Antifection

TMC207 is a first-in-class diarylquinoline compound with a novel mechanism of action, the inhibition of bacterial ATP synthase, and potent activity against drug-sensitive and drug-resistant TB.

Omadacycline tosylate is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.

Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells.

Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. Saquinavir inhibits both HIV-1 and HIV-2 proteases.

Capreomycin Sulfate is a cyclic peptide antibiotic and thought to inhibit protein synthesis by binding to the 70S ribosomal unit.

Amphotericin B is a polyene antifungal antibiotic from Streptomyces sp. Amphotericin B induces K+ leakage, which is separate from its lethal action, as was demonstrated in human erythrocytes and is due to the inhibitory effect on the Na+/K+ pump.

Imipenem is an intravenous betalactam antibiotic discovered by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in 1980.

Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.

Brincidofovir is a prodrug of cidofovir. Conjugated to a lipid, the compound is designed to release cidofovir intracellularly, allowing for higher intracellular and lower plasma concentrations of cidofovir, effectively increasing its activity against dsDNA viruses, as well as oral bioavailability.

Propylparaben is an antifungal agent.

Ethylparaben is the ethyl ester of p-hydroxybenzoic acid, used as an antifungal preservative and food additive. It is a standardized chemical allergen.

Nelfinavir is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.

AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).

Aciclovir is an antiviral agent primarily used for the treatment of herpes simplex virus infections, as well as in the treatment of varicella zoster (chickenpox) and herpes zoster (shingles). It was seen as the start of a new era in antiviral therapy, as it is extremely selective and low in cytotoxicity.

S/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones.

Elvitegravir (GS-9137) is a potent inhibitor of the strand-transfer step of integration mediated by human immunodeficiency virus type 1 (HIV-1) integrase.

Colistin is a cyclic cationic decapeptide linked to a fatty acid side chain, it belongs to a group of similarly structured bacterial antimicrobial peptides.

Retapamulin is an antibacterial agent, specifically a protein synthesis inhibitor

VX-787 is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex.

Bictegravir, also known as GS-9883, is a potent, unboosted, once-Daily HIV-1 Integrase Strand Transfer Inhibitor (INSTI) (IC50 - 1.6 nM) with improved pharmacokinetics and in vitro resistance profile.

Raltegravir (MK-0518) targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV.

BMS-663068 is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.

Bevirimat (MPC-4326, PA-457, YK-FH312) is a first-in-class HIV-1 maturation inhibitor that demonstrates high potency in cell culture and has shown clinical efficacy in HIV-1-infected patients.

Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. It acts by induction of DNA strand breaks.

PA-824 is an experimental anti-tuberculosis drug.

Amikacin sulfate binds to 16S rRNA (bacterial 30S ribosome), causing misreading of mRNA and supressing proteins synthesis.

Linezolid is a synthetic antibiotic used for the treatment of serious infections.

Delamanid is a new antituberculosis drug that inhibits mycolic acid synthesis and has shown potent in vitro and in vivo activity against drug-resistant strains of Mycobacterium tuberculosis.

Sitafloxacin is a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections. Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci.

Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.

Aztreonam is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum.

Sodium Tauroursodeoxycholate (TUDC) is a water soluble bile salt, used for the treatment of gallstones and liver cirrhosis.

SQ109 is an orally active, small molecule antibiotic for treatment of pulmonary T(tuberculosis).

Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2'-oxidase) inhibitor.

AN-2690, an antifungal agent with activity against Trichophyton species, in a topical solution formulation, for the potential treatment of onychomycosis.

Cloxacillin is a semisynthetic antibiotic in the same class as penicillin. Cloxacillin is used against staphylococci that produce beta-lactamase, due to its large R chain, which does not allow the beta-lactamases to bind.

Fusidate Sodium is a sodium salt form of fusidic acid, a bacteriostatic antibiotic derived from the fungus Fusidium coccineum and used as a topical medication to treat skin infections.

Cefoxitin Sodium is a semisynthetic cephamycin antibiotic resistant to beta-lactamase. It is derived from Cephamycin C and is highly resistance to β-lactamase inactivation.

Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.

Tobramycin Sulfate is a broad-spectrum antibiotic. It is effective against gram-negative bacteria, and especially potent against the Pseudomonas species.

Ampicillin Trihydrate is a beta-lactam antibiotic, which inhibits bacterial cell-wall synthesis (peptidoglycan cross-linking) by inactivating transpeptidases on the inner surface of the bacterial cell membrane.

Cefazolin Sodium is a semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.

Clindamycin inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections.

DDX3-IN-1 (Compound 16f) is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50s of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity.

Tigecycline mesylate is a broad-spectrum glycylcycline antibiotic that targets bacterial protein synthesis. It exhibits significant inhibitory activity against various Gram-positive and Gram-negative bacteria, with a mean inhibitory concentration (MIC) for E. coli (MG1655 strain) of approximately 125 ng/mL. For Acinetobacter baumannii, the MIC50 and MIC90 values are 1 mg/L and 2 mg/L, respectively, making it valuable for research focused on antibiotic resistance and infection control.

(Rac)-Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting HIV-1. It demonstrates significant antiviral activity with a Ki of 2.93 nM for the inhibition of the wild-type HIV-1 reverse transcriptase and an IC95 of 1.5 nM against HIV-1 replication in cultured cells. This compound is suitable for research applications focusing on HIV-1 therapy and the development of antiretroviral drugs.

nTZDpa is a partial agonist of PPARG and functions as an antibiotic. It exhibits significant antibacterial activity, particularly against both growing and persistent strains of Staphylococcus aureus, through the mechanism of lipid bilayer disruption. This compound is valuable for research applications focused on antibiotic resistance and the exploration of novel therapeutic strategies against bacterial infections.

Quindoxin is an antibacterial agent that acts by disrupting bacterial cell function. It demonstrates significant growth-promoting activity, particularly in livestock, and has been shown to exhibit dose-dependent mutagenicity against Salmonella typhimurium strains TA98 and TA100. Additionally, Quindoxin is associated with potential DNA damage, highlighting its relevance in studies related to genotoxicity and carcinogenicity.

GKL003 is a bacterial transcription inhibitor that targets the interaction interface of RNA polymerase (RNAP) and the sigma factor, with a Ki value of 5.79 nM. By specifically binding to the RNAP β' clamp helix region at the σA factor binding site, GKL003 disrupts the formation of the RNAP holoenzyme and inhibits bacterial transcription initiation complexes. This compound effectively inhibits the growth of both Gram-positive and Gram-negative bacterial strains, including those that are drug-resistant, making it a valuable tool for research applications in microbiology and antibiotic resistance studies.

(-)-(E)-Guggulsterone is a natural stereoisomer of Guggulsterone that functions as a Farnesoid X Receptor (FXR) antagonist with an IC50 of 24.06 μM. This compound exhibits significant hypolipidemic effects and demonstrates the ability to suppress dengue virus (DENV) replication by enhancing antiviral interferon responses through the activation of Nrf2 and upregulation of HO-1 expression. Additionally, (-)-(E)-Guggulsterone displays antibacterial properties against various strains, including Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa, as well as offering cardiac protective and antioxidant benefits in rat models.