GA-O-02, a 18β-Glycyrrhetinic acid derivative, is a potent antimicrobial and anti-inflammatory agent. GA-O-02 exerts anti-inflammation through the inhibition of NO, pro-inflammatory cytokines and chemokines. GA-O-02 displays a high antimicrobial activity against Gram-positive bacteria.

G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter. Transmembrane ATP-binding cassette (ABC) transporters are crucial cellular machines that move molecules small and large across membranes. G092 has the potential for the research of antimicrobial drugs.

RN-18 is a selective inhibitor of virion infectivity factor (Vif) APOBEC interactions and HIV-1 replication.

Sutezolid (PNU-100480) is an oxazolidinone antimicrobial being developed for the treatment of tuberculosis.

T-00127-HEV1 is a novel potent phosphoinositide kinases (PIK) inhibitor,T-00127-HEV1 inhibited PI4KB activity with a higher specificity for than other PI kinases.

Tubercidin, an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.

YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.

Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor.

UAMC-03011 is a potent anti-trypanosomal compound (IC50=0.63 uM, T. brucei).UAMC-03011 displays selectivity for Trypanosoma brucei over a panel including Trypanosoma cruzi, L.eishmania infantum, and Plasmodium falciparum (IC50>64 uM).

SRI-41897 is a specific small molecule inhibitor of HIV-1 N-terminal region of NL4-3 Vpu (HIV-1 NL4-3 Vpu) with EC50 of 4.4 uM in the GaLV inhibition assays.SRI-41897 blocks Vpu-mediated modulation of CD4, BST-2/Tetherin and antibody dependent cell-mediated toxicity (ADCC).SRI-41897 rescues CD4 surface expression by 47% on infected TZM-GFP cells, also rescues the expression of CD4 and Tetherin in human peripheral blood mononuclear cells (PBMCs).

SBI-0797750 (SBI 0797750) is a potent, fully selective PfGluPho inhibitor with robust nanomolar activity against recombinant PfGluPho, PvG6PD, and P. falciparum blood-stage parasites.SBI-0797750 disturbs the cytosolic glutathione-dependent redox potential, as well as the cytosolic and mitochondrial H2O2 homeostasis of P. falciparum blood stages, at low nanomolar concentrations.SBI-0797750 does not harm red blood cell (RBC) integrity and phagocytosis and thus does not promote anemia.

SBI-0637142 is a potent Smac mimetic that preferentially targets BIRC2, latency-reversing agent (LRA), specifically and potently promote HIV-1 latency reversal activity.SBI-0637142 modestly induced HIV-1 latency ex vivo in CD4+ T cells from ART-suppressed aviremic HIV-infected patients as a single agent, showed robust activity when administered in combination with the HDACi panobinostat.SBI-0637142's latency reversal activity is dependent on the NIK-dependent NF-κB signaling.

S2C3 is a small molecule HIV-1 fusion inhibitor, targets the membrane proximal external region (MPER) of HIV-1 envelope spike.S2C3 interacted with gp41-inter with an affinity of 2.0 uM.S2C3 has been shown to effectively block binding to the intact HIV-1 Env expressed on the cell surface by soluble CD4 but not by CD4 binding the sitedirected NAb VRC01, or the prefusion conformation-specific NAb PG16.S2C3 targets a site in the HIV-1 Env distinct from sites targeted by small-molecule entry inhibitors that have been identified so far.S2C3 could stabilize HIV-1 Env in the prefusion conformation, making it potentially useful in a vaccine preparation to reduce the conformational flexibility of Env.

Rencofilstat (CRV431) is a non-immunosuppressive analogue of cyclosporine A and pan-cyclophilin inhibitor, potently inhibits cyclophilin isoforms A, B, D, and G with IC50 of 1-7 nM.Rencofilstat (CRV431) is more than 13 times more potent than the parent compound, cyclosporine A (CsA).Rencofilstat (CRV431) inhibits liver HBV DNA and HBsAg, reduces liver HBV DNA levels and moderately decreased serum HBsAg levels in HBV transgenic mouse model.Rencofilstat (CRV431) shows potential as a drug candidate for chronic liver diseases.

QZN 34 is a small molecule pseudomonas aeruginosa PQS quorum-sensing system (PqsR) inhibitor with IC50 of 15 uM, kills planktonic Gram-positives (S. aureus, MIC 6.25 uM) but not Gram-negatives.QZN 34 prevented S. aureus biofilm formation, severely damaged established S. aureus biofilms, and perturbed P. aeruginosa biofilm development.QZN 34 killed planktonic Gram-positive pathogens including S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, and Clostridioides difficile but not Gram-negative bacteria such as P. aeruginosa and Escherichia. coli.QZN 34 eradicated the mixed-species biofilm against mixed S. aureus and P. aeruginosa biofilms when combined with aminoglycoside.

Quabodepistat (OPC-167832) is a highly potent antituberculosis agent with MIC of 0.00024 to 0.002 ug/mL against Mycobacterium tuberculosis, targets DprE1 (IC50=258 nM, recombinant DprE1), an essential enzyme for cell wall biosynthesis.OPC-167832 showed MIC90 of 0.0048 and 0.0027 ug/mL against intracellular M. tuberculosis strains H37Rv and Kurono were 0.0048 and 0.0027, respectively.OPC-167832 showed potent bactericidal activities starting at a dose of 0.625 mg/kg of body weight in a mouse model of chronic TB.OPC-167832 exhibited significant combination effects in 2-drug combinations with delamanid, bedaquiline, or levofloxacin.

PTC-847 (PTC847) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.1 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-847 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-847 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-847 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-847 showed 93% inhibition aginst Ng RNR activity at 4 uM, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.

PTC-672 (PTC672) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.4 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-672 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-672 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-672 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-672 showed 78% inhibition at 2.5 μM aginst Ng RNR activity, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.PTC-672 (30 mg/kg) demosntrates in vivo efficacy in a mouse model of gonorrhea.

PDE-I2 is a potent and selective inhibitor of malaria proliferation with Pf IC50 of 18 nM.PDE-I2 is a precursor of the anticancer duocarmycin family that preserves the class's sequence-specific DNA binding but lacks its signature DNA alkylating cyclopropyl warhead.PDE-I2 retains comparable antimalarial potency to chloroquine.PDE-I2 is >1,000-fold less toxic to human cell lines than duocarmycin, with mitigated impacts on eukaryotic chromosome stability.PDE-I2 treatment induces severe defects in parasite nuclear segregation leading to impaired daughter cell formation during schizogony.

NPG9 (NSR inhibitor NPG9) is a small molecule inhibitor of streptococcus agalactiaenisin resistance protein (NSR) with 58% inhibition at 100 uM (specific growth inhibition assay).

NEU-4438 (NEU4438) is a potent inhibitor of P. falciparum with EC50 of 13 nM (T. brucei), demonstrates improved aqueous solubility (880 uM) compared to NEU-1953; reduced parasitemia 109 fold in trypanosome-infected mice.

NBD-14273 is a CD4-mimetic, small-molecule HIV-1 entry inhibitor with IC50 of 0.13 uM.NBD-14273 showed both improved antiviral activity and selectivity index (SI) against HIV-1HXB2 compared to NBD-14136.NBD-14273 displayed potenct against a large panel of 50 HIV-1 Env-pseudotyped viruses representing clinical isolates of diverse subtypes.

N205 is a novel anti-malaria compound with in vitro IC50 of 1.3 nM against Plasmodium falciparum (3D7); demonstrates excellent rodent pharmacokinetic and in vivo antimalarial efficacy studies in the mouse Plasmodium berghei and Plasmodium falciparum Pf3D70087/N9 severe combined immunodeficiency (SCID) mouse models.

Mtb CoaBC inhibitor 1f is a direct small molecule inhibitor of Mtb 4'-phosphopantothenoyl-l-cysteine synthetase (PPCS, CoaB) domain of the bifunctional Mtb CoaBC (IC50=15.6 uM).Mtb CoaBC inhibitor 1f inhibit CoaBC uncompetitively with respect to 4'-phosphopantothenate, the substrate for the CoaB-catalyzed reaction.Mtb CoaBC inhibitor 1f inhibits Mtb growth in whole-cell activity against Mtb H37Rv (MIC=25.9 uM).

MMV688844 (MMV844) is a piperidine-4-carboxamide with bactericidal properties against M. abscessus, targets mycobacterial DNA gyrase.

MMV688533 is a potent antimalarial compound that displays fast parasite clearance in vitro and is not cross-resistant with known antimalarials, MMV688533 is highly potent against multiple P. falciparum strains with IC50 values in low nanomolar range (P. falciparum 3D7, IC50=1.9 nM).MMV688533 also showed excellent ex vivo activity against asexual blood-stage parasites from fresh P. falciparum isolates (median IC50=1.3 nM, range=0.02 to 6.3 nM).MMV688533 remained potent in ex vivo assays against both P. falciparum and P. vivax with IC50 of 18.9 and 12.0 nM respectively.MMV688533 displayed fast and potent in vivo efficacy and favorable in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetic properties.MMV688533 antiplasmodial activity is unrelated to existing antimalarials and selects for low-grade resistance mediated in part by mutations in PfACG1 and PfEHD.

MMV675968 is a potent, small molecule inhibitor of Toxoplasma gondii (T. gondii) with IC50 of 0.02 uM, via the pathogen box.MMV675968 has been shown to be efficient against the planktonic form of C. albicans.MMV675968 showed an antiplasmodial activity against P. falciparum.MMV675968inhibited the growth of all four A. baumannii test strains with IC50 of 0.6-2.7 uM, IC90 of 0.7-3.9 uM, and MIC of 1.6-10 uM.

MMV084978 (MMV 084978) is an antiplasmodial drug-like compound tageting Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS), directly and selectively inhibit PfAcAS activity in vitro with IC50 of 370 nM.MMV084978 directly inhibits PfAcAS by preventing CoA and acetate binding.MMV084978 demonstrated in vitro efficacy (P. falciparum Dd2 EC50=150 nM) with increased liver-stage potency (Pbluc EC50= 520 nM).MMV084978 directly and selectively inhibit PfAcAS activity in vitro.

MMV019721 (MMV019721) is an antiplasmodial drug-like compound tageting Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS), directly and selectively inhibit PfAcAS activity in vitro with IC50 of 73 nM.MMV019721 directly inhibits PfAcAS by preventing CoA binding.MMV019721 has activity against blood-stage parasites in vitro (P. falciparum 3D7, EC50=460 nM) and against liver-stage P. berghei parasites (Pbluc EC50=2,000 nM).MMV019721 directly and selectively inhibits PfAcAS activity in vitro.

MGB-BP-3 is a potent bactericidal antibiotic with a completely novel mode of action, selectively binds to the minor grove of microbial DNA, has the potential for Clostridioides difficile infection (CDI).