Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity[1][2].
Doxycycline (hyclate) is a tetracycline antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization[1].
Ethionamide(2-ethylthioisonicotinamide) is an antibiotic used in the treatment of tuberculosis.Target: AntibacterialEthionamide is a second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. Ethionamide is a prodrug. It is activated by the enzyme EthA, a mono-oxygenase in Mycobacterium tuberculosis, and binds NAD+ to form an adduct which inhibits InhA in the same way as isoniazid. Expression of the ethA gene is controlled by EthR, a transcriptional repressor. It is understood that improving ethA expression will increase the efficacy of ethionamide and so EthR inhibitors are of great interest to co-drug developers. The action may be through disruption of mycolic acid [1, 2].
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1[1].
Asimicin (Bullatacin) is antitumor acetogenin that can be isolated from the bark and seeds of the pawpaw tree, Asimina trilobal Dunal. Asimicin inhibits mitochondrial respiration through the inhibition of complex I. Asimicin shows toxicity to Aphis gossypii, mosquito larvae and mammalian[1][2][3][4].
Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity[1][2].
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1[1][2][3][4].
HIV-1 inhibitor-45 (compound IA-6) is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity[1].
RNA polymerase-IN-2 (compound 5) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-2 inhibits CYP isozymes[1].
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals[1].
Benzyl benzoate is used for treatment of paediatric scabies.
cOB1 phermone, a bacterial sex pheromone, effectively inhibits multidrug-resistant Enterococcus faecalis V583[1].
Marbofloxacin hydrochloride is a potent antibiotic of which depends upon its inhibition of DNA-gyrase.Target: DNA-gyraseMarbofloxacin hydrochloride is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin hydrochloride is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].Administration of Marbofloxacin hydrochloride at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin hydrochloride were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin hydrochloride was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin hydrochloride absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin hydrochloride dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3]. Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.
Aeruginosin 98-B is a protease inhibitor. Aeruginosin 98-B inhibits trypsin, plasmin and thrombin with IC50 values of 0.6, 7.0 and 10.0 μg/mL, respectively[1].
Ampicillin is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
Maduramicin (Maduramycin) is isolated from the actinomycete Actinomadura rubra. Maduramicin is an anticoccidial agent for the the treatment of Eimeria spp., E. adenoeides, E. gallopavonis, and E. dispersa infection[1]. Maduramicin induces cell apoptosis in chicken myocardial cells via intrinsic and extrinsic pathways[2].
1-Phenylsemicarbazide is an antifungal agent. 1-Phenylsemicarbazide has the potential for preventing mold growth on industrial products[1].
Protein kinase G inhibitor-1 (Compound 270) is a mycobacterial protein kinase G inhibitor, with an IC50 of 0.9 μM. Protein kinase G inhibitor-1 can be used for mycobacterial infection research[1].
Afabicin is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase[1]. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml[3]. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB)[2].
GSK656 is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.
Papyracillic acid, a fungal metabolite, a Penicillic acid analog, is a nonselective herbicide. Papyracillic acid has anti-bacterial, anti-fungal, nematicidal, and phytotoxic effects[1].
Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities[1]. Camphor is a TRPV3 agonist[2].
N-dodecanoyl-L-Homoserine lactone (C12-HSL) is a quorum sensing (QS) signaling molecule. N-dodecanoyl-L-Homoserine lactone (C12-HSL) aptamers blocks qurom sensing and inhibits biofilm formation in Pseudomonas aeruginosa[1].
Propylparaben sodium is an antimicrobial agent, preservative, flavouring agent[1].
PC945 is a novel broad spectrum antifungal agent that potently inhibits Aspergillus fumigatus sterol 14α-demethylase (CYP51A and CYP51B) with IC50 of 0.23 and 0.22 uM, respectively; shows MIC values 0.032 to >8 ug/ml against 96 clinically isolated A. fumigatus strains, demonstrates activity against itraconazole-susceptible and -resistant A. fumigatus growth with IC50 of 0.0012 to 0.034 ug/ml; PC945 is a broad spectrum of pathogenic fungi with MIC 0.0078 to 2 ug/ml, and exhibits activity in vivo. Fungal Infection Phase 1 Clinical
Pralurbactam is a β-Lactamase inhibitor. Pralurbactam can be used for research of bacterial infection[1][2].