antibacterial agent

Antibacterial agent 132 showed antimicrobial activity against C. parapsilosis (ATCC 22019) and C. krusei (ATCC 6258) with MIC90 values of <0.06 μg/mL and 62.50 μg/mL, respectively. Antibacterial agent 132 inhibited aromatase enzyme with IC50 of 0.047 μM.

4-(4,5-dibromo-6-oxo-1,6-dihydropyridazin-1-yl)benzene-1-sulfonamide is a sulfonamide derivative used in the synthesis of building blocks for various supramolecular structures such as metal-organic skeletons and coordination polymers. It has antiproliferative activity against a variety of tumor cell lines.

(2S)-4-biphenyl-4-yl-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide is a LpxC inhibitor with IC50 >95.2 nM.

Antibacterial agent 162 trifluoromethanesulfonate (compound 7), a dual-function molecule, demonstrates potent inhibitory effects on Staphylococcus aureus, encompassing MRSA strains, and exerts antiproliferative activity against colon cancer and non-small cell lung cancer cells. This compound is applicable in both anticancer and antibacterial research [1].

Compound 6 (Antibacterial agent 161, trifluoromethanesulfonate) exhibits antibacterial properties and demonstrates significant antiproliferative effects against colon cancer and non-small cell lung cancer [1].

Antibacterial Agent 160 is a potent antibacterial agent that rapidly eradicates bacteria and inhibits the formation of bacterial biofilms. It disrupts the normal functioning of DNA, resulting in cellular death [1].

Antibacterial agent 163 (compound 1), a hydroxyquinoline derivative, potently inhibits methicillin-resistant Staphylococcus aureus (MRSA) [1].

Antibacterial agent 165 (compound 3), a hydroxyquinoline derivative, effectively inhibits methicillin-resistant Staphylococcus aureus (MRSA) [1], demonstrating its potent antibacterial properties.

Antibacterial agent 66 (Compound 6q) is a trifluoromethylpyridine 1,3,4-oxadiazole derivative active against Xanthomonas oryzae pv. oryzae (Xoo) (EC50: 7.2 μg/mL).

Antibacterial agent 37 is an effective antimicrobial compound. It holds potential as a valuable tool for researching bacterial infections.

Antibacterial Agent 42 demonstrates potent antibacterial activity by effectively reducing the Minimum Inhibitory Concentration (MIC) of the broad-spectrum antibacterial agent Ceftazidime.

Antibacterial agent 30 exhibits remarkable in vitro activity against Xoo, as evidenced by its EC50 value of 1.9 μg/mL.

Antibacterial agent 57 (example 25) is a antibacterial agent.

Antibacterial agent 88 is an effective antibacterial agent against B. subtilis (MIC: 4 μg/ml) with MIC values of ≤0.0156 μg/mL for MRSA, MRSE and S. aureus.

Antibacterial agent 131 is a compound with antibacterial properties.

Antibacterial agent 92, a triple-site aminoacyl-tRNA synthetase (aaRS) inhibitor, demonstrates a potent antibacterial effect by inhibiting Salmonella enterica threonyl-tRNA synthetase (SeThrRS) with an IC50 of 0.58 μM.

Aztreonam-siderophore conjugate 63 is an antibacterial agent that exhibits efficacy against Gram-negative bacteria through the linkage of aztreonam to a siderophore mimetic.

Compound A11 (Antibacterial agent 86) exhibits the highest bacteriostatic activity against methicillin-resistant S. aureus, with minimum inhibitory concentration (MIC) values reaching as low as 0.00191 μg/mL. This efficacy is 162 and 32 times greater than the commercial antibiotics tiamulin and retapamulin, respectively [1].

Antibacterial Agent 136 (Compound 3), an oxadiazolone antibiotic, exhibits high antibacterial potency against Methicillin-resistant Staphylococcus aureus (MRSA), with a minimum inhibitory concentration (MIC) 50 value of 0.8 μM [1].

Antibacterial agent 116, a benzophenone-containing salicylanilide compound, exhibits potent antibacterial activity by inhibiting peptidoglycan formation. It is employed as a photoaffinity probe to label Acinetobacter baumannii penicillin-binding protein (PBP1b), thereby blocking the propagation pathway and disrupting the growth of the peptidoglycan chain.

Antibacterial Agent 128, a siderophore analog-Ciprofloxacin (Ciprofloxacin) conjugate connected via a cleavable linker, demonstrates effective antibiotic properties. Specifically, it exhibits activity against P. aeruginosa and B. pseudomallei, with Minimum Inhibitory Concentration (MIC) values ranging from 0.25 to 64 μg/mL and 1 to 32 μg/mL, respectively [1].

Antibacterial Agent 123 (Compound 111) serves as an effective membrane-disrupting agent targeting antibiotic-resistant Gram-positive bacteria [1].

Antibacterial agent 75 (compound 24) possesses antibacterial properties. Its notable attribute is the ability to re-sensitize VRSA (Vancomycin-Resistant Staphylococcus aureus) strains to vancomycin, as reported in reference [1].

Antibacterial agent 46, serves as a potent antibacterial compound. With its versatile properties, this agent demonstrates considerable potential for supporting research on bacterial infections.

Antibacterial agent 101 exhibited antibacterial and antifungal effects (MIC=4-32 μg/mL).

Antibacterial agent 98 (compound g37) is an effective oral antibacterial agent, which can inhibit the ATPase activity of Gyrase B and weaken the DNA super-helix of S. aureus. Antibacterial agent 98 does not induce the development of MRSA (methicillin-resistant Staphylococcus aureus) resistance.

Antibacterial Agent 33, a potent antibacterial compound, effectively decreases the minimum inhibitory concentration (MIC) of Ceftazidime, another antibacterial agent.

Antibacterial agent 80 (compound 20) has antibacterial activity [1].

Antibacterial agent 32 exhibits potent antimicrobial activity against E. coli strains NCTC 13351, M 50, and 7 MP, with minimum inhibitory concentration (MIC) values of 1 mcg/mL, 2 mcg/mL, and 8 mcg/mL, respectively (WO2013030733A1, example 43).

Antibacterial agent 62 is a novel redox cycle anti-tuberculosis compound that exhibits significant bactericidal activity against growth and nutrient deficient phenotypically resistant non-growing bacteria.

Antibacterial agent 55 (example 21) is a antibacterial agent.

Antibacterial agent 48 is an antimicrobial agent that reduces the MIC of the antimicrobial agent Ceftazidime.

Antibacterial agent 94 (compound 5b) is a highly effective antibacterial agent that demonstrates strong activity against various bacterial strains. Notably, Antibacterial Agent 94 is capable of eradicating MRSA persisters, highlighting its potential as a therapeutic solution. Its mechanism of action involves interference with the bacterial membrane and disruption of the phosphatidylglycerol (PG) synthesis pathway [1].

Antibacterial agent 27 has potent anti-Candida activity.

Antibacterial agent 79 is an antibacterial agent.

Compound B12 (Antibacterial agent 157) is a fungicidal agent that can impact protein synthesis in Botrytis cinerea. It is utilized in research for controlling gray mold resistance [1].

Compound B14 (Antibacterial agent 141) exhibits antibacterial activity against the plant pathogens Xoo, Xac, Psa, and Cmm, with an EC50 value of 1.28 μM. It functions by inhibiting cell membrane formation and altering cell permeability.

Antibacterial Agent 144 (compound 8e) exhibits superior efficacy against multi-resistant Staphylococcus aureus compared to Chloromycin and Amoxicillin. It acts by disrupting the bacterial cytoplasmic membrane and inhibiting biofilm formation. Additionally, it binds to human serum albumin (HSA) with a dissociation constant (Kd) of 13.2 μM, enhancing its bactericidal activity. This compound also forms a supramolecular complex with DNA, thereby hindering DNA replication [1].

Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when administered orally. It has been shown to be effective in vivo using a mouse model of staphylococcal sepsis [1].

Antibacterial agent 52 (example 18) is a antibacterial agent.

Antibacterial agent 111 (Compound 3) exhibits potent antibacterial activity against B. cereus and K. pneumonia, with MIC values of 3.90 μg/mL and 0.49 μg/mL, respectively. It achieves this antibacterial effect by strongly binding to specific residues of tyrosyl-tRNA synthetase [1].

Antibacterial agent 99 (compound 7b) is an effective antibacterial agent. antibacterial agent 99 has significant antibacterial and antifungal effects and no haemolytic activity.

Antibacterial Agent 96 (Compound 4k) is a potent antibacterial and antitubercular compound effective against both drug-susceptible and multidrug-resistant Mycobacterium tuberculosis (M. tuberculosis) strains. However, it exhibits toxicity to HepG2 and Vero cells [1].

Antibacterial agent 124 is a potent inhibitor of bacterial prolyl-tRNA synthetase (ProRS), specifically targeting Staphylococcus aureus ProRS (Sa ProRS) with an inhibitory concentration (IC50) of 0.18 μM.

Antibacterial agent 12, a biaryloxazolidinone analogue, effectively combats both antibiotic-susceptible and antibiotic-resistant Gram-positive bacteria [1].

The compound demonstrates enhanced potency against wild-type (WT) strains of Escherichia coli, Acinetobacter baumannii, and Burkholderia cenocepacia, showing significant improvements of up to (>128-fold) due to increased outer-membrane permeability in hyperpermeable E. coli strains and S. Tm.

Antibacterial agent 69 is a novel structural antimicrobial modulator that can be used against lethal multidrug-resistant bacterial infections (MIC: 2.978 μM).

Antibacterial agent 113 was an effective antimicrobial agent (antibacterial) against P. aeruginosa, S. mutans, B. subtilis, E. coli, E. faecalis, S. typhimuriumand and S. aureus microorganisms exhibited antibacterial effects with MIC values of 15625 μM.

Antibacterial agent 65 is a potential antimicrobial agent and antioxidant agent.

Antibacterial agent 104 is an effective antibacterial agent with significant antibacterial effects in vitro and good anti-MRSA effects in vivo.