Isepamicin sulfate (Sch 21420 sulfate) is a broad spectrum aminoglycoside antibiotic. Isepamicin sulfate exhibits considerable antimicrobial activity against Gram-negative non-fermenters in a region with high antimicrobial resistance[1][2].
(9Z)-9,17-Octadecadiene-12,14-diyne-1,11,16-triol is a nature product that could be isolated from the ethyl acetate extract of Cassonia barteri (Araliaceae) leaves. (9Z)-9,17-Octadecadiene-12,14-diyne-1,11,16-triol has antibacterial activity against Bacillus subtilis and Pseudomonas fluorescens, antifungal activity against Cladosporium cucumerinum, moiluscicidal activity against Biomphalaria glabrata[1].
Antitubercular agent-24 (Compound 1) is an anti-tubercular agent with an extracellular IC50 of 0.83 μM and an intracellular IC50 of 0.17 μM against M. tuberculosis H37Rv[1].
Piromidic acid is a quinolone antibiotic.
Cefetamet is a potent antibiotic to treat respiratory and urinary tract infections.
Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)[1]
Ethyl acetoacetate-13C4 is the 13C labeled Ethyl acetoacetate[1]. Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[2][3][4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[5].
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS[1].
Pendulone is a isoflavanquinone with good antiplasmodial activity with an IC50 of 7.0 µM. Pendulone also has antileishmanial, antibacterial and anticancer activity[1][2].
Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
XT-4 is an antimicrobial peptide derived from skin secretions of Xenopus tropicalis. XT-4 has strong activity against E.coli, the vaule of MIC is 18 μM[1].
Penicillin G benzathine (Benzathine benzylpenicillin) is an antibiotic against many bacterial infections[1].
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
SBP1 peptide is a chemically synthesized 23-mer peptide fragment of the ACE2 PD α1 helix. SBP1 peptide associates with micromolar affinity to insect-derived SARS-CoV-2-RBD protein [1].
NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.
C-215 is a novel inhibitor of mycobacterial membrane protein large 3 (MmpL3) with MIC90 of 16 uM against M. tuberculosis.
GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: Target: Anti-parasitic agentGNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
Acetyl-Adhesin (1025-1044) amide is a 20-peptide fragment of Streptococcus pyogenes cell surface adhesin that acts as an antimicrobial peptide to specifically inhibit the binding of adhesin to salivary receptors and prevent recolonization of Streptococcus pyogenes[1].
Tirandamycin A, an antibiotic, is a bacterial RNA polymerase inhibitor. Tirandamycin A has antiamoebic and antibacterial properties[1][2].
Antibacterial agent 123 (compound 111) is a potent membrane-disrupting agent to combat antibiotic-resistant Gram-positive bacteria[1].
Isobellidifolin, a xanthone, is a free radical scavenger and antioxidant compound. Isobellidifolin has potent antifungal effect[1].
Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
Biapenem is a parenteral carbapenem antibacterial agent with a broad spectrum.Target: AntibacterialBiapenem is a carbapenem antibiotic of in vitro antibacterial activity encompassing many Gramnegative and Gram-positive aerobic and anaerobic bacteria, including species producing β-lactamases. Biapenem is more stable than imipenem, mero-penem and panipenem to hydrolysis by human renal dihydropeptidase-I (DHP-I), and therefore does not require the coadministration of a DHP-I inhibitor. In randomised, nonblind or double-blind clinical trials, biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/ cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections.
4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity.
Anti-infective agent 2 (compound 3k) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL[1].
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis[1].
Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Cecropin A (1-7)-Melittin A (2-9) is an antimicrobial peptide with antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative aerobic bacteria, as well as antimalarial activity, without the adverse hemolytic properties of bee venom peptides[1].
Valacyclovir hydrochloride hydrate is a potent antiviral agent. Valacyclovir hydrochloride hydrate can be used in the management of herpes simplex, herpes zoster and herpes B. Valacyclovir hydrochloride hydrate can be formulate ocular inserts for the treatment of ocular herpes. Valacyclovir hydrochloride hydrate is a prodrug and can be rapidly converted into acyclovir in vivo[1][2].
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease[2].