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

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Showing 951 - 960 of 1728 results

Status:
Possibly Marketed Outside US
Source:
CLEARASIL DAILY CLEAR REVIVING TONER by Shelton, R. S.; Campen, M. G. Van; Tilford, C. H.; Lang, H. C.; Nisonger, L.; Bandelin, F. J.; Rubenkoenig, H. L.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Tetradonium is a cationic germicidal detergent, often used in disinfectant and deodorant compositions.
Status:
Possibly Marketed Outside US
Source:
Japan:Lenapenem Hydrochloride Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Lenapenem is an anti-bacterial agent that was tested in late 90's in phase II clinical trials against bacterial infections. Lenapenem was shown to be active against both Gram-positive and Gram-negative bacteria and exerted its therapeutic effect by inhibiting penicillin binding proteins. The development of the drug was terminated due to the safety reason.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefluprenam
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Cefluprenam is an anti-bacterial agent of broad spectrum. It was active in vitro against different bacteria strains with MIC values from 0.78 ug/ml to 3.13 ug/ml. The drug exerts its bactericidal activity through inhibition of penicillin-binding proteins, showing high affinity to all four subtypes. Cefluprenam was tested for the treatment of respiratory tract infections in phase III study, however the drug development was stopped.
Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Dapivirine, an anti-retroviral (ARV)-based microbicide, is a substituted diaminopyrimidine (DAPY) derivative and a potent non-nucleoside reverse-transcriptase inhibitor (NNRTI) with antiviral activity against HIV-1. Dapivirine showed high activity against wild-type and mutant HIV in in virto HIV models inhibiting a broad panel of HIV-1 isolates from different classes, including a wide range of NNRTI-resistant isolates. Developed by Janssen Sciences (formerly Tibotec Pharmaceuticals), dapivirine was initially tested as an oral treatment for HIV in a number of Phase I/II clinical trials. In 2014 the International Partnership for Microbicides (IPM) began its work on the monthly dapivirine ring. Phase I/II clinical trials in Africa, Europe and the United States proved that dapivirine is safe and well-tolerated. Phase III long-term safety and efficacy studies of the monthly dapivirine ring as part of IPM's Dapivirine Ring Licensure Program confirmed that the monthly dapivirine ring can safely help prevent HIV infection in women. In 2016 the ASPIRE Study reported a 27 percent reduction in HIV-1 acquisition with a trend toward greater protection in women over age 21 and no significant protection for women under age 21.
Status:
Possibly Marketed Outside US
Source:
Canada:SYMCLOSENE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Trichloroisocyanuric acid (1,3,5-trichloro-1,3,5-triazine-2,4,6(1H,3H,5H)-tri-one or TCCA) is an N-halo compound which has been known since 1902. It has been used primarily as a disinfectant in swimming pools and water treatment as bleaching agent and bactericide. Recently, TCCA has become attractive candidate as a homogeneous catalyst in organic transformations due to its lack of volatility, commercial availability, low cost and ease of handling. And is also used as a bleaching agent in the textile industry
Neticonazole is an antifungal drug. It is especially active against Candida glabrata, Trichophyton, Microsporum, Aspergillus and Fonsecaea spp. Clinical experience demonstrated neticonazole as a safe and effective treatment of mycoses like trichophytosis, candidiasis, and different types of tinea.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Possibly Marketed Outside US
Source:
Ceftezole sodium for injection by Fujisawa Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ceftezole sodium is a cephalosporin antibiotic. Ceftezole was found to be a broad-spectrum antibiotic, active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole sodium is used as an injectable or through an intravenous mode of delivery. The bactericidal activity of ceftezole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall component from being properly synthesized. Ceftezole has been shown to exhibit potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Ceftezole is used for the treatment of susceptible bacterial infections including septicemia, respiratory, biliary or GU tract, skin and skin structure, endocarditis. Surgical prophylaxis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Amocarzine is an antifilarial antihelminthic drug, derived from amoscanate, that is active against the adult worms of Onchocerca volvulus. In animal studies of filarial infections, amocarzine showed promise as a macrofilaricidal drug and was afterward extensively tried in humans. Amocrazine has an adverse effects: dizziness, itching and rush. There were reversible neurological symptoms, such as impaired coordination and a positive Romberg’s sign. In a study from Ghana, the combination of ivermectin and amocarzine was not more effective than ivermectine alone and adverse effects were more severe. Amocarzine has no role in the treatment of onchocerciasis in Africa. In silico data emphasize that amocarzine could be potential lead compound that can be further developed into nematicidal chemical against Bursaphelenchus xylophilus.