Antibacteriano

<p>Streptothricin F is a biochemical.</p>

<p>Altersolanol A (Stemphylin; NSC 173943) demonstrates effective antimicrobial properties, inhibiting the growth of Bacillus subtilis and Pseudomonas aeruginosa with a minimum inhibitory concentration (MIC) ranging from 25-100 μg/mL. Additionally, it shows no phytotoxic effects on Taxus at a concentration of 4 μg/μL.</p>

<p>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.</p>

<p>Compound 174 (Compound 5g), an antibacterial agent, exhibits potent anti-infective properties in vivo along with appreciable pharmacokinetic profiles. This highly active substance demonstrates favorable biofilm removal capabilities, low hemolysis, and acceptable mammalian cell toxicity [1].</p>

<p>LpxA-IN-1, a novel UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitor exhibiting potent activity (IC 50 2 nM), effectively targets Pseudomonas aeruginosa</p>

<p>Antimicrobial Agent-29 (Compound C35) influences the interaction between human hemoglobin and the Staphylococcus aureus IsdB hemophore. This compound facilitates the identification of IsdB:Hb PPI inhibitors [1].</p>

<p>Metallo-β-lactamase-IN-14 (Compound 17e) serves as an inhibitor of Metallo-β-Lactamase, displaying inhibitory activity against VIM-1 and VIM-2. This compound also exhibits antibacterial effects on Gram-negative (GN) bacteria and P. aeruginosa [1].</p>

<p>Antibacterial Agent 172 (Compound 6a), a &lt;i&gt;Clostridioides difficile (Cd) SpoVD inhibitor with an IC50 value of 89 nM, effectively inhibits the sporulation of Clostridioides difficile. It is useful for research on bacterial infections [1].</p>

<p>844-TFM, a NBTI DNA gyrase blocker, IC50: 1.5 μM, kills Mycobacterium abscessus.</p>

<p>OPC-167832: oral dprE1 inhibitor, IC50 0.258 μM, anti-tuberculosis, for Mycobacterium tuberculosis research.</p>

<p>Antibacterialagent 279 (compound A12) is an effective antibacterial agent. It inhibits the SOS response of Pseudomonas aeruginosa.</p>

<p>Antifungal agent 27 shows moderate action against MRSA, weak against C. albicans, with MICs of 8 μg/mL and 32 μg/mL, respectively.</p>

<p>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.</p>

<p>DL-2-Aminopimelic Acid acts as a weak agonist for glutamate receptors and also reduces the sensitivity of leech glutamate receptors to glutamate.</p>

<p>Compound 5q is a potent antitubercular with low MIC90 values (0.40-23.51 μg/mL) against M. tuberculosis strains, showing minimal cytotoxicity.</p>

<p>Elongation factor P-IN-2, a β-lysine derivative, is a potent EFP inhibitor reducing E. coli growth.</p>

<p>VEGFR-2/DHFR-IN-2 inhibits VEGFR-2 &amp; DHFR (IC50: 0.623 &amp; 9.085 μM), toxic to C26, HepG2, MCF7 cells (IC50: 3.59-8.38 μM), promising for cancer study.</p>

<p>Rubropunctatin is a monascus pigment with very potent cancer cell proliferation inhibitory effects.</p>

<p>RmlA-IN-2: Strong RmlA blocker, hinders l-rhamnose synthesis &amp; alters bacterial wall permeability (IC50: 0.303 μM).</p>

<p>Antibacterial agent 118, potent against various mycobacteria, has MIC values ranging from 10.2 to 163.0 μM. Useful in TB research.</p>

<p>LpxC-IN-10 is a selective LpxC inhibitor with an MIC of 0.5 μg/mL against E. coli and K. pneumoniae and is capable of being used to study bacterial infections.</p>

<p>LasR-IN-3 inhibits LasR in Pseudomonas, disrupting its dimer, causing loss of function.</p>

<p>PqsR-IN-2, potent PqsR inhibitor, curbs Pseudomonas aeruginosa communication, reduces pyocyanin, with low toxicity.</p>

<p>FG-2101 is a selective, orally active non-hydroxamate LpxC inhibitor with an IC50 of approximately 1 nM. It demonstrates exceptional selectivity over other bacterial and human metalloproteases. FG-2101 is useful for studying infections caused by Gram-negative bacteria, including resistant strains.</p>

<p>Antibacterial agent 77 (compound 12) is an antibacterial agent [1].</p>

<p>GSK656 (GSK3036656) inhibits Mtb LeuRS with IC50 of 0.20 μM, promising for tuberculosis treatment.</p>

<p>PptT-IN-3 (5p), an inhibitor of PptT in Mycobacterium tuberculosis, IC50=3.5μM, is key for TB research.</p>

<p>RhlR antagonist 1: IC50 of 26 μM, selective for RhlR, inhibits P. aeruginosa biofilm and virulence factors.</p>

<p>Antitubercular agent-11 (Compound 1e) is an antitubercular agent with a bulkier electron-donating group (Bu-t) that shows the best MIC value of 0.060 μg/mL [1].</p>

<p>MtTMPK-IN-2 inhibits M. tuberculosis TMPK (IC50: 1.1 μM), Mtb H37Rv (MIC: 12.5 μM), and is cytotoxic in MRC-5 cells (EC50: 6.1 μM).</p>

<p>NFC nitro probe 1 (compound 18) is a chemical probe designed for the detection of Mtb, exhibiting high potency against both R-Mtb and NR-Mtb.</p>

<p>Probenecid sodium is the sodium salt of Probenecid, a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Additionally, Probenecid acts as an inhibitor of pannexin 1 channels.</p>

<p>Antibacterialagent 262 (compound A23) is a potent antibacterial agent that inhibits the activity of Xanthomonas oryzae pv oryzae. It also disrupts the integrity of bacterial cell membranes by preventing the formation of biofilms of Xanthomonas oryzae pv oryzae.</p>

<p>Cephalosporin C exhibits relatively weak resistance to Gram-positive and Gram-negative bacteria. It is stable against penicillinase, but can be decomposed by cephalosporinase. When hydrolyzed to remove its side chain, it yields 7-amino-cefenoic acid (7-ACA), which is an essential raw material for the production of semisynthetic cephalosporins.</p>

<p>Colistin adjuvant-2 is a compound that acts as a potentiation agent for colistin, effectively enhancing its activity against Gram-negative bacteria [1].</p>

<p>MurA-IN-6 (Compound L16) is a selective MurA inhibitor with an IC50 of 26.63 μM. It exhibits antibacterial activity by inhibiting the function of MurA, a key protein essential for bacterial cell wall synthesis.</p>

<p>4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.</p>

<p>NBTIs-IN-5 inhibits Mycobacterium abscessus DNA with IC50 1.5μM, halts growth at MIC90 0.4μM.</p>

<p>Diclosulam (XDE 564) is an herbicide with a Ki value of less than 32 nM. It exhibits a MIC of 6.25 and 12.5 μM, and a MIC50 of 1.40 and 3.01 μM against the CBS10913 and CBS12373 strains, respectively.</p>

<p>Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding to the PqsR protein. It suppresses the expression of quorum sensing system-related genes lasB, rhlA, and pqsA, thereby preventing the production of virulence factors elastase, pyocyanin, and rhamnolipid. Quorum sensing-IN-9 disrupts the motility of P. aeruginosa, inhibits biofilm formation, and reduces the bacterium's virulence and pathogenicity. Additionally, it exhibits anti-infective activity in the Galleria mellonella larval model.</p>

<p>MsbA-IN-4 (Compound 32) is a highly selective and potent inhibitor of MsbA (IC50: 3 nM).MsbA-IN-4 inhibits Escherichia coli (MIC: 12 μM).</p>

<p>MsbA-IN-5 (compound 40) is a potent and highly selective inhibitor of MsbA (IC50: 2 nM). MsbA-IN-5 can be used in Gram-negative studies.</p>

<p>Antibiofilm agent-14 (compound 11) functions as an antibiofilm agent. It exhibits antifungal activity against C.albicans SC5314, with a minimum inhibitory concentration (MIC) of 50 μM.</p>

<p>Antimicrobial agent-38 (compound 10) effectively inhibits methicillin-resistant Staphylococcus aureus (S. aureus) strain ATCC 700699 and non-resistant strain ATCC 29213, with minimum inhibitory concentrations (MIC) of 32 mg/L and 64 mg/L, respectively.</p>

<p>Antibacterial agent 76 (compound 9) is a potent antibacterial agent.</p>

<p>FtsZ-IN-13 (Compound C11) functions as an inhibitor of the temperature-sensitive mutant Z (FtsZ), exhibiting IC50 values of 47.97 μM for FtsZSa and 34 μM for FtsZPa. It demonstrates notable antibacterial activity against Staphylococcus aureus (with a minimum inhibitory concentration of 2 μg/mL), cystic fibrosis Staphylococcus aureus clinical isolates, and methicillin-resistant Staphylococcus aureus (MRSA). FtsZ-IN-13 is applicable in research on antibiotic resistance.</p>

<p>MtTMPK-IN-8 inhibits MtbTMPK, has low cytotoxicity, shows 0.78-9.4 μM activity against Mycobacterium, useful for tuberculosis research.</p>

<p>ACHN-975: potent LpxC inhibitor with subnanomolar activity; targets many gram-negative bacteria; MIC ≤1 μg/mL.</p>

MB076 is an innovative heterocyclic triazole designed with enhanced plasma stability. It effectively inhibits seven distinct Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with K i values less than 1 μM. Additionally, MB076 demonstrates a synergistic effect when combined with various cephalosporins to restore pBCSK(−) susceptibility [1].

<p>(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium TFA (Compound 4a) functions as a Gram-negative outer membrane permeabilizer by targeting Met47 in LptA to disrupt LptA/LptC interactions, exhibiting synergistic antibacterial activity. This compound, when in the form of (trifluoromethanesulfonate), enhances the efficacy of pol B against both wild-type and multi-drug resistant A. baumannii and E. coli strains. Additionally, (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) serves as an adjuvant for antibiotics combating multi-drug resistant Gram-negative bacteria.</p>