Lipopospohonoxins – novel broad spectrum antimicrobial agents

INTRODUCTION:

Growing antimicrobial resistance to currently available antibiotics poses a major threat to public health worldwide and presents an urgent need for novel effective antimicrobial compounds. Here, we present a novel class of antimicrobial compounds with low potential for resistance development.

TECHNOLOGY (INVENTION) DESCRIPTION:

The compounds show significant inhibitory and bactericidal activities against a broad spectrum of clinically relevant Gram-positive and Gram-negative pathogens, including resistant strains. Our compounds selectively target the bacterial membrane. Their action is rapid, allowing the pathogens limited time to develop resistance mechanisms. Our compounds do not damage eukaryotic cell membranes (at therapeutically relevant concentrations) and show no in vivo toxicity up to a dose of 2000 mg/kg (when administered orally to mice). They are well tolerated when applied on the skin or into the eye. As the compounds do not absorb through the gastrointestinal tract, they are intended for topical treatment.

ADVANTAGES OVER EXISTING SOLUTIONS:

Mechanism of action distinct from currently approved treatments. Effective against resistant strains. Low potential for resistance development. Excellent ocular and dermal tolerance.

DEVELOPMENT STATUS (STAGE):

preclinical (in vitro evidence, in vivo study ongoing)

PUBLICATIONS:

Seydlová G, Pohl R, Zborníková E, Ehn M, Šimák O, Panova N, Kolář M, Bogdanová K, Večeřová R, Fišer R, Šanderová H, Vítovská D, Sudzinová P, Pospíšil J, Benada O, Křížek T, Sedlák D, Bartůněk P, Krásný L, Rejman D. Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents. J Med Chem. 2017 Jul 27;60(14):6098-6118. doi: 10.1021/acs.jmedchem.7b00355. Epub 2017 Jul 12.

IP PROTECTION STATUS:

EP 2 527 351 B1, 11.12.2013

TECHNOLOGY / IP OWNERS :

Ústav organické chemie a biochemie AV ČR, v.v.i., 166 10 Praha 6 (CZ) Mikrobiologický ústav AV ČR, v.v.i. 142 20 Praha 4 - Krc (CZ) Ústav molekularní genetiky AV ČR, v.v.i. 142 20 Praha 4 (CZ) Trios, spol. s r.o. (CZ)

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