U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 21 - 30 of 70 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Viridicatol is a polar metabolite first isolated from Penicillium cyclopium and P. viridicatum by Birkinshaw and collaborators in 1963. Viridicatol is a 2,3-dihydroxyquinoline which, like its analogue viridicatin, exists in equilibrium with its keto-tautomer. Viridicatol acts as an anti-inflammatory agent by suppressing the expression of pro-inflammatory mediators such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, via inhibition of the nuclear factor-kappa B (NF-κB) pathway in LPS stimulated cells. Further, viridicatol is a selective inhibitor of PTP1B, a potential drug target for the treatment of type 2 diabetes and obesity. Viridicatol revealed potent antibacterial activity against Staphylococcus aureus.
Vulpinic Acid is a lichen metabolite with anti-inflammatory properties. Vulpinic Acid acts as photoprotective agent and antifungal agent. Vulpinic acid mainly affects cell cycle, glycogen metabolism, transcription and translation to fungi. Vulpinic acid showed very strong inhibition effect on TrxR (mitochondrial thioredoxin reductase), so it may be used as a potential drug for cancer therapy. Vulpinic acid possesses diverse biological activities, and lichens containing Vulpinic acid have a strong history of medicinal use. For example, Eskimos and people of Northern Europe have used lichens containing Vulpinic acid to poison the wolf and fox.Lichens containing Vulpinic acid are used as fodder for reindeer and emergency food by Arctic and Subarctic peoples. In central Europe, members of the genus Cetraria, which is known to produce Vulpinic acid, have been used as laxatives and have been taken for coughing, including that associated with tuberculosis.
Helvolic acid is a mycotoxin with antibacterial activity that shows broad activity against Gram positive and negative bacteria. For example Helvolic acid showed potent inhibitory effects against Staphylococcus aureus and Pseudomonas aeruginosa with MIC (minimum inhibitory concentration) values of 5.8 and 4.6ug/mL, respectively. It is a steroidal triterpene that is an inhibitor of the protein biosynthesis through archeal EF-2 (elongation factor 2). Shows antioxidant effects. Helvolic acid also showed in vitro antitrypanosomal activity against Trypanosoma brucei brucei. It showed inhibitory activity against Candida albicans and Plasmodium falciparum.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimethylhydroquinone (2,3,5-Trimethylhydroquinone, TMHQ) is a compound with a wide range of important practical applications. As shown by data from the patent literature, this compound can be used in the synthesis of dyes, pigments, antioxidants, polymerization inhibitors, and other important chemicals. However, the main use of this compound is as an intermediate in the industrial synthesis of vitamin E. Because of the importance of vitamin E in medicine, food manufacturing, and cattle breeding, there is continuing interest in the methods for the preparation of 2,3,5-trimethylhydroquinone. Trimethylhydroquinone presented obvious in vitro anti-MRSA activity.
Status:
US Previously Marketed
First approved in 2024

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ceftobiprole is a fifth-generation cephalosporin antibiotic. It was discovered by Basilea Pharmaceutica and was developed by Johnson & Johnson Pharmaceutical Research and Development. The drug is demonstrates activity against clinically important gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, penicilliin-resistant Staphylococcus pneumoniae, and Enterococcus faecalis. The drug also has demonstrated activity against gram-negative bacteria including Citrobacter spp., Escherichia coli, Enterobacter spp., Klebsiella spp., Serratia marcescens, and Pseudomonas aeruginosa. The drug has gained regulatory authorization from European states for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP).
Alatrofloxacin is a fluoroquinolone antibiotic developed as a mesylate salt and was sold under brand name Trovan, but was withdrawn from the U.S. market in 2001. Trovan was indicated for the treatment of patients initiating therapy in in-patient health care facilities (i.e., hospitals and long term nursing care facilities) with serious, life- or limb-threatening infections caused by susceptible strains of the designated microorganisms in the conditions listed below. Nosocomial pneumonia caused by Escherichia coli, Pseudomonas aeruginosa, Haemophilus influenzae, or Staphylococcus aureus. Community acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Klebsiella pneumoniae, Staphylococcus aureus. Complicated intra-abdominal infections, including post-surgical infections caused by Escherichia coli. Gynecologic and pelvic infections including endomyometritis, parametritis, septic abortion and post-partum infections caused by Escherichia coli, Bacteroides fragilis, viridans group streptococci, Enterococcus faecalis. Complicated skin and skin structure infections, including diabetic foot infections, caused by Staphylococcus aureus, Streptococcus agalactiae, Pseudomonas aeruginosa, Enterococcus faecalis, Escherichia coli, or Proteus mirabilis. After intravenous administration, alatrofloxacin is rapidly converted to trovafloxacin, which is responsible for therapeutic effect. Plasma concentrations of alatrofloxacin are below quantifiable levels within 5 to 10 minutes of completion of a 1 hour infusion.
Niclosamide is an antihelminth used against tapeworm infections. It may act by the uncoupling of the electron transport chain to ATP synthase. The disturbance of this crucial metabolic pathway prevents creation of adenosine tri-phosphate (ATP), an essential molecule that supplies energy for metabolism. Niclosamide works by killing tapeworms on contact. Adult worms (but not ova) are rapidly killed, presumably due to uncoupling of oxidative phosphorylation or stimulation of ATPase activity. The killed worms are then passed in the stool or sometimes destroyed in the intestine. Niclosamide may work as a molluscicide by binding to and damaging DNA. Niclosamide is used for the treatment of tapeworm and intestinal fluke infections: Taenia saginata (Beef Tapeworm), Taenia solium (Pork Tapeworm), Diphyllobothrium latum (Fish Tapeworm), Fasciolopsis buski (large intestinal fluke). Niclosamide is also used as a molluscicide in the control of schistosomiasis. Niclosamide was marketed under the trade name Niclocide, now discontinued.
Totarol is a meroterpene, and more precisely a terpenophenolic, a chemical compound that is part terpene and part natural phenol. It is a naturally produced diterpene that is bioactive as (+)-totarol. It was first isolated by McDowell and Esterfield from the heartwood of Podocarpus totara, a yew tree found in New Zealand. Totarol showed good activity against Mycobacterium tuberculosis H(37)Rv (MIC of 73.7 uM). It was also most active against the isoniazid-, streptomycin-, and moxifloxacin-resistant variants (MIC of 38.4, 83.4 and 60 uM, respectively). Totarol demonstrated nematicidal and antifouling activities against Caenorhabditis elegans and Artemia salina, it inhibited Leishmania donovani promastigotes, showed good antimicrobial activity against effluxing strains of Staphylococcus aureus. Totarol inhibits bacterial proliferation by targeting FtsZ and it may be useful as a lead compound to develop an effective antitubercular drug.
Zinc Ascorbate can be used as a dietary supplement and as a nutrient. Zinc is an important antioxidant nutrient. It is necessary for protein synthesis, wound healing, for blood stability, normal tissue function, and aids in the digestion and metabolism of phosphorus. It also governs the contractility of muscles and maintains the body’s alkaline balance. Zinc ascorbate has superoxide dismutase-like activity and in vitro antimicrobial activity against Staphylococcus aureus and Escherichia coli. Zinc ascorbate may be effective for acne treatment. Zinc ascorbate inhibits the growth of P. acnes (MIC, 640 ug/mL).