Acetylazide is a synthetic broad-spectrum bacteriostatic antibiotic.
Saccharothrixin K, a glycosylated saccharothrixin, shows moderate inhibition against Helicobacter pylori G27, H. pylori 159, and Staphylococcus aureus ATCC25923 with MIC values of 16 μg/mL[1].
S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively[1].
PPm, a derivative of penthiopyrad and hapten, is a representative member of the succinate dehydrogenase inhibitors group of fungicides[1].
BO3482 has Antimicrobial activity and can inhibit the growth of methicillin-resistant Staphylococci (MRS) with an MIC90 of 6.25 mg/mL.
Vidarabine monohydrate is an adenine arabinoside. Vidarabine monohydrate an antiviral drug which is active against herpes simplex viruses (HSV) and varicella zoster viruses[1].
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%)[1].
Metallo-beta-lactamase ligand 1 is a class B β-lactamase inhibitor with antibacterial activity extracted from patent WO2019221122A1, compound A[1].
Fmoc-Pro-OH-13C5,15N is a 15N-labeled and 13C-labled Pyrimethanil. Pyrimethanil is an anilinopyrimidine and broad-spectrum contact fungicide for the control of Botrytis spp. on a wide variety of crops[1]. Pyrimethanil inhibits the biosynthesis of methioni
Jaceidin triacetate(compound 54) is a natural compound isolated formmarulabark.Jaceidin triacetatecan inhibitSARS-CoV-2 Mpro, with theIC50of 11.9μM.Jaceidin triacetateinhibits the replication of Sars-Cov-2 Viral in Vero-E6 cells[1][2].
Oritavancin diphosphate is a novel semisynthetic glycopeptide antibiotic being developed for the treatment of serious Gram-positive bacterial infections. Target: AntibacterialOritavancin is a lipoglycopeptide.Oritavancin has completed clinical trials and submitted a new drug application for treatment of skin infections.
Sulfachloropyridazine-13C6 is the 13C6 labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
3′-Omethyl-5′-hydroxydiplacone (compound 2), an C-6-geranylflavonoid, can be isolated from the ethanol extract of Paulownia tomentosa fruits. 3′-Omethyl-5′-hydroxydiplacone has antibacterial activity against Gram-positive bacteria[1].
Furagin, nitrofurantoin analog, is an anti-bacterial agent. Furagin is 2-substituted 5-nitrofuran, chemically and structurally similar to well-known antibacterial compound nitrofurantoin.IC50 Value: Target: Antibacterialin vitro: The furagin concentrations in serum remain several hours above the MIC concentrations of many pathogenic bacteria. Despite the high concentrations in serum, the urine levels of furagin were generally lower than those of nitrofurantoin. The 24 hr recoveries in urine were 8--13% for furagin and about 36% for nitrofurantoin [1].in vivo: A time-independent increase in SCE frequency was found in lymphocytes of children treated with furagin. Total CA frequency did not differ significantly between groups of children with various duration of furagin treatment [2]. Women were randomised into two groups receiving either ciprofloxacin 250mg twice a day for 3 days (n=13) or furagin 100mg three times a day for 7 days (n=14). Median lengths of follow-up were 4 days and 5 days in the ciprofloxacin and furagin groups, respectively [3].
VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.IC50 Value: Target: HCVVCH-916 is a novel allosteric inhibitor of HCV NS5B polymerase. The RNA-dependent RNA polymerase (NS5B) of HCV is one of the attractive validated targets for development of new drugs to block HCV infection. VCH-916 is currently being evaluated for safety/tolerability, pharmacokinetics and anti-viral efficacy in chronically infected HCV patient.
pUL89 Endonuclease-IN-2 (Compound 15k) is a potent inhibitor of human cytomegalovirus (HCMV) pUL89 endonuclease with the IC50 of 3.0 μM. Antiviral activities[1].
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively[1].
BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].
Valnemulin hydrochloride is a pleuromutilin antibiotic which inhibits protein synthesis in bacteria by binding the peptidyl transferase enzyme in the 50s ribosomal subunit.
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra L, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes[1]. Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE[2].
Zabofloxacin (DW-224a Free base) is a novel fluoronaphthyridone quinolone with a 7-pyrrolidone substituent that is considered a potent antibacterial candidate for clinical trials.Zabofloxacin (DW-224a Free base) has excellent activity against gram-positive pathogens including Steptococcus aureus , Streptococcus pyogenes and S.pneumonia.Zabofloxacin (DW-224a Free base) is considered as an alternative candidate for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP)[1].
Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC50 range of 0.1-0.5 μM[1]. Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against S. aureus 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively[2]. Micrococcin P1 is also a potent inhibitor of the malaria parasite Plasmodium falciparum[3].
Bifendate (DDB) is a synthetic intermediate of Schisandrin C with anti-HBV efficacy in research of chronic hepatitis B[1].
OX11 is a selective inhibitor of S. pneumoniae, P. aeruginosa, and E. coli bacterial strains[1].
Alisol F 24-acetate is a triterpene compound that can be isolated from the rhizomes of Alisma orientalis. Alisol F 24-acetate inhibits the secretion of HBV surface antigen HBsAg and HBeAg with IC50 values of 7.7 µM and 5.1 µM. Alisol F 24-acetate has proapoptotic activity and can be used for cancer research[1][2].
Penetratin-Arg is an antimicrobial and is used for drug delivery vehicle[1].
ThrRS-IN-1 (Compound 30d) is a threonyl-tRNA synthetase (ThrRS) inhibitor with an IC50 of 1.4 µM and a Kd of 1.36 µM against Salmonella enterica ThrRS (SeThrRS). ThrRS-IN-1 simultaneously targets the tRNAThr and L-threonine binding pockets of ThrRS. ThrRS-IN-1 shows potent antibacterial activities[1].
A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively; inhibits cancer cell growth, modulates P-glycoprotein, and synergizes with doxorubicin in MCF7 and MCF ADR cells with IC50 in nanomolar range; increase G0-G1-phase fraction and caspase-independent apoptosis, also reduces P-gp expression.
Nelfinavir(AG-1341) 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. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
NOSO-502 (NOSO502) is a novel inhibitor of bacterial translation, has MIC values of 0.5-4 ug/ml against standard Enterobacteriaceae strains and carbapenem-resistant Enterobacteriaceae (CRE) isolates that produce KPC, AmpC, or OXA enzymes and metallo-β-lactamases; interacts strongly with a specific site on the 30S subunit of bacterial ribosomes but has no significant activity against any of the 55 cell surface receptors, transporters, or ion channels; NOSO-502 is active against a panel of Gram-positive and Gram-negative bacteria, including carbapenem-resistant and polymyxin-resistant strains, and exhibits promising in vivo activity in various murine infection models, a favorable in vitro safety profile, and a low potential for resistance development.