interrupted alkylene, wherein R1NYNR2 comprises a heterocycle;
- or a salt thereof.
A method of inhibiting the growth of a Mycobacterium, the method comprising contacting the Mycobacterium with an OCG, the OCG comprising a general structure of:
- wherein
- n is an integer from 3 to 50;
- X is an alkylene, a heteroatom interrupted alkylene;
- an arylene;
- a heteroarylene;
- or a combination thereof;
- Y is an alkylene;
- a heteroatom interrupted alkylene;
- an arylene;
- a heteroarylene;
- or a combination thereof;
- wherein the heteroatom interrupted alkylene and the heteroarylene have one or more heteroatoms selected from the group consisting of O, S, and N;
- and
- R1 and R2 are each independently H;
- substituted or unsubstituted linear, branched, or cyclic alkyl;
- one or more heteroatom interrupted substituted or unsubstituted linear branched or cyclic alkyl;
- unsubstituted or substituted aryl;
- unsubstituted or substituted heteroarylene;
- or a combination thereof;
- or R1 and R2 are combined as an alkylene or heteroatom interrupted alkylene, wherein R1NYNR2 comprises a heterocycle;
- or a salt thereof.
A method of disrupting a mycobacterial membrane potential, the method comprising contacting a Mycobacterium with an OCG, the OCG comprising a general structure of:
- wherein
- n is an integer ranging from 3 to 50;
- X is an alkylene;
- a heteroatom interrupted alkylene;
- an arylene;
- a heteroarylene;
- or a combination thereof;
- Y is an alkylene;
- a heteroatom interrupted alkylene;
- an arylene;
- a heteroarylene;
- or a combination thereof;
- wherein the heteroatom interrupted alkylene and the heteroarylene have one or more heteroatoms selected from the group consisting of O, S, and N;
- and
- R1 and R2 are each independently H;
- substituted or unsubstituted linear, branched, or cyclic alkyl;
- one or more heteroatom interrupted substituted or unsubstituted linear branched or cyclic alkyl;
- unsubstituted or substituted aryl;
- unsubstituted or substituted heteroarylene;
- or a combination thereof;
- or a salt thereof.
Dependencies are inferred from the claim text.