43 results about "Peptide deformylase" patented technology

The present invention provides methods and compositions for increasing the susceptibility of PDF inhibitors against Gram-negative organisms by using efflux pump inhibitors.

PDF inhibitors and novel methods for their use are provided.

Nobel PDF inhibitors and novel methods for their use are provided.

A macrocyclic peptide deformylase (PDF) inhibitor comprising a peptide or peptide mimetic having three residues, P1′, P2′, and P3′, wherein P2′ connects P1′ and P3′, wherein P1′ and P3′ each have a side chain, and wherein the side chains on P1′ and P3′ are crosslinked to form the macrocyclic PDF inhibitor. The side chains of P1′ and P3′ interact with the PDF active site, and preferably, P2′ has a side chain that interacts with a solvent. Also provided are methods of inhibiting the growth of a bacterium, the methods comprising contacting the bacterium with an anti-bacterial effective amount of the inventive macrocyclic PDF inhibitor. Additionally, a method of treating a bacterial infection in a subject comprising administering an effective amount of a macrocyclic PDF inhibitor to a subject in need of treatment. Additionally, methods of preparing macrocyclic PDF inhibitors comprising a) choosing an acyclic base molecule, having at least some PDF inhibitory activity, the acyclic base molecule having a first residue having a first side chain that interacts with the PDF active site and a second residue having a second that interacts with the PDF active site; and b) crosslinking the first side chain and the second side chain to form a macrocyclic PDF inhibitor.

The invention relates to a method of identifying herbicides and to the use of inhibitors of plant peptide deformylase as broad spectrum herbicides.

This invention provides compounds and methods for using them to inhibit the growth of microorganism that expresses Peptide Deformylase, the compounds having the general formula:

The present invention relates to the novel antibacterial compounds having potent antibacterial activity as inhibitors of peptide deformylase. This invention further relates to pharmaceutically acceptable salts thereof, to processes for their preparation, and to pharmaceutical compositions containing them as an active ingredient.

The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.

The invention discloses a novel peptide deformylase inhibitor containing spiro-three-membered ring and spiro-five-membered ring types. The novel peptide deformylase inhibitor containing the spiro-three-membered ring and spiro-five-membered ring types has antibacterial activity and anti-tumor activity. The peptide deformylase inhibitor containing the spiro-three-membered ring and spiro-five-membered ring types can serve as a novel antibacterial agent, by inhibiting the activity of peptide deformylase needed in synthesis of bacterium proteins, the novel peptide deformylase inhibitor is effective on multiple antibiotic resistant Gram-positive bacterium strains, the synthesis process of proteins of human bodies is not affected, and accordingly bacteria are killed selectively. The peptide deformylase inhibitor containing the spiro-three-membered ring and spiro-five-membered ring types can further serve as a novel anti-cancer drug; by inhibiting peptide deformylase in mitochondria of cancer cells, energy balance of the cells can be affected, accordingly mitochondrial membranes are depolarized, ATP is used up, and cell apoptosis is promoted; and the novel peptide deformylase inhibitor has good inhibiting activity to multiple cancer cell bacterial strains such as colorectal cancer cell bacterial strains, lung cancer cell bacterial strains, gastric cancer cell bacterial strains and liver cancer cell bacterial strains at the low concentration.

Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of: