antibacterial compound 1

Antibacterial compound 1 is an antibacterial compound.

Chlamydia pneumoniae-IN-1 (compound 55), a benzimidazole derivative, exhibits potent antibacterial activity, inhibiting 99% of C. pneumoniae growth at a concentration of 10 μM while maintaining 95% viability of host cells. It effectively inhibits the CV-6 strain of C. pneumoniae with a minimum inhibitory concentration (MIC) of 12.6 μM, demonstrating its antichlamydial efficacy [1].

D-(+)-Phenyllactic acid (D-3-Phenyllactic acid), an antibacterial compound produced by Geotrichum candidum, effectively inhibits various Gram-positive and Gram-negative bacteria originating from humans and food products[1].

Ppc-1 is a chemical compound known for its inhibitory effects on the Gram-negative periodontopathogen Porphyromonas gingivalis. It acts as a mitochondrial uncoupler, enhancing mitochondrial oxygen consumption without affecting ATP production. Additionally, Ppc-1 serves as a cell-permeate inhibitor of interleukin-2 (IL-2). This compound exhibits various beneficial activities, including anti-obesity, antibacterial, and anti-inflammatory properties.

Arcopilin A (compound Arcopilin A(1)) functions as an antibacterial agent with moderate inhibitory capabilities against fungal pathogens and Gram-positive bacteria, exhibiting IC 50 values of 8.9 μg mL for KB-3-1 cells and 14 μg mL for L929 cells. Notably, it can effectively eradicate preformed biofilms of Staphylococcus aureus. Additionally, Arcopilin A significantly boosts the efficacy of gentamicin (GM) and vancomycin (Vac), enhancing their activities by 115 and 31 times, respectively.

Antimicrobial agent-34 (compound 4h), characterized by its clogP value of 9.14, effectively disrupts the integrity of bacterial cell membranes. This compound boasts a minimum inhibitory concentration (MIC) ranging from 1–4 μg mL and shows notable plasma stability with an HC50 of 131.1 μg mL. Additionally, it exhibits excellent membrane selectivity, as evidenced by its HC50 MIC ratio of 65.6, and possesses rapid sterilization capabilities. It not only increases intracellular reactive oxygen species but also causes the leakage of protein and DNA, culminating in bacterial death. Antimicrobial agent-34 has demonstrated significant antibacterial effectiveness in vivo, particularly in a mouse sepsis model infected with Staphylococcus aureus ATCC43300.

Cerastecin D (compound 1), an antibacterial agent, demonstrates effectiveness by inhibiting Acinetobacter baumannii ATCC19606 with MITC 95 values at 165 nM.

TcNTPDase1-IN-1 (compound 16) serves as an inhibitor of nucleoside triphosphate diphosphohydrolase 1 (TcNTPDase1) from Trypanosoma cruzi in vitro. This compound is applicable in research related to antibacterial, antitoxic, and antitumor activities.

HldA E-IN-1 (compound 8) is a dual inhibitor of HldA E, exhibiting IC50 values of 17.2 μM and 67.8 μM, respectively. This compound is utilized in research on antibacterial infections.

Antibacterialagent 244 is a compound that exhibits broad-spectrum antibacterial activity and oral efficacy, primarily targeting Gram-positive bacteria with a minimum inhibitory concentration (MIC) of 1-4 μg mL. It possesses low hemolytic toxicity (HC50 of 111.6 μg mL). The mode of action for Antibacterialagent 244 involves disrupting the bacterial transmembrane potential and increasing membrane permeability, which leads to the leakage of cellular contents such as DNA and proteins, ultimately causing bacterial death. This compound is useful in research related to infections caused by Gram-positive bacteria.

Antibiofilm agent-13 (compound 14b) is an effective broad-spectrum antibacterial agent that functions by disrupting the integrity of bacterial cell membranes. It achieves this through the degradation of transmembrane potential and increased membrane permeability, which leads to the production of intracellular ROS and the leakage of DNA and proteins, ultimately resulting in bacterial death. Antibiofilm agent-13 effectively inhibits both Gram-positive bacteria (MIC ranging from 0.5-1 μg mL) and Gram-negative bacteria (MIC ranging from 1-32 μg mL).

1-Amino-2,5-anhydro-1-deoxy-D-mannitol is a potent antibacterial compound effective against various Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). Its application potential lies in its ability to combat common antibiotic-resistant bacterial infections effectively. 1-Amino-2,5-anhydro-1-deoxy-D-mannitol may emerge as a novel antimicrobial agent in clinical inhibition.

Carbonic anhydrase inhibitor28 (Compound 11) serves as an inhibitor for the Pseudomonas aeruginosa carbonic anhydrase. It exhibits antibacterial activity, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 0.5 and 1 μg mL, respectively, against P. aeruginosa. Carbonic anhydrase inhibitor28 is utilized in research focused on anti-infection applications.

Antibacterialagent 255 (compound (±)-1) is a potent antibacterial agent, acting as an effective and selective inhibitor of 4-diphosphocytidyl-2-C-methyl-D-erythritol (IspE). It exhibits IC50 values of 13.0, 8.0, and 20 µM against EclspE, KplspE, and AblspE, respectively.

Anti-MRSA agent 21 (Compound 27) demonstrates antibacterial activity against MRSA with a minimum inhibitory concentration (MIC) of 1 μM. It disrupts the bacterial cell membrane and increases reactive oxygen species.

Antibacterialagent 119 (Compound 21 g) is a potential antibacterial agent effective against methicillin-resistant Staphylococcus aureus, with a minimum inhibitory concentration (MIC) of less than 1 μg mL against tested strains. It induces reactive oxygen species (ROS) generation and disrupts bacterial cell membranes, causing their rupture. Antibacterialagent 119 exhibits strong antimicrobial activity, low cytotoxicity, rapid bactericidal action, and favorable in vivo antibacterial efficacy.

DNA gyrase Topo IV-IN-1 (Compound 27) is an inhibitor of DNA gyrase and topoisomerase IV with antibacterial properties. It exhibits IC50 values of 11 and 17 nM against the DNA gyrase of Escherichia coli and methicillin-resistant Staphylococcus aureus, respectively, and IC50 values of 83 and 21 nM against topoisomerase IV of the same organisms. DNA gyrase Topo IV-IN-1 is applicable in anti-infective research.

Antimicrobial-IN-1 (compound 17) demonstrates potent antibacterial activity against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli), exhibiting inhibition zone diameters of 18 mm mg and 16 mm mg, respectively.

NDM-1 inhibitor-8 (Compound 18b) is a covalent inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1), with an IC50 of 7.03 μM. It effectively inhibits resistant bacterial strains and demonstrates synergistic antibacterial effects when used in combination with Meropenem. In mouse models, NDM-1 inhibitor-8 exhibits anti-infective activity.

Pks13-IN-1 (Compound 44) is an orally active inhibitor of Mycobacterium tuberculosis polyketide synthase 13 (Pks13). It inhibits the M. tuberculosis H37Rv strain with a minimum inhibitory concentration (MIC) of 0.07 μM. In mouse models, Pks13-IN-1 demonstrates antibacterial activity.

FtsZ-IN-12 (Compound 16e) is an inhibitor of filamentous temperature-sensitive mutant Z (FtsZ) that promotes the polymerization of the FtsZ protein and suppresses its GTPase activity, thus disrupting the bacterial cell division process. This compound exhibits broad-spectrum antibacterial activity, effectively inhibiting B. subtilis ATCC 9372, B. pumilus CMCC 63202, S. aureus ATCC 25923, E. coli BW25113, and A. baumannii ATCC 19606 with MIC values ranging from 0.062-1 µg mL. Additionally, FtsZ-IN-12 can inhibit biofilm formation and eliminate mature biofilms. It possesses bactericidal properties and shows no hemolytic toxicity to mammalian red blood cells at a dosage of 15 mg kg.

BioA-IN-1 (Compound 15) is an inhibitor of the key enzyme BioA in the biotin biosynthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. It exhibits antibacterial activity without cytotoxicity.

NDM-1 inhibitor-7 (Compound A8) is an NDM-1 inhibitor with an IC50 of 10.284 μM. It restores the ability of meropenem (MEM) to penetrate the cell wall of Gram-negative bacteria and effectively reinstates MEM's antibacterial activity against NDM-1 positive Escherichia coli. Moreover, NDM-1 inhibitor-7 demonstrates significant efficacy in both Galleria mellonella and murine peritonitis infection models.

Antibiofilm agent prodrug 1 (Compound 5c) demonstrates antibacterial properties by inhibiting biofilm formation and iron uptake. It effectively suppresses Pseudomonas aeruginosa PAO1 with a minimum inhibitory concentration (MIC) of 1.07 μM. In addition, Antibiofilm agent prodrug 1 exhibits anti-infective activity in Caenorhabditis elegans, enhancing the survival rate of the nematodes.