Flucytosine (5-Fluorocytosine, 5-FC, Ancobon), a fluorinated pyrimidine analogue, is an antifungal drug.Target: antifungalFlucytosine, or 5-fluorocytosine, a fluorinated pyrimidine analogue, is a synthetic antimycotic drug. It is structurally related to the cytostatic fluorouracil and to floxuridine. It is available in oral and in some countries also in injectable form. A common brand name is Ancobon. Flucytosine was first synthesized in 1957 but its antifungal properties were discovered in 1964. The drug is dispensed in capsules of 250 mg and 500 mg strength. The injectable form is diluted in 250 mL saline solution to contain 2.5 g total (10 mg/mL). The solution is physically incompatible with other drugs including amphotericin B.Flucytosine is well absorbed (75 to 90%) from the gastrointestinal tract. Intake with meals slows the absorption, but does not decrease the amount absorbed. Following an oral dose of 2 grams peak serum levels are reached after approximately 6 hours. The time to peak level decreases with continued therapy. After 4 days peak levels are measured after 2 hours. The drug is eliminated renally. In normal patients flucytosine has reportedly a half-life of 2.5 to 6 hours. In patients with impaired renal function higher serum levels are seen and the drug tends to cumulate in these patients. The drug is mainly excreted unchanged in the urine (90% of an oral dose) and only traces are metabolized and excreted in the feces. Therapeutic serum levels range from 25 to 100 ?g/ml. Serum levels in excess of 100 ug are associated with a higher incidence of side effects. Periodic measurements of serum levels are recommended for all patients and are a must in patients with renal damage.
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea[1][2].
Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Antifungal agent 69 (compound 13) is a eugenol-imidazole against Candida albicans (MIC: 4.6 μM) with no relevant cytotoxicity. Antifungal agent 69 alters the fungal ergosterol biosynthesis and shows antifungal activity[1].
Broxaldine is an antiprotozoal drug.
Trypanothione synthetase-IN-3 is a noncompetitive mixed hyperbolic Trypanothione synthetase (TryS) inhibitor (Ki: 0.8 μM). Trypanothione synthetase-IN-3 can be used in the study of parasites, such as L. infantum[1].
L 696229 is a specific inhibitor ofhuman immunodeficiency virus type 1 (HIV-1)reverse transcriptase (RT) activity that possesses antiviral activity[1].
3β,7β,15β-Trihydroxy-11-oxo-lanosta-8-en-24→20 lactone is a natural compound that could be isolated from G. lucidum with antimycobacterial activity.
FtsZ-IN-1 is a potent FtsZ inhibitor with quinolinium ring. FtsZ-IN-1 has stronger antibacterial activity against Gram-positive bacteria with MICs of 0.5-8 μg/mL. FtsZ-IN-1 significantly causes cell elongation of B. subtilis by enhancing FtsZ polymerization. FtsZ-IN-1 exhibits low hemolytic toxicity and low tendency to induce drug resistance. FtsZ-IN-1 has against drug-resistant bacteria activity[1].
Defensin HNP 4 (HNP 4) is a single 11 amino acid long fragment of HNP-41-11. Defensin HNP 4 has inhibitory effect against multidrug-resistant and non-resistant strains[1].
Phenothiazine is an antibiotic which has insecticidal, fungicidal, antibacterial and anthelmintic activities. Phenothiazine also can be used for the research of neurological diseases[1][2].
(-)-Ketoconazole-d3 is deuterium labeled (-)-Ketoconazole. (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway[1]. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro[2].
Pentamidine isethionate is an antimicrobial agent for prevention and treatment of Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii.
Icariside D2, isolated from Annona glabra fruit, inhibits angiotensin-converting enzyme. Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM. Icariside D2 induces apoptosis [1][2].
Bibrocathol is antiseptic agent plays important role in acute eyelid diseases like blepharitis[1].
5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].non-alcoholic fatty liver disease[1][2][3].
Tuberculosis inhibitor 12 (compound 12) is an oxadiazole derivative and an inhibitor of Mycobacterium tuberculosis. The inhibition rates of Tuberculosis inhibitor 12 (20 μM) on 7H9-Tw-OADC and 7H9-Tw-OADC reached 82% and 78% respectively[1].
Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.IC50 Value: Target: HCV
Alamethicin, isolated from Trichoderma viride, is a channel-forming peptide antibiotic and induces voltage-gated conductance in model and cell membranes[1][2].
Antibacterial agent 72 displays the antibacterial activities by targeting the bacterial membrane.
Squalene is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity.
A potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 89 nM; shows anti-RSV activity with IC50 of 57.6 nM and 47.8 nM for RSV A2 and RSV B-EST, respectively; shows weak cytotoxicity (CC50=600 nM).
Synthalin A sulfate is a biguanylated diamine with antibacterial and hypoglycemic properties. Synthalin A sulfate against S. aureus with a MIC of 64 μg/mL[1].
Doxycycline hydrochloride is a tetracycline antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
DL-Pyroglutamic acid (CAE) as an inactivator of hepatitis B surface, inactivates vaccinia virus, herpes simplex virus, and influenza virus except poliovirus. DL-Pyroglutamic acid is also a possible inhibitor of GABA transaminase, increases GABA amount with antiepileptic action[1][2].
Enpp-1-IN-5 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-5 has the potential for the research of cancer and infectious diseases (extracted from patent WO2019046778A1/WO2021203772A1, compound 1)[1][2].
Methisazone (Marboran) is an antiviral agent that works by inhibiting mRNA and protein synthesis. Methisazone is also a SARS-CoV-2 (COVID-19) inhibitor. Methisazone is mainly used in pox viruses[1].