Albomycin is an inhibitor of aminoacyl-tRNA synthetases with Trojan-horse effect. Albomycin is delivered by iron-chelator portion into bacterial through ferrichrome-specific transporter system. Albomycin combats against a wide range of Gram-positive and Gram-negative bacteria. Albomycin also serves as an efficient iron-scavenger of producer[1].
Thiostrepton is a natural cyclic oligopeptide antibiotic, is a natural product of the ribosomally synthesized and post-translationally modified peptide (RiPP) class.
Oxytetracycline dihydrate is a broad-spectrum antibiotic that acts by inhibiting protein synthesis in bacteria[1].
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.
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1][2][3][4].
Cefazolin is an antibiotic used for the research of a number of anti-bacterial infections. Cefazolin can be used for the prophylaxis of surgical antimicrobial. Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD)[1].
MtUng-IN-1 (Compound 18a) is a Uracil DNA glycosylase of Mycobacterium (MtUng) inhibitor (IC50: 300 μM). MtUng-IN-1 can be used for research of cancers and infectious diseases[1].
Faltan is a dicarboximide fungicide, widely used on vines and several vegetable crops, and is also cytotoxic effect on human bronchial epithelial cells[1].
Bromodiphenhydramine (Ambodryl) is a potent antihistamine with antimicrobial property. Bromodiphenhydramine inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine can be used for cutaneous allergies research[1][2][3].
Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells[1][2].
Moiramide B is a potent acetyl-CoA carboxylase (ACC) inhibitor with an IC50 value of 6 nM. Moiramide B has antibacterial activity[1].
Artemisone (Artemifone) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains, with a mean IC50 of 0.83 nM[1].
Levofloxacin-13C,d3 is the 13C- and deuterium labeled.
Emtricitabine-13C,15N2 (BW1592-13C,15N2) is a 13C- and 15N-labeled Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Indole-3-acetaldehyde inhibits Escherichia coli O157:H7 biofilm formation[1].
FPI-1523 sodium, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 sodium also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 sodium exhibits considerable antimicrobial activity[1].
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].
Schisanwilsonin C (Arisanschinin K) shows anti-HBV activity[1].
Gontivimab (ALX-0171; VR-465) is a poent anti-RSV prefusion F protein nanobody with a KD value of 0.113 nM. Gontivimab shows antiviral activity. Gontivimab reduces the RSV load in the nose and lung[1].
Tamarixin is flavonoid that isolated from Astragalus tanae Sosn that has hepatoprotective, antioxidant, anticancer, and antimicrobial activities[1].
Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
(-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity[1].
AZD5099, an antibacterial agent, is a potent and selective bacterial topoisomerase II inhibitor. AZD5099 potently inhibits the infections caused by Gram-positive and fastidious Gram-negative bacteria[1].
Moxifloxacin-d3-1 hydrochloride (BAY 12-8039-d3-1) is a deuterium labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2][3].
Lomefloxacin (SC47111A) aspartate is a broad-spectrum quinolone antibacterial agent. Lomefloxacin aspartate can be used for researching respiratory tract infections, genitourinary infections, gastrointestinal infections, ENT infections, etc.[1][2].
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].
L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis[1][2].
Protionamide (or prothionamide) is a drug used in the treatment of tuberculosis; has also been tested for use in the treatment of leprosy.Target: Anti tuberculosisAlthough ETH and PTH are both potent drugs against M. tuberculosis (MIC = ～0.5 μg/ml) (24), they do not affect E. coli growth, even at very high concentrations (100 μg/ml), which is primarily caused by the absence of an EthA homologue in E. coli [1]. Clinical improvement was noted in 74% of the patients treated with ethionamide and in 83% of those treated with prothionamide. Therapy was well tolerated and drug-related hepatotoxicity did not require discontinuation of therapy. The 500-mg dose of both ethionamide and prothionamide resulted in loss in Mycobacterium leprae viability more rapidly than did the 250-mg dose, and prothionamide at both dose levels was superior to the equivalent dose of ethionamide [2].
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].