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

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Showing 411 - 420 of 1728 results

Status:
Investigational
Source:
INN:pirinidazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pirinidazole was found to be the compound from a series of 5-nitroimidazoles with the broadest action against protozoans. Its effect against trichomonads is the most pronounced. The comparison of the effective doses of different 5-nitroimidazoles against Trichomonas fetus demonstrates that the compound Pirinidazole is slightly superior to Tinidazole, distinctly superior to Metronidazole, and very much superior to Nitrimidazine. Some toxicological data of Pirinidazole show that the compound is well tolerated.
Status:
Investigational
Source:
INN:dietifen [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Dietifen is an anesthetic, vasodilator and antifungal agent. The main pharmacological feature of the drug is its ability to cause expansion of the coronary vessels. It also has a moderate spasmolytic activity (reduces spasms of the muscles of the intestine and other internal organs) and somewhat inhibits the conduction of nervous excitement through the vegetative nodes. Significant changes in blood pressure and pulse rate does not cause, does not possess hormonal (estrogenic) activity. It is indicated for the treatment of chronic coronary insufficiency, angina pectoris, severe forms of coronary sclerosis and pre-infarction conditions (simultaneously with anticoagulants).
Rupintrivir is a peptide aldehyde that targets the human rhinovirus (HRV) 3C proteinase enzyme and has the potential for the treatment of the common cold. Rupintrivir is derived from AG-6084 - in order to develop human rhinovirus 3C protease inhibitors with improved pharmacological properties, Agouron replaced the backbone amide moiety of the series which yielded AG-6084, with a ketomethylene isostere. A phase II efficacy study has been completed in healthy patients infected with the rhinovirus. Ruprintrivir was well tolerated; blood-tinged mucus and nasal passage irritation were the most common adverse effects reported. Pharmacokinetic analysis of plasma and nasal ruprintrivir concentrations revealed intranasal drug residence with minimal systemic absorption. The fact that rupintrivir is active against noroviruses belonging to genogroup I (Norwalk virus), genogroup V (murine norovirus), and the recombinant 3C-like protease of a GII norovirus suggests that the drug exerts cross-genotypic anti-norovirus activity and will thus most likely be effective against the clinically relevant human norovirus strains. Rupintrivir is also a high affinity inhibitor of Enterovirus-71 3C protease.
Status:
Investigational
Source:
NCT00002315: Phase 3 Interventional Completed HIV Infections
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Netivudine [882C, 882C87, BW 882, Py-araU, Zonavir®] is an orally active thymidine analogue which was being investigated as a treatment for herpes zoster virus infections. Netivudine is a nucleoside analog with potent, specific activity against varicella-zoster virus. It is approximately seven times as potent as acyclovir with an in vitro 50% inhibitory concentration of 1 to 2 uM.
Status:
Investigational
Source:
INN:maleylsulfathiazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Maleylsulfathiazole is a sulphonamide antibacterial. It was used in the treatment of diarrhea.
Status:
Investigational
Source:
INN:dicresulene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dicresulene is the antiseptic agent. It was used as a hemostatic drug for the control of persistent bleeding.
Status:
Investigational
Source:
INN:ceftiolene
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ceftiolene (42980RP) is a new cephalosporin with a broad antibacterial spectrum similar to cefotaxime or ceftriaxone. The affinities of ceftiolene for penicillin-binding proteins are very comparable with those of ceftriaxone and cefotaxime for Escherichia coli, and generally greater than those of latamoxef (moxalactam) for the higher molecular weight PBPs of E. coli. Enterobacter cloacae. The affinity of ceftiolene for PBP1 of Staphylococcus aureus is greater than those of cefotaxime or latamoxef but comparable with these antibiotics for PBP3. The bacteriolytic activity of ceftiolene at defined concentrations against Gram-negative organisms is similar to that of ceftriaxone and significantly better than that of the other third-generation cephalosporins tested.
Status:
Investigational
Source:
INN:aminoquinol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Aminoquinol (XIB4035) is a nonpeptidyl small molecule agonist for GFRalpha-1. XIB4035 concentration-dependently inhibited [(125)I]GDNF binding in Neuro-2A cells with an IC(50) of 10.4 uM. GDNF induced autophosphorylation of Ret protein, and promoted neurite outgrowth in Neuro-2A cells. XIB4035, like GDNF, induced Ret autophosphorylation in the Neuro-2A cells. Moreover, XIB4035 promoted neurite outgrowth in a concentration-dependent manner. These results show that XIB4035 may act as an agonist at GFRalpha-1 receptor complex, and mimic neurotrophic effects of GDNF in Neuro-2A cells. It has been shown that topical application of XIB4035 is an effective treatment for small-fiber neuropathy (SFN). Topical application of GFRα/RET receptor signaling modulators may be a unique therapy for SFN, and XIB4035 is a candidate therapeutic agent. Aminoquinol has been also used in the therapy of cutaneous leishmaniasis and lambliasis.
Status:
Investigational
Source:
INN:subathizone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Subathizone (also known as Berculon B) is a thiosemicarbazone derivative useful for the chemotherapy of tuberculosis. In preclinical models, Subathizone shows potent activity in experimental tuberculosis in the mouse. In clinical trial, Subathizone shows moderate efficacy and frequent adverse events. Gastrointestinal disturbances and progressive anemia were the most toxic effects, but liver dysfunction, malaise, depression and lassitude, exanthemata, and conjunctival irritation also occurred.
Status:
Investigational
Source:
INN:debropol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Debropol is an aliphatic nitro compound, synthesized by The Boots Company. Debropol possesses antimicrobial activity against Pseudomonas aeruginosa.