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].
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].
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]
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].
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.
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].
Antibacterial agent 45, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 mg/mL.
Trovafloxacin-d4 mesylate is the deuterium labeled Trovafloxacin mesylate. 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].
Influenza A virus-IN-7 (compound 16r) is a potent and orally active influenza A virus inhibitor with an IC50 of 3.43 µM and CC50 of >100 µM. Influenza A virus-IN-7 shows anti-IAV activity with low cytotoxicity. Influenza A virus-IN-7 inhibits the transcription and replication of viral RNA[1].
Butylparaben sodium strongly influences the later stages of the spermatogenesis in the testis through the deterioration of hormonal control and/or RNA and protein synthesis[1].
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro[1][2].
HCV-IN-39 (Compound 18a) is a potent hepatitis C virus (HCV) nucleoside inhibitor with EC50 values of 0.644, 0.952 and 0.154 μM against GT1a, GT1b and GT1b CES1 replicons[1].
Kievitone, an isoflavanone, could be isolated from hypocotyls of Phaseolus vulgaris L. infected with Rhizoctonia solani Kühn. Kievitone has antifungal activity and antitumor activity[1][2].
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs)[1][2].
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines[1].
Arg-Trp is a dipeptide composed of arginine and tryptophan, and analogues of Arg-Trp-octyl ester show antibacterial activity[1].
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8[1].
Antibacterial agent 47, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway[1].
Libivirumab (17.1.41) is a humanized anti-HBV monoclonal antibody. Libivirumab shows neutralization activity with IC50s of 35, 130 ng/mL for HBsAg, HBeAg, respectively[1].
Moronic acid, a triterpenoid, is an anti-HIV agent. Moronic acid inhibits viral replication with an EC50 value <1 μg/mL, and shows cytotoxicity in H9 lymphocytes with an IC50 value of 18.6 μg/mL. Moronic acid can be isolated from Brazilian propolis[1].
Cyclopetide 1 (Compound 1) is an antimicrobial peptide with moderate activity against B. subtilis, with a MIC of 25 μg/mL[1].
Cefditoren pivoxil is a new-third generation cephalosporin antibiotic that has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens.Target: AntibacterialCefditoren pivoxil, a new-third generation cephalosporin antibiotic that has recently been granted approval in Spain, shows important activity over a large part of the pathogens causing skin, soft tissue and respiratory tract infections, including Gram-negative and Gram-positive bacteria. Cefditoren is also marketed under the name Meiact. Cefditoren has a broad spectrum of activity and has been used to treat bacterial infections of the skin and respiratory tract including bronchitis, pneumonia, and tonsillitis. The following represents MIC susceptibility data for a few medically significant microorganisms.Cefditoren has shown excellent in vitro activity against the Gram-positive pathogens penicillin-susceptible and -intermediate Streptococcus pneumoniae, S. pyogenes and methicillin-susceptible Staphylococcus aureus. Cefditoren was inactive against methicillin-resistant S. aureus. Of the important Gram-negative pathogens, cefditoren had potent antibacterial effects against beta-lactamase-positive and -negative Haemophilus influenzae, H. parainfluenzae and beta-lactamase-positive and -negative Moraxella catarrhalis.
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent[1].