Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.Target: AntiparasiticArtemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy. Artemether exhibits the highest activity against juvenile stages of the parasites, while adult worms are significantly less susceptible. There was no indication of neurotoxicity following repeated high doses of artemether given fortnightly for up to 5 months. Artemether-integrated with other control strategies-has considerable potential for reducing the current burden of schistosomiasis in different epidemiological settings [1]. There were remarkably inhibitory effects of artmeter on brain glioma growth and angiogenesis in SD rats and the mechanism that artemether inhibited brain glioma growth might be penetrating the blood-brain barrier and inhibiting angiogenesis [2].
RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.IC50 value: 0.86 uM(EC50) [1]Target: RSV inhibitorRSV604, a novel benzodiazepine with submicromolar anti-RSV activity. It proved to be equipotent against all clinical isolates tested of both the A and B subtypes of the virus. The compound has a low rate of in vitro resistance development. Sequencing revealed that the resistant virus had mutations within the nucleocapsid protein. This is a novel mechanism of action for anti-RSV compounds. In a three-dimensional human airway epithelial cell model, RSV604 was able to pass from the basolateral side of the epithelium effectively to inhibit virus replication after mucosal inoculation. RSV604, which is currently in phase II clinical trials, represents the first in a new class of RSV inhibitors and may have significant potential for the effective treatment of RSV disease.
Cethromycin (ABT-773, Abbott-195773, A-195773) is a ketolide antibiotic[1].
3,5-Dimethoxybenzoic acid, isolated from Melia azedarach L. leaves with antifungal activity, is an intermediate in organic synthesis[1].
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
Isoaltenuene is an anti-bacterial agent with moderate activity against Staphylococcus aureus. Isoaltenuene can be isolated from fungus Alternaria alternate cib-137[1].
Fosmidomycin sodium salt is a phosphonic acid antibiotic and a antimalarial drug, which is active against both Gram-negative and Gram-positive bacteria.
Erythrocentaurin, a natural compound, is a new class of hepatitis B virus inhibitor[1].
Antibacterial agent 56 (example 22) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity[1].
HCoV-OC43-IN-1 (Compound IV-16) is a coronavirus HCoV-OC43 inhibitor. HCoV-OC43-IN-1 has antiviral efficacy (EC50: 90 nM). HCoV-OC43-IN-1 inhibits the mRNA level and expression of viral nucleocapsid protein (NP)[1].
2',3'-Dehydrosalannol is a potent antibacterial agent. 2',3'-Dehydrosalannol shows antibacterial activity against K. pneumonia ATCC 13883, P. aeruginosa ATCC 27853, S. aureus ATCC 25922, E. coli ATCC 11775, and E. faecalis ATCC 10541, with MIC values of 0.78, 1.56, 1.56, 6.25, and 25 µg/mL, respectively[1].
Zanamivir–cholesterol conjugate is a long-acting neuraminidase inhibitor with potent efficacy against drug-resistant influenza viruses.
Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].
(R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNA damage[1][2][3].
4'-Hydroxy-2,4-dimethoxychalcone is a natural chalcone derivatives in the red herbal resin of Dracaena cochinchinensis. 4'-Hydroxy-2,4-dimethoxychalcone displays a wide range of biological activities including antimalarial, antiprotozoal, antibacterial, antifungal activity[1][2].
Lesofavumab (MHAB5553A) is a human IgG1κ anti-influenza B virus antibody[1].
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
UGM-IN-3 (compound 10a) is a UDP-galactopyranose mutase (UGM) inhibitor with a Kd of 66 μM. UGM-IN-3 inhibits the growth of Mycobacterium tuberculosis with a MIC value of 6.2 μg/mL[1].
Cepharanthine, an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities[1][2][3]. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R)[3]. Cepharanthine induces autophagy, apoptosis and cell cycle arrest in breast cancer cells[4]. Cepharanthine inhibits the HIV-1 entry process by reducing plasma membrane fluidity[5].
Treating Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections[1].
SARS-CoV-2 nsp13-IN-3 (Compound C3) is a SARS-CoV-2 non-structural protein 13 (nsp13) small-molecule inhibitor with an IC50 of 32 μM against nsp13 ssDNA+ ATPase[1].
Flurithromycin ((8S)-8-Fluoroerythromycin A) is an orally active broad spectrum antibiotic. Flurithromycin can be used in the research of bacterial infections[1][2][3].
Enoxacin is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.Target: antibacterialEnoxacin is a new quinolone carboxylic acid compound. Its activity against 740 bacterial isolates was determined. It inhibited 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml [1]. Daily plasma theophylline concentrations were measured in 14 patients. The mean +/- s.d. theophylline concentrations increased from 8.5 +/- 2.8 micrograms ml-1 prior to enoxacin to a maximum of 21.7 +/- 7.8 micrograms ml-1 during coadministration [2].
Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Picropodophyllone, an aryltetralin lignan, is isolated from leaves of Podophyllum hexandrum, and has antifungal activities[1][2].
Cyclacillin (Wy-4508) is an orally active aminopenicillin antibiotic, shows antibacterial activity against a wide range of gram-positive and gram-negative pathogens[1].
Cefalexin monohydrate is a cephalosporin antibiotic.Target: AntibacterialCefalexin (INN, BAN) or cephalexin (USAN, AAN) is a first-generation cephalosporin antibiotic introduced in 1967 by Eli Lilly and Company. It is an orally administered agent with a similar antimicrobial spectrum to the intravenous agents cefalotin and cefazolin. It was first marketed as Keflex (Lilly), and is marketed under several other trade names. As of 2008, cefalexin was the most popular cephalosporin antibiotic in the United States, with more than 25 million prescriptions of its generic versions alone, for US$255 million in sales (though less popular than two other antibiotics, amoxicillin and azithromycin, each with 50 million prescriptions per year).Cefalexin is marketed by generic pharmaceutical manufacturers under a wide range of brand names, including: Apo-Cephalex, Biocef, Cefanox, Ceforal, Cephabos, Cephalexin, Cephorum, Ceporex, Cilex, Ialex, Ibilex, Kefexin, Keflet, Keflex, Rekosporin, Keforal, Keftab, Keftal, Lopilexin, Larixin, Novo-Lexin, Ospexin, Tenkorex, Zephalexin, Panixine Disperdose, Rancef, Sialexin, Sporidex and Ulexin. A version of Keflex 750 mg capsules is marketed for twice-daily dosage, to improve compliance. However, it is not a sustained release formulation, and since it is more expensive than the older strengths, some physicians prescribe three 250 mg capsules to be taken twice daily, as a less expensive alternative.
Antibacterial agent 46 is an antibacterial agent extracted from patent WO2013030735A1, example 9. Antibacterial agent 46 can be used for the research of bacterial infections[1].