Antifection

Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

Carbendazim is a broad-spectrum benzimidazole fungicide which can be used to control a broad range of diseases on arable crops, fruits, vegetables, ornamentals and medicinal herbs.

BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.

Lanopepden (GSK 1322322) is a peptide deformylase inhibitor active against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively.

Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice.

VXc-486 is a gyrase B inhibitor, with bactericidal activity.

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

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

Omadacycline hydrochloride is novel, aminomethyl tetracycline antibiotic being developed for the treatment of community-acquired bacterial infections. The ED50 for Escherichia coli is 2.02 mg/kg.

Blasticidin S is a nucleoside antibiotic isolated from Streptomyces griseochromogenes. Blasticidin S is a potent inhibitor of protein synthesis in both prokaryotic and eukaryotic cells.

l-Atabrine dihydrochloride is a less active enantiomer of quinacrine which displays antiprion activity.

d-Atabrine dihydrochloride is an active enantiomer of quinacrine which displays antiprion activity.

Eprinomectin(MK-397) is an avermectin selected for development as a topical endectocide; has anthelmintic, insecticidal and miticidal activity.

Dianemycin (Nanchangmycin free acid), produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Dianemycin is a broad spectrum antiviral active against Zika virus.

Gatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

Gatifloxacin (mesylate) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials.

MAC13243, an antibacterial agent, is a likely inhibitor of the bacterial lipoprotein targeting chaperone, LolA.

Tilbroquinol is an antiprotozoal agent effective against amoebiasis. It has also been used against Vibrio cholerae.

PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.

Dimboa is an antifungal agent used in crops.

Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay.

Neuraminidase-IN-1 is a neuraminidase inhibitor, with an IC50 of 0.21 μM. Neuraminidase-IN-1 has excellent activity against H1N1 influenza virus.

Pyrimorph is a fungicide with high activity against the plant pathogen Phytophthora capsici.

Cenobamate (YKP-3089) is a novel antiepileptic drug candidate with broad-spectrum anticonvulsant activity.

GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains.

Lawsone methyl ether (2-Methoxy-1,4-naphthoquinone), isolated from Impatiens balsamina L. and Swertia calycina, exhibits potent antifungal and antibacterial activities.

(R)-Ofloxacin is a R-isomer of Ofloxacin.Ofloxacin is an antibiotic useful for the treatment of a number of bacterial infections.

Plitidepsin is a cyclic depsipeptide isolated from the marine tunicate Aplidium albicans. Plitidepsin displays a broad spectrum of antitumor activities, inducing apoptosis by triggering mitochondrial cytochrome c release, initiating the Fas/DC95, JNK pathway and activating caspase 3 activation. This agent also inhibits elongation factor 1-a, thereby interfering with protein synthesis, and induces G1 arrest and G2 blockade, thereby inhibiting tumor cell growth.

Ezeprogind, also known as AZP-2006, is an artificial zinc-finger protein used to inhibit DNA replication of human papillomavirus (HPV).

Riamilovir, also known as Triazavirin, is a nucleoside analogue of nucleic acid and an antiviral agent, works by inhibiting the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is shown active in inhibition of the tick-borne encephalitis virus reproduction (strain Sofiin) by accumulation in the SKEV cell culture.

Cyantraniliprole(HGW-86) is an insecticide of the ryanoid class; has activity against pests such as Diaphorina citri that have developed resistance to other classes insecticides.

Loflucarban is an antiinfective drug.

Cosan-528 is a fungicide.^[1] It is active against the fungus A. pullulans (MIC = 8 ppm). Cosan-528 completely inhibits the growth of A. pullulans, A. niger, and Penicillium on paint-coated white pine sapwood for at least six weeks.

TCMTB is an antimicrobial agent used as a substitute for chlorophenols in industrial applications. Biocide used in the leather, pulp and paper, and water-treatment industries.

MBX2329 is a specific inhibitor of HA-mediated viral entry that inhibits HPAI H5N1 virus strain and HA-mediated viral entry.

LolCDE-IN-1 is an inhibitor of the Lol proteins (LolCDE) complex, with antibacterial activity.

6-Diazo-5-oxo-L-nor-Leucine is a glutamine antagonist that shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 

Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).

Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM.

Lariatins is a novel anti-mycobacterial peptides with a lasso structure produced by Rhodococcus jostii K01-B0171.

SMAP-29, a promising antiinfective agent, is a broad spectrum antibacterial and antifungal α-helical cathelicidin-derived peptide. SMAP-29 acts by permeabilizing bacterial membranes and inducing remarkable changes in the surface morphology of susceptible microorganism.

Dermaseptin, a peptide isolated from frog skin, exhibits potent antimicrobial activity against, bacteria, fungi, and protozoa at micromolar concentration.

Safracin B, a tetrahydroisoquinoline (THIQ) alkaloid, is a naturally occurring antibiotic from Pseudomonas fluorescens. Safracin B exhibits broad spectrum antimicrobial and strong antitumor activities.

Isavuconazonium sulfate (BAL8557-002) is an orally active, broad-spectrum antifungal prodrug that is rapidly hydrolyzed in vivo to yield the active triazole compound **Isavuconazole**. It exhibits potent antifungal activity by inhibiting lanosterol 14α-demethylase, a key enzyme in the ergosterol biosynthesis pathway, thereby disrupting fungal cell membrane integrity. Isavuconazonium sulfate is effective against a wide range of pathogenic fungi, including *Aspergillus* and *Mucorales* species, and is used in the study and treatment of invasive aspergillosis, mucormycosis, blastomycosis, and *Acanthamoeba* keratitis. Its excellent oral bioavailability and favorable safety profile make it a valuable therapeutic and research tool in antifungal pharmacology.

Delmopinol is a surface-active cationic compound that functions as an anti-plaque and anti-gingivitis agent. It interacts with the acquired pellicle—a thin salivary film composed of proteins and glycoproteins that coats the teeth and gums—and forms a protective barrier over oral surfaces. This barrier inhibits microbial adhesion and biofilm formation, thereby preventing plaque accumulation and gingival inflammation. Although Delmopinol does not possess direct bactericidal activity, its ability to interfere with bacterial colonization makes it effective in maintaining oral hygiene. It has been approved by the U.S. FDA under the trade name **Decapinol** for the treatment of gingivitis and the prevention of periodontitis.

Cytochalasin D (also known as Zygosporin A) is a cell-permeable fungal metabolite and a potent inhibitor of actin polymerization. It binds to G-actin, thereby disrupting the G-actin–cofilin interaction and preventing cofilin association with F-actin. Through this mechanism, Cytochalasin D reduces both actin polymerization and depolymerization rates in living cells, leading to profound effects on cytoskeletal organization and cell morphology. In addition, Cytochalasin D suppresses exosome release, consequently decreasing survivin levels within the tumor microenvironment. It also promotes phosphorylation and cytoplasmic retention of YAP, implicating it in the regulation of mechanotransduction and tumor cell signaling.

Azaserine (CI-337) is a glutamine analog and competitive inhibitor of glutamine amidotransferase, an enzyme involved in nucleotide biosynthesis. It exhibits both antibiotic and antitumor properties by disrupting glutamine-dependent metabolic processes essential for cell proliferation. Azaserine demonstrates antibacterial activity and has shown antitumor effects in various cancer models. However, it has also been reported to possess tumorigenic potential under certain conditions, warranting cautious evaluation.

Dusquetide (SGX-942, SGX94) is a synthetic 5-amino acid peptide and innate defense regulator (IDR) with immunomodulatory, anti-inflammatory, anti-infective, and anti-mucositis properties. Upon intravenous administration, it binds to the ZZ domain of sequestosome-1 (p62), activating key signaling pathways such as MAPK p38 and C/EBP involved in innate immune regulation. Dusquetide is a promising agent for modulating immune responses in various inflammatory and infectious conditions.

ANS (8-Anilino-1-naphthalenesulfonic acid) is a competitive inhibitor of thyroxine binding globulin (TBG), exhibiting a Ki value of 2.09×10^6 M^-1. This compound is utilized in radioimmunoassays to enhance detection sensitivity by displacing bound triiodothyronine (T3) and facilitating its recognition by antibodies. Additionally, ANS serves as a fluorescent probe, selectively binding to hydrophobic regions of proteins, particularly membrane proteins, allowing for real-time monitoring of protein conformational dynamics through fluorescence changes. Its applications extend to biochemical research and the development of antibacterial materials.