STEROID ALKALOIDS AND USES THEREOF AS ANTIMICROBIAL AGENTS AGAINST ELECTRON TRANSPORT-DEFICIENT MICROBES AND AS POTENTIATORS FOR ANTIMICROBIAL AGENTS AGAINST PATHOGENIC BACTERIA

The present invention includes novel compounds based on the tomatidine skeleton as well as composition comprising these compounds alone and in combination with known compounds, which exhibit antimicrobial activity against extracellular or intracellular electron transport-deficient microbes and/or increase the antimicrobial activity of aminoglycoside antibiotics against their targets, and which are useful as antibacterial agents for treatment or prophylaxis of monomicrobiotic or polymicrobic bacterial infections or for the reduction of antibiotic resistance development in animals or in humans, or for use as antiseptics or agents for sterilization or disinfection. 1103.-. (canceled)105. A method of disinfecting and/or sterilizing an object of (a) an electron transport-deficient bacterium; or (b) a polymicrobial infection as defined in ; or (c) a bacterial pathogen , said method comprising applying an effective amount of the compound as defined in or of a composition comprising said compound , and , for (c) , an aminoglycoside antibiotic , to said object , whereby said object is disinfected and/or sterilized.106. The method of claim 105 , wherein said object is an animal claim 105 , an animal tissue claim 105 , animal cells claim 105 , food claim 105 , a synthetic material or a natural material.107. (canceled)108. The method of claim 104 , wherein the electron transport-deficient bacterium is an intracellular bacterium.109. The method of claim 104 , wherein the electron transport-deficient bacterium is a bacterial small-colony variant (SCV).110. (canceled)111. The method of claim 109 , wherein the SCV or the bacterial pathogen is of the Firmicutes phylum.112114.-. (canceled)115staphylococcus.. The method of claim 104 , wherein the electron transport-deficient bacterium is a116staphylococcusStaphylococcus.. The method of claim 115 , wherein the is an antibiotic-resistant117staphylococcusStaphylococcus aureusStaphylococcus epidermidisStaphylococcus ...

Steroid alkaloids and compositions and kits thereof

The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): There are provided compositions and kits using such compounds and inhibitors.

ATP SYNTHASE INHIBITORS AND STEROID ALKALOIDS AND USES THEREOF AS ANTIMICROBIAL AGENTS AND AS POTENTIATORS FOR AMINOGLYCOSIDES AGAINST PATHOGENIC BACTERIA

The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): (Formula (I)) (A) in combination with an aminoglycoside antibiotic for preventing or treating a bacterial infection in a subject; or (B) (a) for preventing or treating an infection caused by an electron transport-deficient bacteria in a subject; or (b) for the disinfection, sterilization and/or antisepsis of an object contaminated with an electron transport-deficient bacteria. There are provided compositions and kits using such compounds and inhibitors. 2. The method of claim 1 , wherein R3 is —C(CH)(NHR9) claim 1 , and R4 is H claim 1 , with the proviso that when R1 is OH and R2 is H claim 1 , R9 is substituted or unsubstituted alkyl.3. The method of claim 1 , wherein R9 is substituted or unsubstituted alkyl.4. The method of claim 3 , wherein R9 is —(CH)qCHR15R16 claim 3 , wherein q is 1 to 6.5. The method of claim 4 , wherein R15 and R16 are (i) identical or different and are selected from the group consisting of H claim 4 , substituted or unsubstituted alkyl claim 4 , substituted or unsubstituted aryl claim 4 , substituted or unsubstituted cycloalkyl claim 4 , and substituted or unsubstituted aralkyl claim 4 , wherein substituted alkyl claim 4 , substituted aryl claim 4 , substituted cycloalkyl claim 4 , substituted aralkyl and substituted —(CH)pNR13R14 comprises one or more identical or different substitutions selected from alkyl claim 4 , aryl claim 4 , cycloalkyl and aralkyl; (ii) are identical or different and are selected from the group consisting of H claim 4 , substituted or unsubstituted alkyl; (iii) identical or different and are selected from the group consisting of H and unsubstituted alkyl; (iv) identical or different and are selected from the group consisting of H and —CH; (v) H; or (vi) —CH.6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. The method of claim 1 , wherein q is 2 or 3.12. The method of claim 1 , wherein q is 2.13. ...

Atp synthase inhibitors and steroid alkaloids and uses thereof as antimicrobial agents and as potentiators for aminoglycosides against pathogenic bacteria

The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): (Formula (I)) (A) in combination with an aminoglycoside antibiotic for preventing or treating a bacterial infection in a subject; or (B) (a) for preventing or treating an infection caused by an electron transport-deficient bacteria in a subject; or (b) for the disinfection, sterilization and/or antisepsis of an object contaminated with an electron transport-deficient bacteria. There are provided compositions and kits using such compounds and inhibitors.

Steroid alkaloids and uses thereof as antimicrobial agents against electron transport-deficient microbes and as potentiators for antimicrobial agents against pathogenic bacteria

The present invention includes novel compounds based on the tomatidine skeleton as well as composition comprising these compounds alone and in combination with known compounds, which exhibit antimicrobial activity against extracellular or intracellular electron transport-deficient microbes and/or increase the antimicrobial activity of aminoglycoside antibiotics against their targets, and which are useful as antibacterial agents for treatment or prophylaxis of monomicrobiotic or polymicrobic bacterial infections or for the reduction of antibiotic resistance development in animals or in humans, or for use as antiseptics or agents for sterilization or disinfection.

Steroid alkaloids and uses thereof as antimicrobial agents against electron transport-deficient microbes and as potentiators for antimicrobial agents against pathogenic bacteria

The present invention includes novel compounds based on the tomatidine skeleton as well as composition comprising these compounds alone and in combination with known compounds, which exhibit antimicrobial activity against extracellular or intracellular electron transport-deficient microbes and/or increase the antimicrobial activity of aminoglycoside antibiotics against their targets, and which are useful as antibacterial agents for treatment or prophylaxis of monomicrobiotic or polymicrobic bacterial infections or for the reduction of antibiotic resistance development in animals or in humans, or for use as antiseptics or agents for sterilization or disinfection.

Atp synthase inhibitors and steroid alkaloids and uses thereof as antimicrobial agents and as potentiators for aminoglycosides against pathogenic bacteria

Atp synthase inhibitors and steroid alkaloids and uses thereof as antimicrobial agents and as potentiators for aminoglycosides against pathogenic bacteria