AU1235 is an adamantyl urea inhibitor of Mycobacterium tuberculosis.
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].
Meropenem trihydrate is a carbapenem antibiotic with broad-spectrum antibacterial activity.
cis-β-Terpineol, a monoterpene compound, can be isolated from the aerial parts of A. turcomanica. However, the stems, leaves and flowers of P. turkmen showed antibacterial activity[1].
CCR-11 is an antibacterial agent. CCR-11 can inhibit the proliferation of B. subtilis cells with an IC50 value of 1.2 μM. CCR-11 inhibits HeLa cell proliferation with an IC50 value of 18.1 μM. CCR-11 inhibits bacterial cytokinesis by inhibiting FtsZ assembly. CCR-11 can be used for the research of FtsZ-targeted antibacterial agents[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].
Friulimicin D, a lipopeptide antibiotic, like Friulimicin B, is isolated from the actinomycete Actinoplanes friuliensis[1].
2-Hydroxy-1-methoxyanthraquinone could be isolated from the stem bark of Morinda lucida Benth. (Rubiaceae) and possesses antibacterial activity[1].
alpha-Mangostin-d3 (α-Mangostin-d3) is the deuterium labeled alpha-Mangostin. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM[1][2][3].
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].
Garenoxacin-d4 (BMS284756-d4) is the deuterium labeled Garenoxacin. Garenoxacin (BMS284756) is a quinolone antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections[1][2].
Duramycin (Moli1901;Lancovutide) is a cyclic peptide lantibiotic derived from Streptomyces cinnamoneuma. Duramycin stimulates chloride secretion in airway epithelium and has the potential for cystic fibrosis treatment. Duramycin interacts with phosphatidylethanolamine (PE) and has antibacterial, antiviral effects[1][2].
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].
Efrotomycin is an orally active antibiotic. Efrotomycin can be isolated from the Streptomyces Lactamdurans. Efrotomycin has insignificant effect on Salmonella typhimurium quantity, duration, shedding rate, and antimicrobial susceptibility in infected pigs[1][2].
Norstictic acid is a potent and selective allossteric transcriptional regulator. Norstictic acid shows anticancer activity. Norstictic acid shows antioxidant activity and antimicrobial activity[1][2][3][4].
Omadacycline is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.IC50 Value:Target: Antibacterialin vitro: in vivo: Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
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].
Vincetoxicoside B, isolated from Polygonum paleaceum Wall, shows antifungal activity[1].
Antibacterial agent 96 (compound 4k) is a potent antibacterial agent. Antibacterial agent 96 shows antitubercular activity against drug-susceptible and multidrug-resistantMycobacterium tuberculosis (M. tuberculosis) strains. Antibacterial agent 96 shows toxicity to HepG2 and Vero cells[1].
Lauryl-LF 11, N-terminally acylated analogue of LF11, is a peptide with antibacterial activity[1].
Danofloxacin Mesylate(CP76136-27 mesylate) is a fluoroquinolone antibacterial for veterinary use.Target: AntibacterialDanofloxacin is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase, which is necessary for supercoiling of DNA to provide a suitable spatial arrangement of DNA within the bacterial cell. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, is 0.125 μg/ml [1]. Danofloxacin shows protective dose (PD50) of 0.38, 0.8, 2.42 mg/kg for P. multocida, E. coli and S. choleraesuis in in vivo mouse protection assay [2].
Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively[1].
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice[1].