Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics, with activity similar to oxolinic acid and nalidixic acid.
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase[1][2][3].
Herbicidin A is an adenosine-derived nucleoside antibiotic, but also is a herbicide against dicotyledonous plants. Herbicidin A can be isolated from Streptomyces scopuliridis M40[1][2].
Ferroquine is an ingenious antimalarial agent.
BMAP-18 is a biological active peptide. (BMAP-18 is a truncated form of the antimicrobial peptide BMAP-27. Bovine myeloid antimicrobial peptide-27 (BMAP-27) belongs to the Cathelicidin family of peptides which displays rapid bactericidal activity against Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. BMAP-27 is cytotoxic to human erythrocytes and neutrophils, although at higher than microbicidal concentrations. BMAP-18 displays much higher cell selectivity as compared to parental BMAP-27 because of its decreased hemolytic activity and retained antimicrobial activity.)
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities[1].
Aurodox is an antibiotic obtained from a streptomyces variant, Aurodox can against a number of gram-positive bacteria. Aurodox shows a very low toxicity in mice and promoted poultry growth[1].
Enoxacin-d8 (AT 2266-d8) is the deuterium labeled Enoxacin. Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing[1][2][3][4].
EcAMP3 is a hairpin-like peptide. EcAMP3 has antifungal and antibacterial activity. EcAMPs precursor family contains seven identical cysteine motifs: C1XXXC2(11–13)C3XXXC4[1].
Pinellic acid is a natural product that could be isolated from a medicinal plant Pinelliae tuber. Pinellic acid is an effective oral adjuvant for nasal influenza vaccine[1].
Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity[1][2].
SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomerof the octahydroisochromene scaffold, directs the P1 site imidazole[1].
Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species[1].
Ribostamycin (Vistamycin) is a broad-spectrum aminoglycoside antibiotic. Ribostamycin is effective against Gram-Negative and Gram-Positive bacterial infection. Ribostamycin also inhibits the chaperone activity of PDI[1][2].
Magnoflorine chloride (Magnoflorine chloride), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm[1]. Magnoflorine chloride has anti-fungal, anti-antidiabetic and anti-oxidative activity[2].
CpG ODN 10101, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 has antiviral and immunomodulatory properties that can influence chronic infection with HCV[1][2].
NSC-60339, an efflux pump inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent[1][2].
ZINC475239213 is an inhibitor of the SARS-CoV-2 Nsp14 N7-Methyltransferase (IC50: 20 μM)[1].
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1, demonstrates significantly acitive MIC50 and MIC90 values of 0.004 and 0.031 ug/ml (16 strains of C. auris); inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50 of 0.3 to 0.6 uM but has no inhibitory activity against human Pig-Wp; shows significant efficacy in murine model of disseminated C. auris infection, and log reduction in CFU counts in kidney, lung, and brain tissue. Fungal Infection Phase 1 Clinical
Ascr#18, an ascaroside, is a hormone of nematodes. Ascr#18 is expressed during nematode development. Ascr#18 increases resistance in Arabidopsis, tomato, potato and barley to viral, bacterial, oomycete, fungal and nematode infections[1].
Valacyclovir hydrochloride is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. Target: HSVValacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. VACV uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 +/- 0.06 mM and 23.34 +/- 0.36 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro . For treatment of a first episode of genital herpes, a large comparative trial has shown that valacyclovir (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day. The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1,000 mg of valacyclovir three times a day. EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b.i.d., 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA.
4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC50 of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA)[1].
Erythromycin gluceptate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin gluceptate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin gluceptate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Isopsoralenoside is a benzofuran glycoside from Psoralea corylifolia. Isopsoralenoside can be quickly metabolized to Psoralen (HY-N0053) in digestive tract contents. Isopsoralenoside show estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity[1].
Cefoselis is a widely used beta-lactam antibiotic.Target: AntibacterialCefoselis, a new parenteral cephalosporin, was active against clinical isolates of both gram-positive and gram-negative aerobic bacteria. The activity of Cefoselis was similar to that of cefpirome and cefepime and generally superior to that of ceftazidime. Cefoselis showed potent antibacterial activity against Hemophilus influenzae and Moraxella catarrhalis.Cefoselis was highly active against MSSA and MSCNS. Cefoselis was poor in the activity against MRSA,MRCNS,PRSP and Enterococcus faecalis,and no activity for Enterococcus faecium.
TH-Z93, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 90 nM)[1].
Pardaxin P5 is an antimicrobial peptide that inhibits Escherichia coli with a MIC value of 13 μM[1].
Aplaviroc, a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM)[1].