ENILCONAZOLE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C14H14Cl2N2O
Molecular Weight	297.18
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

ClC1=CC(Cl)=C(C=C1)C(CN2C=CN=C2)OCC=C

InChI

InChIKey=PZBPKYOVPCNPJY-UHFFFAOYSA-N

InChI=1S/C14H14Cl2N2O/c1-2-7-19-14(9-18-6-5-17-10-18)12-4-3-11(15)8-13(12)16/h2-6,8,10,14H,1,7,9H2

HIDE SMILES / InChI

Molecular Formula	C14H14Cl2N2O
Molecular Weight	297.18
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Enilconazole is a synthetic broad-spectrum antimycotic with a high activity against most of the common dermatophytes and various other fungi and yeasts. It is a selective inhibitor of ergosterol biosynthesis, an essential component of the cell membrane of fungi and yeasts. This results in irreversible changes which are the origin of the fungicidal effect. Enilconazole is marketed under the brand name Imaverol among others. Imaverol concentrated solution is a synthetic antimycotic with a potent antifungal action against dermatophytes such as: Trichophyton verrucosum, Trichophyton mentagrophytes, Trichophyton equinum, and Microsporum canis in horses and dogs.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cytochrome P450 3A4 127	Inhibitor 8,297
Cytochrome P450, fungi 3	Inhibitor 8,297
Cytochrome P450 1A1 31	Activator 1,430
Nuclear receptor subfamily 1 group I member 2 8	Agonist 2,678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Dermatomycosis 20	Curative		Approved 8,429	IMAVEROL

PubMed

Show entries

Title	Date	PubMed
Screening of selected pesticides for inhibition of CYP19 aromatase activity in vitro.	2000 Jun	10806373
Evaluation of topically applied enilconazole for the treatment of dermatophytosis in a Persian cattery.	2002 Feb	11896967
Evaluation of the efficacy of oral lufenuron combined with topical enilconazole for the management of dermatophytosis in catteries.	2002 Jun 8	12081306
Intranasal infusion of enilconazole for treatment of sinonasal aspergillosis in dogs.	2002 Nov 15	12458610
Use of computed tomography to predict the outcome of a noninvasive intranasal infusion in dogs with nasal aspergillosis.	2003 Apr	12715982

Showing 1 to 5 of 43 entries

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Patents

Sample Use Guides

In Vivo Use Guide

The concentrated Imaverol (Enilconazole) is diluted in 50 parts of lukewarm water, which yields a 0.2% emulsion. Dispose of all unused diluted solutions. Dermatophytes will extend into the hair follicles. Possible crusts must therefore be removed with a hard brush, which has been soaked in the diluted IMAVEROL emulsion. It is highly recommended that the animal be sprayed entirely at the first treatment so as to reach the subclinical lesions as well. Horse: The lesions and surrounding skin are to be washed with the diluted emulsion 4 times at 3 to 4 day intervals. Dog: The animals are to be washed with the diluted emulsion 4 times at 3 to 4 day intervals. While doing this, one should rub thoroughly in the direction opposite to the hair growth to make sure that the skin is thoroughly wet. For the same reason, it is recommended to clip long-haired dogs prior to treatment.

Route of Administration: Topical

In Vitro Use Guide

A. niger strains were most susceptible to enilconazole. MIC ranged from 0.0625 to 0.5 ug/ml for enilconazole, with MIC90-0.5 ug/ml and MIC50-0.125 ug/ml.