W13 is a potent MsbA inhibitor. W13 is an ATPase stimulator with an EC50 of 5.5 µM[1].
Eberconazole is a dichlorinated imidazole derivative with antifungal activity. Eberconazole is more active than Clotrimazole, Ketoconazole, and Miconazole. Eberconazole has the potential for the research of dermatophytoses with a topical administration[1].
Famciclovir(BRL 42810) is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections.IC50 Value: Refer to penciclovirTarget: HSVFamciclovir is the diacetyl 6-deoxy analog of the active antiviral compound penciclovir with potential use in the treatment of infections caused by the herpes family of viruses [1]. Famciclovir, a synthetic acyclic guanine derivative, is a prodrug which, after oral administration, is rapidly metabolised to the highly bioavailable antiviral compound penciclovir [2].in vitro: Famciclovir induced rapid, dose-dependent suppression of viral replication and reduction in alanine aminotransferase (ALT), with greatest efficacy in the 500-mg tid treatment group. HBV DNA reduction was maintained throughout the treatment period. ALT also steadily declined during the treatment period [3]. in vivo: In rat, following dosing at 40 mg/kg, famciclovir was rapidly and extensively metabolized to the active antiviral compound penciclovir, which reached peak concentrations in the plasma (mean 3.5 micrograms/ml) at 0.5 h [4]. Necrotic hepatitis was significantly (p < 0.01) reduced by treatment with FCV, VACV and ACV at a dose of 50 mg/kg per day divided into 3 doses. No significant effect was achieved with BVDU at 200 mg/kg per day. Treatment with FCV at 50 mg/kg per day, ACV at 100 mg/kg per day, and VACV at 200 mg/kg per day significantly (p < 0.001) decreased mortality in mice [5].Clinical trial: Famciclovir Pediatric Formulation In Children 1 to 12 Years Of Age With Herpes Simplex Infection. Phage3
Secologanin dimethyl acetal (Compound Ⅱ) is an iridoid glucoside that can be isolated from Pterocephalus perennis. Secologanin dimethyl acetal shows antimicrobial activity against S.aureus and S.epidermidi[1].
Punicalin is a hydrolyzable tannin isolated from Punica granatum L. or the leaves of Terminalia catappa L.. Punicalin is a anti-hepatitis B virus (HBV) agent and has anti-inflammatory activity[1][2].
RSV-IN-4 (Compound 2) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza virus A (IAV). RSV-IN-4 shows anti-RSV activity (EC50 = 11.76 μM)[1].
1,3-Dithiane is a protected formaldehyde anion equivalent that could serve as a useful labeled synthon[1]. 1,3-Dithiane is also a sulfur-containing Maillard reaction products (MRPs) found in boiled beef extracts. 1,3-Dithiane shows a potent direct-acting mutagenicity toward S. typhimurium TA98 and TA100[2].
Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens.
Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM[1].
1-Methoxyberberine chloride is a plant alkaloid that can be found in Corydalis longipes. 1-Methoxyberberine chloride exhibits antifungal effects[1].
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].
Asperglaucin A represents an unusual phthalide-like derivative. Asperglaucin A exhibits potent antibacterial activities against two plant pathogens Pseudomonas syringae pv actinidae (Psa) and Bacillus cereus, with an MIC value of 6.25 μM[1].
5-(Hydroxymethyl)furan-2-carbaldehyde, derived from lignocellulosic biomass, inhibits yeast growth and fermentation as stressors.
PD 113270 (CL 1565-B) is an antitumor agent. PD 113270 exhibits inhibitory effects to yeasts[1].
Sulfacetamide Sodium is an anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections.Target: AntibacterialSulfacetamide is a sulfonamide antibiotic. Sulfacetamide is able to inhibit the growth of all isolated strains. Depending on the type of bacteria concentrations of 0.006 up to 6.4% sodium sulfacetamide proved to be effective. Simultaneously, all patients were treated with sulfacetamide containing ointment and/or eye drops 4 times daily for maximum of 14 days. With swabs taken at intervals of 7 and 14 days no bacterial growth was detected. Sulfacetamide 10% topical lotion, sold under the brand name Klaron or Ovace, is approved for the treatment of acne and seborrheic dermatitis. Sulfacetamide has been investigated for use in the treatment of pityriasis versicolor and rosacea. It may also have anti-inflammatory properties when used to treat blepharitis or conjunctivitis. It is believed to work by limiting the presence of folic acid which bacteria need to survive. It has been suggested that sulfacetamide may also serve as a treatment for mild forms of hidradenitis suppurativa. Sulfacetamide has antibacterial activity and is used to control acne. Some research indicates that sulfacetamide derivatives may act as antifungals by an CYP51A1-independent mechanism [1-4].
Cephapirin sodium (Cefapirin sodium), a semisynthetic cephalosporin antibiotic, is bactericidal against strains of gram-positive and gram-negative bacteria[1].
Macranthoside A is a triterpene glycoside with anti-microbially activity[1].
Gatifloxacin (mesylate) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.Target: AntibacterialGatifloxacin (mesylate) is the mesylate salt of Gatifloxacin which is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].Clinical indications: Bacterial infection Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Swinholide A is the actin-binding marine polyketide and dimerizes actin with the Kd of ~ 50 nM[1]. Swinholide A is a microfilament disrupting marine toxin that stabilizes actin dimers and severs actin filaments. Swinholide A disrupts the actin cytoskeleton of cells.Antifungal activity[2].
Rimteravimab (XVR011) is a bivalent VHH-Fc antibody with potent neutralizing activity with high stability, broad coverage and silenced Fc effector functions against the disease caused by SARS-CoV-2[1].
2-Chloro-N-(2-methyl-4-bromophenyl)acetamide is an antifungal compound[1].
Enfumafungin, a triterpene glycoside, is isolated from extracts derived from an endophytic species of Hormonema. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis[1][2].
Poly-L-lysine hydrochloride is a nonspecific attachment factor for cells useful in promoting cell adhesion to solid substrates by enhancing electrostatic interaction between negatively charged ions of the cell membrane and the culture surface. Poly-L-lysine is a strong-attraction regulator that promotes liquid-liquid phase separation (LLPS) at low concentrations but suppresses LLPS at high concentrations. Antibacterial cationic peptide.[1].
Aspoxicillin is a broad-spectrum antimicrobial agent against 68 isolates of Actinobacillus pleuropneumoniae with an MIC90 value of <= 0.05 μg/ml. Aspoxicillin has a long half-life in mouse serum of 55 minutes[1][2].
SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent nsp13 (non-structural protein 13) inhibitor. SARS-CoV-2 nsp13-IN-1 only inhibits nsp13 ssDNA+ ATPase, with an IC50 of 6 μM. SARS-CoV-2 nsp13-IN-1 does not inhibit ssDNA- ATPase. SARS-CoV-2 nsp13-IN-1 can be used for COVID-19 research[1].
Antitubercular agent-18 (Compound 9a) is an antitubercular agent with MIC values of 2, 2, 2 and 128 µg/ml against M. tuberculosis H37Rv, Spec. 192, Spec 210 and Spec. 800, respectively. Antitubercular agent-18 shows highly selective antimycobacterial effects[1].
Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
Neophellamuretin is a flavonoid. Neophellamuretin inhibits Trichophyton sp. with an MIC value of 62.5 µg/mL[1].
Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria[1].