Microbiology/Virology

12-Bromododecanoic acid, a halogenated derivative of lauric acid, serves in the synthesis of clickable myristic acid derivatives and functions as a model fatty acid ligand for elucidating the X-ray crystal structure of bovine β-lactoglobulin-ligand complexes. This compound, at a concentration of 10 µg/ml, has been shown to diminish virion DNA in the culture supernatant of primary hepatocytes from a duckling model of hepatitis B virus (HBV) infection and exhibits inhibitory activity against HIV replication in CEM-SS T cells with an EC50 value of 38 µM.

FIKK9.1-IN-1 (Compound 1), an antimalarial agent (IC50: 2.68 μg/mL), serves as a FIKK9.1 inhibitor by interacting with the ATP-binding residues within FIKK9.1,

SARS-CoV-2 3CLpro-IN-2 is a potent inhibitor of the 3CL protease pair and has shown research potential for SARS-CoV-2 disease.

Yimitasvir diphosphate, also known as Emitasvir, is an orally-administered inhibitor of the hepatitis C virus (HCV) nonstructural protein 5A (NS5A).

L 694746 is an inhibitor of HIV-1 protease.

Zika virus-IN-1 is an inhibitor of Zika virus (EC50: 1.56 μM).

DB-766: Chagas' treatment candidate with potent, selective trypanocidal action. IC50: 60 nM (bloodstream), 25 nM (intracellular). Promising new lead.

BILR-355 is a reverse transcriptase inhibitor.

JTK-853: novel non-nucleoside HCV polymerase inhibitor with strong antiviral activity (EC50: 0.38 μM genotype 1a, 0.035 μM 1b).

Valtorcitabine dihydrochloride, a DNA polymerase inhibitor, is used potentially for the treatment of HBV infection.

NCI-B16 is a small-molecule RNA binder that inhibits HCV (hepatitis C virus) replication [1].

FX-06 (Fibrin-derived peptide Bβ15-42) is a peptide derived from the fibrin Bbeta chain.

Frenolicin is a selective inhibitor of Prx1 and Grx3 through covalent modification of active-site cysteines.

Antifungal agent 24 (Compound 6) is an antifungal agent that inhibits Candida albicans (MIC: 0.03 μg/ml).

HBV-IN-17 (compound 8) is a potent regulator of HBV capsid assembly (EC50: 511 nM).

Brevicompanine B: fungal metabolite, regulates plant growth/circadian rhythm, inhibits Arabidopsis roots, affects gene transcription, anti-P. falciparum.

HOE961, a diacetate ester prodrug of S2242, is an oral anti-orthopoxvirus agent effective against cowpox.

OM173-αA is a quinone bacterial metabolite that inhibits the growth of the bacteria M.

Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when

Photosensitizer-1 shows promise in treating infections, effective against S. aureus in mouse wounds.

SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM.

Mansonone F is a topoisomerase II inhibitor with cytotoxic and topo inhibitory potencies.

Daldinone A (Compound 4), isolated from Nigrospora oryzae, exhibits antibacterial properties, specifically demonstrating antimicrobial potential against P. aeruginosa [1].

Tuberculosis Inhibitor 12, an oxadiazole derivative, effectively inhibits Mycobacterium tuberculosis, demonstrating inhibition rates of 82% and 78% at a

FWM-4 is a potent inhibitor of SARS-COV-2 NSP13 decapping enzyme.

Antifungal agent 48 (Example 308), active against Cryptococcus neoformans, exhibits a minimum inhibitory concentration (MIC) value of 11 μM [1].

Balapiravir HCl, an NS5B inhibitor, is used potentially for the treatment of HCV infection.

HIV-1 inhibitor-3 is an HIV infection inhibitor.

Phylloflavan, an antileishmanial compound, exhibits an intracellular half maximal effective concentration (EC50) of 3.2 nM in RAW 264.7 cells and inhibits the

Antibacterial Agent 135 (example 7) effectively inhibits various bacteria, including P.

Valnemulin, a broad-spectrum pleuromutilin antibiotic, targets peptidyl transferase within the 50S ribosomal subunit, effectively used in veterinary medicine to address swine diseases such as B. hyodysenteriae and M. hyopneumoniae.

Ianthelliformisamine B TFA, an antibiotic enhancer, is used to against resistant Gram-negative bacteria.

Zndm19 is an inhibitor of New Delhi Metallo-β-lactamase-1 (NDM-1), utilized in researching drug-resistant bacterial infections [1].

Fosalvudine tidoxil, a nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

17(R)-Resolvin D4 (17(R)-RvD4) is an epimer of RvD4, generated through the aspirin-induced modification process.

Flurofamide is an effective bacterial urease inhibitor and has potential in the treatment of infected urinary calculi.

1R-cis-Permethrin, an insecticide and neurotoxin, acts on neuron membranes by extending the activation of sodium channels [1].

GSK-3532795: a broader-spectrum HIV-1 maturation inhibitor than bevirimat, effective in vitro and clinically.

Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]

Avarofloxacin (JNJ-Q2) is a fluoroquinolone for treating bacterial skin infections and pneumonia.

MAC13772 is a potent inhibitor of the enzyme BioA with an IC50 of 250 nM thereby inhibiting biotin biosynthesis. MAC13772 exhibits antibacterial activity.

Byssochlamic acid, a mycotoxin identified in the agricultural fungal pathogen B. fulva, exhibits lethality in mice with an LD50 of 94 mg/kg.

WRN Inhibitor 5 (Example 157), a cyclic vinyl sulfone-based compound, serves as an inhibitor of Werner Syndrome ATP-dependent helicase enzyme (WRN).

Ulonivirine is an orally active non-nucleoside reverse transcriptase inhibitor that exhibits high antiviral activity and can be used to study HIV-1 infection.

Ipflufenoquin, an insecticide, effectively combats primary apple scab infections. Its application is optimal between the stages of half an inch of green and fruit set [1].

12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX.

HCV-IN-44 (compound 28) is an inhibitor of the HCV NS5B protein, efficacious in suppressing HCV virus replication and useful for researching HCV infection [1].

Antituberculosis agent-6: potent against M. tuberculosis (MIC 3.49 μM), antifungal (MIC 62.5 μM), high GI absorption.

Cap-dependent endonuclease-IN-13 is a potent inhibitor of cap-dependent endonuclease (CEN) and shows research potential against influenza virus infection (

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

(+)-Thienamycin, a powerful broad-spectrum antibacterial and β-lactamase inhibitor, is isolated from Streptomyces cattleya [1].

A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.

5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor and other folate related enzymes inhibitor.

ZINC475239213 acts as an inhibitor targeting the SARS-CoV-2 Nsp14 N7-Methyltransferase with an IC50 value of 20 μM [1].

Cyclic HPMPC: Potent antiviral, raises O2 in mice with lethal vaccinia, lowers guinea pig CMV replication.

Antifungal agent 49 (Example 112) exhibits activity against Cryptococcus neoformans, demonstrating a minimum inhibitory concentration (MIC) of 49 μM [1].

Cefteram (T-2525), an orally active ester of the cephalosporin class, is the free acid form of Cefteram pivoxil.

Zevotrelvir (Compound 52) serves as an inhibitor of coronavirus, demonstrating IC50 values below 0.1 μM for 229E hCoV protease and below 0.1 mM for SARS-CoV-3C-

HEC72702: New HBV capsid inhibitor, from GLS4. No CYP1A2, CYP3A4, CYP2B6 induction at 10μM.

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

HBV-IN-30, a flavone derivative, inhibits cccDNA in HBV research.

Ibuzatrelvir (PF-07817883) is an antiviral compound designed to inhibit the SARS-CoV-2 3CL protease, and is utilized in the treatment of COVID-19 [1].

Mtb-IN-4 (compound 17h) is a non-toxic isoxazole that exhibits anti-Mycobacterium tuberculosis (Mtb) activity, with an IC50 value of 0.70 μM.

Antifungal agent 66 (compound 10) exhibits broad-spectrum antifungal activity against seven phytopathogenic fungal mycelia and significant inhibitory effects on

Sulfisoxazole acetyl (Gantrisin) is an agent with antibacterial activity.

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

GNE-371 is a probe for human transcription initiation factor TFIID subunit 1 and transcription initiation factor TFIID subunit 1-like second bromodomain.

Murabutide, a safe synthetic immunomodulator, diminishes the expression of CD4 and CCR5 receptors and promotes the secretion of high levels of beta-chemokines,

β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.

GSK3839919A is a potent allosteric inhibitor of HIV-1 integrase [1].

DMP 323 is a potent inhibitor of HIV-1 protease.

DQn-1, a potent antifolate, demonstrates efficacy against Mycobacterium tuberculosis (Mtb) with an MIC 90 of 0.03 µM.

Disoxaril (BRN 3626820, WIN 51711), an anti-picornavirus, blocks enterovirus by targeting VP1; boosts poliovirus inhibition with Ambioxime, Bioxazole.

RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is a respiratory syncytial virus (RSV) replication inhibitor.

Ravidasvir, also known as PPI-668 and ASC16, is a second-generation, orally active, potent and selective HCV NS5A protein inhibitor.

LtaS-IN-1 inhibits LTA synthesis in MDR E. faecium; alters cell walls; MIC: 0.5-64 μg/mL for 28 Enterococcus strains.

AZ-27 is a respiratory syncytial virus inhibitor which differentially inhibits different polymerase activities at the promoter.

Fervenulin, from Streptomyces sp. CMU-MH021, halts egg hatch (MIC: 30 μg/mL) and kills J2 larvae (MIC: 120 μg/mL) of M. incognita.

Compound 5k (Antiproliferative Agent-18) is an antiproliferative agent that exhibits moderate antibacterial and antifungal activities [1].

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7

NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.

Besifovir Dipivoxil maleate, an oral HBV prodrug (LB80380), suppresses HBV DNA in naive and lamivudine-resistant CHB cases.

4-Aminobenzylphosphonic acid, an inhibitor of alkaline phosphatase (Ki= 1.1 mM for the bovine intestine enzyme), is utilized in affinity chromatography for alkaline phosphatase purification and in the electrochemical modification of glassy carbon electrodes.

Zika virus-IN-2 (Compd 3) is a Zika virus inhibitor (EC 50= 7.4 μM).

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

Laninamivir Octanoate Monohydrate is a neuraminidase inhibitor.

hDHODH-IN-1 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an anti-inflammatory effect.

Limocrocin is an inhibitor of reverse transcriptase.

L 687908 is a potent inhibitor of hydroxyethylene-containing HIV protease.

MK-3281: Oral, potent HCV NS5B inhibitor with promising properties and efficacy in replication trials, suitable for clinical use.

APX001 is a prodrug of APX-001A. APX001 is the first-in-class inhibitor of the fungal protein Gwt1.