antimicrobial-in-1

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.

ClpB-IN-1 is a potential antimicrobial agent.ClpB-IN-1 is a potent ClpB inhibitor.

CTP Synthetase-IN-1 Ammonium salt is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antimicrobial, anti-inflammatory and antitumor activity for the study of SARS-CoV-2 viral infections.

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].

1. Octyl Gallate is an antioxidant approved by the US Food and Drug Administration (FDA) as a food additive. 2. Octyl Gallate has antimetastatic activity. 3. Octyl Gallate shows antimicrobial activity against H. pylori, with a minimum inhibitory concentration (MIC) value of 125 ug/mL. 4. Combination therapy with octyl gallate and ferulic acid improves cognition and neurodegeneration in a transgenic mouse model of Alzheimer's disease.5. Octyl Gallate is a potential anticancer agent, it exhibited decreased MCF-7 & MDA-MB-231 survival and induced apoptosis, with IC50 value of 40 uM. 6. Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) has antiviral activity, it shows an inhibitory effect on the growth of herpes simplex virus type 1 (HSV-1) in HEp-2 or Vero cells. 7. Octyl gallate shows antifungal activity against Saccharomyces cerevisiae ATCC7754 and Zygosaccharomyces bailii ATCC 60483.

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS/GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.

Sodium diacetate (Acetic acid, sodium salt (2:1)) is a salt of acetic acid. Sodium diacetate is a colorless solid that is used in seasonings and as an antimicrobial agent. As a kind of new-type grain, beverage additive of food, it is used in the food additive extensively.

cis-1-(3-Chloroallyl)-3,5,7-triaza-1-azoniaadamantane chloride (Quaternium-15 cis-form) is an antimicrobial agent used in cosmetics as a cosmetic preservative and antistatic agent.cis-1-(3-Chloroallyl)-3,5,7-triaza-1-azoniaadamantane chloride is an oral teratogen, but not a dermal teratogen, and has been dosed in rats at doses exceeding the expected cumulative exposures for cosmetics.

1. 4-Methoxybenzoic acid could be used as raw material in cosmetic and dermatologic products and/or aroma components in foodstuffs, it has antiinflammatory and antimicrobial activities.

TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.

Nigericin is a polyether antibiotic with potent antimicrobial, antimalarial, anticoronaviral and anticancer activities. It is capable of promoting cellular potassium efflux, inducing Caspase-1/GSDMD and Caspase-3-mediated cellular pyroptosis and apoptosis in triple-negative breast cancer, and inducing apoptosis in PEL (primary exudative lymphoma) cells through mitochondrial dysfunction and Wnt/β-catenin signaling downregulation.

N-Butanoyl-L-homoserine lactone (C4-HSL) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It exhibits antibacterial activity and is employed in antibacterial biofilm[1].

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.

ChlaDUB1-IN-1 (Compound 8) is an inhibitor of the Chlamydia deubiquitinase enzyme 1 (ChlaDUB1) and serves as a potential agent in antimicrobial research.

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.

Metallo-β-lactamase-IN-16 (compound 18), a sulfone-containing metallo-β-lactamase inhibitor, exhibits antimicrobial activity. It effectively inhibits various metallo-β-lactamases, including NDM-1 (New Delhi metallo-β-lactamase-1), IMP-1 (imipenemase-1), VIM-1 (Verona Integron-encoded Metallo-β-lactamase), and VIM-2. The IC50 values for these enzymes are 0.16 nM, 0.23 nM, 0.31 nM, and 1.0 nM respectively.

CPPD-Q is an antimicrobial and insecticidal agent. It exhibits an EC50 of 6.98 mg/L against Vibrio fischer. CPPD-Q, at doses of 1 or 10 µg/mL, exerts its insecticidal effects by inducing reactive oxygen species (ROS) production in the intestines of Caenorhabditis elegans.

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.

Antibacterialagent 258 (Compound 11e) is an antimicrobial agent capable of disrupting bacterial cell membranes and inhibiting various Gram-positive bacteria, with a MIC of 1-2 μg/mL against Staphylococcus aureus. It exhibits low hemolytic activity and cytotoxicity, and demonstrates anti-infective properties in mouse models.

Biotin protein ligase-IN-1 (Compound Bio-9) is an inhibitor of biotin protein ligase (BPL) with a Kd of 7 nM. This compound exhibits antimicrobial activity, with minimum inhibitory concentration (MIC) values of 0.2 μM against Staphylococcus aureus (including MRSA and MSSA) and 20 μM against Mycobacterium tuberculosis.

hERG-IN-1 (compound 2a) acts as both an antimicrobial agent and an hERG inhibitor. It is effective in suppressing lung infections caused by Pseudomonas aeruginosa strain ATCC 27853.

Indomethacin sodium hydrate is an effective orally active, competitive, and reversible inhibitor of COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. It possesses anti-inflammatory, anticancer, and antimicrobial activities and is commonly used in research related to cancer, inflammation, and viral infections. Additionally, it can induce migraines and gastrointestinal injury and is used to study increased intracranial pressure secondary to severe traumatic brain injury in adults, as well as rheumatoid arthritis. It can also be used to induce gastric ulcer models.

SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonist with an IC50=70 nM with antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects that attenuates thrombin-induced increase in CH25H expression in astrocytes, inhibits peritoneal dissemination of gastric cancer, and attenuates repetitive traumatic brain injury.

1. Negletein (7-O-Methylbaicalein) has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β. 2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. 3. Negletein shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. 4. Negletein shows significant antimicrobial activity. 5. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.6. Negletein has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. 7. Negletein (IC50: 3.89 +/- 0.39 microM) exhibits potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor.