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Primary Target

Trichophyton rubrum

5

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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US Approved Rx

3

Possibly Marketed Outside US

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Highest Phase

Approved

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Approval Year

1982

3

Unknown

2

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Condition

Tinea pedis

3

Allergic asthma

1

Cerebral ischemia

1

Herpes simplex virus type 1 infection

1

Mycoses

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Treatment Modality

Curative

3

Primary

2

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CNS Active

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Originator

Merz

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Chemical

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CAS

5

EPA CompTox

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FDA UNII

5

PUBCHEM

5

ChEMBL

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ATC Level 1

DERMATOLOGICALS

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GENITO URINARY SYSTEM AND SEX HORMONES

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ATC Level 2

ANTIFUNGALS FOR DERMATOLOGICAL USE

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GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS

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ANTIFUNGALS FOR TOPICAL USE

2

ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS

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ATC Level 4

Imidazole and triazole derivatives

1

Imidazole derivatives

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Other antifungals for topical use

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Showing 1 - 5 of 5 results

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ECONAZOLE

6Z1Y2V4A7M

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Status:

US Approved Rx (2002)

First approved in 1982

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Cytochrome P450 51

Trichophyton rubrum

Conditions:

Econazole (commonly used as the nitrate salt) is an antifungal medication of the imidazole class. It is a broad spectrum antimycotic with some action against Gram positive bacteria. It is used topically in dermatomycoses also orally and parenterally....

Sold under the brand name Ecoza among others, it is indicated for the treatment of interdigital tinea pedis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum in patients 12 years of age and older. Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

HYDROXYRESVERATROL

6V071CP5CR

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cyclooxygenase-1

Trichophyton rubrum

Oxidative Stress

Conditions:

Cerebral ischemia

Allergic asthma

Herpes simplex virus type 1 infection

Skin pigmentation

Type 2 diabetes mellitus

Hydroxyresveratrol (Oxyresveratrol) is a major active compound in the heartwood of Artocarpus lacucha. It was first isolated from the heartwood of Artocarpus lakoocha, and has also been found in various plants, including Smilax China, Morus alba, Var...

atrum nigrum, Scirpus maritinus, and Maclura pomifera. Oxyresveratrol, an aglycone of mulberroside A, has been produced by microbial biotransformation or enzymatic hydrolysis of a glycosylated stilbene mulberroside A, which is one of the major compounds of the roots of M. alba. Oxyresveratrol plays an important role in anti-tyrosinase, antioxidant, anti-inflammatory, antiviral and neuroprotective properties. There are many A. lacucha commercial products available on the market for skin whitening and anti-aging effects. OxyResvenox™ is the registered trademark of Oxyresveratrol from Sabinsa. Oxyresveratrol is an analog of Resveratrol and is of synthetic origin. The hydroxystilbene compounds including oxyresveratrol and resveratrol showed the potent inhibitory effect on tyrosinase activity. Oxyresveratrol is also naturally present in Morus alba L., Morus bombycis. Oxyresveratrol exhibits a potent inhibitory effect on dopa oxidase activity of tyrosinase which catalyzes rate-limiting steps of melanin biosynthesis. Oxyresveratrol showed superoxide scavenging effects with the IC50 values 3.81 ± 0.5 uM, Oxyresveratrol exhibited a DPPH free radical scavenging effect (IC50 = 23.4 ± 1.5 uM). Oxyresveratrol also showed hepatoprotective effects with EC50 values 32.3 ± 2.62 uM, on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. Oxyresveratrol significantly inhibited LPS-evoked nuclear translocation of NF-kappaB and cyclooxygenase-2 (COX-2) activity in RAW 264.7 cells. The results suggest that the anti-inflammatory properties of oxyresveratrol might be correlated with inhibition of the iNOS expression through down-regulation of NF-kappaB binding activity and significant inhibition of COX-2 activity. Oxyresveratrol revealed a dose-dependent neuroprotective effect in an in vivo stroke model. This may prove to be beneficial for a therapeutic strategy to limit brain injury in acute brain ischemia.

BROMOCHLOROSALICYLANILIDE

6GK715PWMQ

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Microsporum gypseum

Trichophyton rubrum

Trichophyton mentagrophytes

Conditions:

Bromochlorosalicylanilide (Multifungin) is a bromsalan antifungal that has been applied topically. It may cause allergic contact dermatitis in some individuals.

ECONAZOLE SULFOSALICYLATE

JCB50IOD4Y

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Status:

US Approved Rx (2002)

First approved in 1982

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Cytochrome P450 51

Trichophyton rubrum

Conditions:

Econazole (commonly used as the nitrate salt) is an antifungal medication of the imidazole class. It is a broad spectrum antimycotic with some action against Gram positive bacteria. It is used topically in dermatomycoses also orally and parenterally....

Sold under the brand name Ecoza among others, it is indicated for the treatment of interdigital tinea pedis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum in patients 12 years of age and older. Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

ECONAZOLE NITRATE

H438WYN10E

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Status:

US Approved Rx (2002)

First approved in 1982

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Cytochrome P450 51

Trichophyton rubrum

Conditions:

Econazole (commonly used as the nitrate salt) is an antifungal medication of the imidazole class. It is a broad spectrum antimycotic with some action against Gram positive bacteria. It is used topically in dermatomycoses also orally and parenterally....

Sold under the brand name Ecoza among others, it is indicated for the treatment of interdigital tinea pedis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum in patients 12 years of age and older. Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

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