CLIMBAZOLE (KLMBAZOL)
CLIMBAZOLE (KLMBAZOL)
CAS No. : 38083-17-9
EC No. : 253-775-4
Synonyms:
Climbazole; 38083-17-9; Climbazol; Baypival; Baysan; BAY-E 6975; 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethylbutan-2-one; Climbazol [INN-Spanish]; Climbazolum [INN-Latin]; 2-Butanone, 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-; 1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one; EINECS 253-775-4; BRN 0618020; CHEBI:83719; 1-(4-Clorophenoxy)-3,3-dimethyl-1-(imidazole-1-yl)-2-butanone; NCGC00166153-01; AK161858; 1-(4-Chlorophenoxy)-1-(imidazol-1-yl)-3,3-dimethylbutanone; 1-(p-Chlorophenoxy)-1-imidazol-1-yl-3,3-dimethyl-2-butanone; 1-(p-Chlorophenoxy)-3,3-dimethyl-1-(1-imidazolyl)-2-butanone; 1-(4-Chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-2-butanone; DSSTox_CID_26555; DSSTox_RID_81715; DSSTox_GSID_46555; AO-295/40848554; Q-100974; Climbazolum; 1-(4-Chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-2-butanone [ACD/IUPAC Name]; 1-(4-Chlorophénoxy)-1-(1H-imidazol-1-yl)-3,3-diméthyl-2-butanone [French] [ACD/IUPAC Name]; 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethylbutan-2-one; 1-(4-Chlorophenoxy)-1-(imidazol-1-yl)-3,3-dimethylbutan-2-one; 1-(4-Chlorphenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-2-butanon [German] [ACD/IUPAC Name]; 1-(4-Chlorphenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethylbutan-2-on; 253-775-4 [EINECS]; 2-Butanone, 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl- [ACD/Index Name]; 38083-17-9 [RN]; 4374; 618020; 9N42CW7I54; Climbazole [BAN] [INN] [Wiki]; CLIMBAZOLE, (R)-; CLIMBAZOLE, (S)-; Climbazolum [Latin] [INN]; EL7085000; MFCD00055505 [MDL number]; UNII:9N42CW7I54; (±)-Climbazole; (±)-Climbazole; [38083-17-9]; 1-(4-Chlorophenoxy)-1-(1H-imidazolyl)-3,3-dimethyl-2-butanone; 1-(4-Chlorophenoxy)-1-(imidazol-1-yl)-3,3-dimethyl-2-butanone; 1-(4-Chlorophenoxy)-1-(imidazol-1-yl)-3,3-dimethylbutanone; 1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one; 1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethyl-butan-2-one; 1-(4-chlorophenoxy)-1-imidazolyl-3,3-dimethylbutan-2-one; 1-(4-Chlorophenoxy)-3,3-dimethyl-1-(imidazole-1-yl)-2-butanone; 1-(4-clorophenoxy)-3,3-dimethyl-1-(IMIDAZOLE-1-yl)-2-butanone; 1-(p-Chlorophenoxy)-1-imidazol-1-yl-3,3-dimethyl-2-butanone; 1-(p-Chlorophenoxy)-3,3-dimethyl-1-(1-imidazolyl)-2-butanone; 1185117-79-6 [RN]; 2-Butanone, 1-(p-chlorophenoxy)-3,3-dimethyl-1-(1-imidazolyl)-; BAY e-6975; BAY-E 6975; BAY-e 6975;Baypival; Baypival; BAYSAN [Wiki]; Climbazol; Climbazol 10 ?g/mL in Cyclohexane; Climbazol 10 µg/mL in Cyclohexane; Climbazol 10 �g/mL in Cyclohexane; Climbazole 10 µg/mL in Cyclohexane; Climbazole 10 �g/mL in Cyclohexane; CLIMBAZOLE-D4; climbazolum; KS-5112; Pharmakon1600-01504833; QA-2612; TL8002789; климбазол; 1-(4-Chlorophenoxy)-1-(1H-imidazolyl)-3,3-dimethyl-2-butanone; 1-(4-Chlorophenoxy)-1-(imidazol-1-yl)-3,3-dimethylbutan-2-one; 1-(4-Chlorophenoxy)-1-(imidazol-1-yl)-3,3-dimethylbutanone; 1-(p-Chlorophenoxy)-3,3-dimethyl-1-(1-imidazolyl)-2-butanone; 2-Butanone, 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-; 2-Butanone, 1-(p-chlorophenoxy)-3,3-dimethyl-1-(1-imidazolyl)-; BAY-E 6975; Baypival; (R,S)-1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one; (RS)-1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one; 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-2-butanone; 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethylbutan-2-one; 1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one; 1-(4-chlorophenoxy)-3,3-dimethyl-1-(imidazole-1-yl)-2-butanone; 2-Butanone, 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethyl-; Climbazole; climbazole; Crinipan AD
EN
Climbazole IUPAC Name 1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one
Climbazole InChI 1S/C15H17ClN2O2/c1-15(2,3)13(19)14(18-9-8-17-10-18)20-12-6-4-11(16)5-7-12/h4-10,14H,1-3H3
Climbazole InChI Key OWEGWHBOCFMBLP-UHFFFAOYSA-N
Climbazole Canonical SMILES CC(C)(C)C(=O)C(N1C=CN=C1)OC2=CC=C(C=C2)Cl
Climbazole Molecular Formula C15H17ClN2O2
Climbazole CAS 38083-17-9
Climbazole European Community (EC) Number 253-775-4
Climbazole NSC Number 759808
Climbazole DSSTox Substance ID DTXSID6046555
Climbazole Appearance White crystalline powder
Climbazole Purity ≥99%
Climbazole Melting Point 96-98℃
Climbazole P-Chlorophenol ≤0.015%
Climbazole Chloride ≤0.1%
Climbazole Water ≤0.5%
Climbazole Molecular Weight 292.76 g/mol
Climbazole XLogP3-AA 3.7
Climbazole Hydrogen Bond Donor Count 0
Climbazole Hydrogen Bond Acceptor Count 3
Climbazole Rotatable Bond Count 5
Climbazole Exact Mass 292.097855 g/mol
Climbazole Monoisotopic Mass 292.097855 g/mol
Climbazole Topological Polar Surface Area 44.1 Ų
Climbazole Heavy Atom Count 20
Climbazole Formal Charge 0
Climbazole Complexity 335
Climbazole Isotope Atom Count 0
Climbazole Defined Atom Stereocenter Count 0
Climbazole Undefined Atom Stereocenter Count 1
Climbazole Defined Bond Stereocenter Count 0
Climbazole Undefined Bond Stereocenter Count 0
Climbazole Covalently-Bonded Unit Count 1
Climbazole Compound Is Canonicalized Yes
Climbazole is a topical antifungal agent commonly used in the treatment of human fungal skin infections such as dandruff[2] and eczema. Climbazole has shown a high in vitro and in vivo efficacy against Malassezia spp. that appear to play an important role in the pathogenesis of dandruff.[2] Its chemical structure and properties are similar to other fungicides such as ketoconazole and miconazole.It is most commonly found as an active ingredient in OTC anti-dandruff and anti-fungal products, including shampoos, lotions and conditioners. It may be accompanied by other active ingredients such as zinc pyrithione or triclosan.May cause localized irritation of the skin with symptoms including redness, rashes and itching.Climbazole is white or off-white crystal or crystalline powder. It is easily soluble in alcohol, but hardly soluble in water. It has broad-spectrum bactericidal properties. It is mainly used in anti-itch and anti-dandruff conditioning shampoos and hair care shampoos, and can also be used in high-end detergents such as antibacterial soap, shower gel, medical toothpaste, mouthwash and other high-end detergents.It is mainly used for anti-itching and anti-dandruff conditioning shampoos, hair care shampoos, and also used for antibacterial soaps, shower gels, medical toothpastes, mouthwashes, etc.Dandruff is a common condition, affecting up to half the global population of immunocompetent adults at some time during their lives and it has been highly correlated with the over-expression of the fungus Malassezia spp. Climbazole (CBZ) is used as an antifungal and preservative agent in many marketed formulations for the treatment of dandruff. While the efficacy of Climbazole in vitro and in vivo has previously been reported, limited information has been published about the uptake and deposition of Climbazole in the skin. Hence, our aim was to investigate the skin permeation of Climbazole as well as the influence of various solvents on Climbazole skin delivery. Four solvents were selected for the permeability studies of Climbazole, namely propylene glycol (PG), octyl salicylate (OSal), Transcutol® P (TC) and polyethylene glycol 200 (PEG). The criteria for selection were based on their wide use as excipients in commercial formulations, their potential to act as skin penetration enhancers and their favourable safety profiles. 1% (w/v) solutions of Climbazole were applied under infinite and finite dose conditions using Franz type diffusion cells to human and porcine skin. In line with the topical use of Climbazole as an antidandruff agent, comparatively low amounts of Climbazole penetrated across the skin barrier (<1% of the applied dose of Climbazole). Finite dose studies resulted in a higher extraction of Climbazole from human skin compared with infinite dose studies (p < 0.05). Climbazole was also taken up to a higher extent in porcine skin (>7-fold) compared with human skin (p < 0.05). Nevertheless, no statistical differences were observed in the amounts that permeated across the different membranes. These preliminary results confirm the potential of simple formulations of Climbazole to target the outer layers of the epidermis. The PG and OSal formulations appear to be promising vehicles for Climbazole in terms of overall skin extraction and penetration. Future work will expand the range of vehicles studied and explore the reasons underlying the retention of Climbazole in the outer layers of the skin.Climbazole (CBZ) is an imidazole antifungal agent used to manage dandruff in formulations such as shampoos or conditioners and as a preservative (Fig. 1). It has a molecular weight of 292.8 g mol−1 and a reported melting point of 95–97 °C and it acts by inhibiting the synthesis of ergosterol, a major component in fungal plasma membranes (SCCP, 2009). In addition, CBZ has been shown to upregulate keratinocyte differentiation promoting the expression of small-proline-rich proteins in primary keratinocytes (Pople et al., 2014). Bhogal et al. (2014) also reported inhibitory effects of CBZ on hair proteases involved in anchorage of the hair shaft in an in vitro study.Climbazole is a topical antifungal agent commonly used in the treatment of human fungal skin infections such as dandruff[2] and eczema. Climbazole is an antimycotic agent with a high in vitro and in vivo efficacy against P. ovale. After a 1-week washout and a 4-week treatment the clinical evaluation showed a successful reduction of dandruff under the Climbazole 0.65% shampoo, skin redness and itching in 80% of the volunteers and a mild improvement in 20% of the volunteers. The cosmetic acceptability was very good by the majority. It is concluded that the formulation tested is effective in the treatment of moderate to severe dandruff. It is most commonly found as an active ingredient in OTC anti-dandruff and anti-fungal products, including shampoos, lotions and conditioners. May cause localized irritation of the skin with symptoms including redness, rashes and itching.Cosmetic industry shall pay attention to the new limit of Climbazole and its intended function in cosmetic product. Reducing the usage level of Climbazole may be necessary.The cosmetic ingredient Climbazole (CAS 38083-17-9), with the chemical name 1-(4-chlorophenoxy)-1-imidazol-1-yl-3,3-dimethyl-2-butanone, is currently regulated in the Cosmetics Regulation (EC) 1223/2009 as a preservative in Annex V, entry 32, up to a maximum authorized concentration of 0.5%.In particular, in the opinions of 2009 and later in 2013, the experts assessed the combined use of Climbazole in different cosmetic product categories as preservative at concentration up to 0.5% in leave-on cosmetics and as anti-dandruff agent in rinse-off hair products up to a maximum concentration of 2%. Margin of Safety (MoS) values were calculated for each product type and then combined to assess the safety of Climbazole for use in different product types (i.e. shampoo, hair lotion, face cream, foot care).The previous results of an old Draize eye test and a combination of two newly carried out in vitro screening tests for eye irritation (HET-CAM and CEET) suggest that Climbazole is not an eye irritant. Its potential to cause skin irritation is assessed through a human single patch test and shows only mild to no skin irritation. Considering the results of the above studies and considering the dilution of the compound in its intended use, there appears to be no reason to suspect any irritation problems with the use of Climbazole in cosmetic products. As far as sensitising potential is concerned, a well-performed LLNA shows Climbazole to be non-sensitising in the performed mice assay.Climbazole showed to be negative in an Ames test, in an in vitro micronucleus test and in an in vitro mammalian cell gene mutation test (with the exception of the prolonged exposure scheme, where some mutagenic potential became apparent). An in vivo micronucleus test and an in vivo UDS assay with Climbazole showed the substance to be negative, meaning that no mutagenic/genotoxic effects are to be expected.Climbazole was tested in a 1-generation reproductive toxicity test which was considered questionable as far as its overall scientific validity is concerned. Also, a well-performed teratogenicity study was present, leading to a NOAEL (embryotoxicity) of 30 mg/kg bw/day and a NOAEL (maternal toxicity) of 15 mg/kg bw/day.An oral bioavailability assay of 14C Climbazole in mice confirmed the results that were described earlier, namely that Climbazole is rapidly absorbed and excreted and that its maximum concentration in plasma is reached after approximately 8 hours. These data were published by Pérez-Rivera et al.(2009).Climbazole has shown a high in vitro and in vivo efficacy against Pityrosporum ovale that appears to play an important role in the pathogenesis of dandruff. Its chemical structure and properties are similar to other fungicides such as ketoconazole and miconazole. For Climbazole, the range of MICs is between < 0.06 and 1 μg/mL with an empirical median of 0.06 μg/mL. Climbazole is not mutagenic in the Salmonella typhimurium or Escherichia coli Ames assay and does not induce micronuclei in human lymphocytes. An in vivo mouse micronucleus test also shows it is non-mutagenic up to a maximum tolerated dose (MTD) of 150 mg/kg administered orally. In the in vivo/in vitro unscheduled DNA synthesis assay, Climbazole shows no evidence of DNA damage in the livers of rats at doses up to the MTD of 200 mg/kg orally. A toxicokinetic study is performed in mice with oral administration of [14C]-Climbazole (150 mg/kg). Radioactivity (20.42 μg-equiv./g plasma) is detected 15 min after oral administration of [14C]-Climbazole, and the peak concentration is 62.96 μg-equiv./g plasma at 8 h after dosing.Pityrosporum ovale appears to play an important role in the pathogenesis of dandruff as a symptom of seborrheic dermatitis. Climbazole is an antimycotic agent with a high in vitro and in vivo efficacy against P. ovale. In the presented work we investigated the efficacy and safety of a Climbazole 0.65% shampoo on seborrheic dermatitis of 30 volunteers. Subjects were diagnosed as having moderate to severe seborrheic dermatitis of the scalp. After a 1-week washout and a 4-week treatment the clinical evaluation showed a successful reduction of dandruff, skin redness and itching in 80% of the volunteers and a mild improvement in 20% of the volunteers. The cosmetic acceptability was very good by the majority. It is concluded that the formulation tested is effective in the treatment of moderate to severe dandruff.Emerging pollutants such as personal care products can reach the environment via effluents of wastewater treatment plants (WWTP) and digested sludge. Only recently, the anti-dandruff agent and antimycotic Climbazole was detected for the first time in a WWTP effluent with concentrations up to 0.5 µg/L. Despite its mode of action as C14-demethylase inhibitor (DMI) fungicide and thus its high efficacy against fungi, knowledge on its potential environmental impact is lacking. Therefore, the aim of this work is to characterise Climbazole’s ecotoxicity by conducting standard biotests with organisms representing different trophic levels from the aquatic as well as the terrestrial compartment. It was found that the toxicity of Climbazole is mostly similar to that of other DMI fungicides, while it proved to be particularly toxic towards primary producers. The lowest median effect concentrations (EC50) were determined for Lemna minor with 0.013 mg/L (biomass yield) and for Avena sativa with 18.5 mg/kg(-) soil dry weight (d.w.) (shoot biomass). Reduction of frond size in water lentils and shootlength in higher plants suggested an additional, plant growth retarding mode of action of Climbazole. In addition, it was demonstrated here that for an ionisable compound such as Climbazole, the soil pH can have a considerable influence on phytotoxicity. Environ Toxicol Chem © 2013 SETAC.
TR
Klimbazol IUPAC sim 1- (4-klorofenoksi) -1-imidazol-1-il-3,3-dimetilbutan-2-on
Klimbazol InChI 1S / C15H17ClN2O2 / c1-15 (2,3) 13 (19) 14 (18-9-8-17-10-18) 20-12-6-4-11 (16) 5-7 -12 / h4-10,14H, 1-3H3
Klimbazol InChI Anahtar OWEGWHBOCFMBLP-UHFFFAOYSA-N
Klimbazol Kanonik SMILES CC (C) (C) C (= O) C (N1C = CN = C1) OC2 = CC = C (C = C2) Cl
Klimbazol Moleküler Formül C15H17ClN2O2
Klimbazol CAS 38083-17-9
Klimbazol Avrupa Topluluu (EC) Numaras 253-775-4
Klimbazol NSC Numaras 759808
Klimbazol DSSTox Madde Kimlii DTXSID6046555
Klimbazol Görünüm Beyaz kristal toz
Klimbazol Saflk ≥% 99
Klimbazol Erime Noktas 96-98 ℃
Klimbazol P-Chlorophenol ≤0.015%
Klimbazol Klorür ≤% 0,1
Klimbazol Su ≤% 0,5
Klimbazol Moleküler Arlk 292.76 g / mol
Klimbazol XLogP3-AA 3,7
Klimbazol Hydrogen Bond Donör Says 0
Klimbazol Hidrojen Ba Alcs Says 3
Klimbazol Dönebilen Bond Says 5
Klimbazol Tam Kütle 292.097855 g / mol
Klimbazol Monoisotopik Kütle 292.097855 g / mol
Klimbazol Topolojik Polar Yüzey Alan 44.1 Ų
Klimbazol Ar Atom Says 20
Klimbazol Resmi arj 0
Klimbazol Karmaklk 335
Klimbazol zotop Atom Says 0
Klimbazol Tanml Atom Stereocenter Says 0
Klimbazol Tanmsz Atom Stereocenter Says 1
Klimbazol Tanml Bond Stereocenter Says 0
Klimbazol Tanmsz Bond Stereocenter Says 0
Klimbazol Kovalent Bal Birim Says 1
Klimbazol Bileii Kanonikalize Edilmitir Evet
Klimbazol, kepek [2] ve egzama gibi insan mantar deri enfeksiyonlarnn tedavisinde yaygn olarak kullanlan topikal bir antifungal ajandr. Klimbazol, Malassezia spp’ye kar yüksek in vitro ve in vivo etkinlik göstermitir. kepek patogenezinde önemli bir rol oynad görülmektedir. [2] Kimyasal yaps ve özellikleri ketokonazol ve mikonazol gibi dier fungisitlere benzer.Çounlukla OTC kepek önleyici ve ampuanlar, losyonlar ve saç kremleri dahil mantar önleyici ürünlerde aktif bir bileen olarak bulunur. Çinko pirition veya triklosan gibi dier aktif maddeler elik edebilir. Kzarklk, kzarklk ve kant gibi semptomlarla deride lokal tahrie neden olabilir. Alkolde kolayca çözünür, ancak suda hemen hemen hiç çözünmez. Geni spektrumlu bakteri yok edici özelliklere sahiptir. Esas olarak kant önleyici ve kepek önleyici ampuanlarda ve saç bakm ampuanlarnda kullanlr ve ayrca antibakteriyel sabun, du jeli, medikal di macunu, gargara ve dier üst düzey deterjanlar gibi üst düzey deterjanlarda da kullanlabilir. esas olarak kant önleyici ve kepek önleyici ampuanlar, saç bakm ampuanlar için kullanlr ve ayrca antibakteriyel sabunlar, du jelleri, tbbi di macunlar, az gargaralar, vb. için kullanlr. yaamlarnn bir döneminde ve bu, Malassezia spp. mantarnn ar ekspresyonu ile yüksek oranda ilikilendirilmitir. Klimbazol (CBZ), kepek tedavisi için pazarlanan birçok formülasyonda antifungal ve koruyucu ajan olarak kullanlmaktadr. Klimbazol ‘un in vitro ve in vivo etkinlii daha önce bildirilirken, Klimbazol’ un ciltte alm ve birikmesi hakknda snrl bilgi yaynlanmtr. Bu nedenle amacmz, Klimbazol ‘un deri geçiini ve çeitli çözücülerin Klimbazol deri verimi üzerindeki etkisini aratrmakt. Klimbazol geçirgenlik çalmalar için propilen glikol (PG), oktil salisilat (OSal), Transcutol® P (TC) ve polietilen glikol 200 (PEG) olmak üzere dört çözücü seçildi. Seçim kriterleri, ticari formülasyonlarda eksipiyan olarak geni kullanmlarna, deriye nüfuz etmeyi artrc olarak etki etme potansiyellerine ve uygun güvenlik profillerine dayanyordu. Klimbazol ‘ün% 1 (w / v) çözeltileri, Franz tipi difüzyon hücreleri kullanlarak sonsuz ve sonlu doz koullar altnda insan ve domuz derisine uyguland. Bir kepek önleyici ajan olarak Klimbazol ‘un topikal kullanmna paralel olarak, nispeten düük miktarlarda Klimbazol cilt bariyerini amtr (uygulanan Klimbazol dozunun <% 1’i). Sonlu doz çalmalar, sonsuz doz çalmalarna kyasla insan derisinden daha yüksek bir Klimbazol ekstraksiyonu ile sonuçland (p <0.05). Klimbazol da insan derisine göre domuz derisinde (> 7 kat) daha yüksek oranda alnd (p <0.05). Bununla birlikte, bana düen miktarlarda istatistiksel bir farkllk gözlenmemitir.farkl zarlar boyunca etli. Bu ön sonuçlar, Klimbazol basit formülasyonlarnn epidermisin d katmanlarn hedefleme potansiyelini dorulamaktadr. PG ve OSal formülasyonlar, genel cilt çkarma ve penetrasyon açsndan Klimbazol için umut verici araçlar gibi görünmektedir. Gelecekteki çalmalar, incelenen araçlarn yelpazesini geniletecek ve cildin d katmanlarnda Klimbazol tutulmasnn altnda yatan nedenleri aratracaktr.Klimbazol (CBZ), ampuanlar gibi formülasyonlarda kepei yönetmek için kullanlan bir imidazol antifungal ajandr. veya saç kremleri ve koruyucu olarak (ekil 1). Moleküler arl 292.8 gmol − 1 ve bildirilen erime noktas 95-97 ° C’dir ve fungal plazma membranlarnda önemli bir bileen olan ergosterolün sentezini inhibe ederek etki eder (SCCP, 2009). Ek olarak, CBZ’nin, birincil keratinositlerde küçük prolin bakmndan zengin proteinlerin ekspresyonunu tevik ederek keratinosit farkllamasn yukar düzenledii gösterilmitir (Pople ve dierleri, 2014). Bhogal vd. (2014) ayrca bir in vitro çalmada, CBZ’nin saç aftnn ankrajnda yer alan saç proteazlar üzerindeki inhibe edici etkilerini bildirmitir.Klimbazol, kepek gibi insan mantar deri enfeksiyonlarnn tedavisinde yaygn olarak kullanlan topikal bir antifungal ajandr [2] ve egzama. Klimbazol, P. ovale’ye kar yüksek in vitro ve in vivo etkinlie sahip bir antimikotik ajandr. 1 haftalk arnma ve 4 haftalk bir tedaviden sonra klinik deerlendirme, Klimbazol ampuan altnda% 0,65 kepek azalmas, gönüllülerin% 80’inde cilt kzarkl ve kant ve% 20’sinde hafif bir iyileme gösterdi. gönüllüler. Kozmetik kabul edilebilirlik çounluk tarafndan çok iyiydi. Test edilen formülasyonun orta ila iddetli kepek tedavisinde etkili olduu sonucuna varlmtr. ampuanlar, losyonlar ve saç kremleri dahil olmak üzere en yaygn olarak OTC kepek önleyici ve mantar önleyici ürünlerde aktif bir bileen olarak bulunur. Ciltte kzarklk, kzarklk ve kant gibi semptomlarla lokalize tahrie neden olabilir. Kozmetik endüstrisi Klimbazol ‘ün yeni snrna ve kozmetik üründe amaçlanan ilevine dikkat edecektir. Klimbazol kullanm seviyesinin azaltlmas gerekli olabilir. Kozmetik içerii Klimbazol (CAS 38083-17-9), kimyasal ad 1- (4-klorofenoksi) -1-imidazol-1-yl-3 , 3-dimetil-2-butanon, u anda Kozmetik Yönetmelii (EC) 1223/2009’da Ek V, giri 32’de bir koruyucu olarak, maksimum% 0,5’lik bir izin verilen konsantrasyona kadar düzenlenmektedir. 2009’un görülerinde özellikle ve daha sonra 2013 ylnda uzmanlar, Climbazole’un (Klimbazol) farkl kozmetik ürün kategorilerindeki kombine kullanmn, braklan kozmetiklerde% 0,5’e varan konsantrasyonda koruyucu olarak ve maksimuma kadar durulanan saç ürünlerinde kepek önleyici madde olarak deerlendirdiler. % 2’lik konsantrasyon. Her ürün türü için Güvenlik Marj (MoS) deerleri hesapland ve ardndan farkl ürün türlerinde (yani ampuan, saç losyonu, yüz kremi, ayak bakm) kullanm için Klimbazol güvenliini deerlendirmek için birletirildi. eski Draize göz testi ve göz tahrii için yeni yaplan iki in vitro tarama testinin bir kombinasyonu (HET-CAM ve CEET), Climbazole’un (Klimbazol) gözü tahri edici olmadn göstermektedir. Cilt tahriine neden olma potansiyeli, bir insan tek yama testi ile deerlendirilir ve sadece hafif veya hiç cilt tahrii göstermez. Yukardaki çalmalarn sonuçlar göz önüne alndnda ve amaçlanan kullanmda bileiin seyreltilmesi göz önüne alndnda, kozmetik ürünlerde Klimbazol kullanmyla herhangi bir tahri probleminden üphelenmek için hiçbir neden yok gibi görünmektedir. Hassaslatrma potansiyeli söz konusu olduunda, iyi performans gösteren bir LLNA, Climbazole’un (Klimbazol) gerçekletirilen fare testinde hassaslatrc olmadn gösterir.Climbazol (Klimbazol), bir Ames testinde, bir in vitro mikronükleus testinde ve bir in vitro memeli hücresi gen mutasyon testi (baz mutajenik potansiyelin belirgin hale geldii uzun süreli maruz kalma emas hariç). Bir in vivo mikronükleus testi ve Klimbazol ile bir in vivo UDS testi, maddenin negatif olduunu gösterdi, bu da mutajenik / genotoksik etkilerin beklenmeyecei anlamna gelir.Climbazol (Klimbazol), 1 nesil üreme toksisitesi testinde test edilmitir. genel bilimsel geçerlilii söz konusu olduunda üpheli kabul edildi. Ayrca, 30 mg / kg vücut arl / gün NOAEL (embriyotoksisite) ve 15 mg / kg vücut arl / gün NOAEL’e (maternal toksisite) yol açan iyi uygulanm bir teratojenite çalmas mevcuttu. Klimbazol), daha önce açklanan sonuçlar, yani Climbazole’un (Klimbazol) hzla emildiini ve atldn ve plazmadaki maksimum konsantrasyonuna yaklak 8 saat sonra ulaldn dorulad. Bu veriler, Pérez-Rivera ve dierleri (2009) tarafndan yaynland.Klimbazol, yüksek in vitro ve in vivo ekepek patogenezinde önemli bir rol oynad görülen Pityrosporum ovale’ye kar etkililik. Kimyasal yaps ve özellikleri, ketokonazol ve mikonazol gibi dier fungisitlere benzer. Klimbazol için, MIC aral <0,06 ile 1 μg / mL arasndadr ve ampirik medyan 0,06 μg / mL’dir. Klimbazol, Salmonella typhimurium veya Escherichia coli Ames testinde mutajenik deildir ve insan lenfositlerinde mikronükleileri indüklemez. Bir in vivo fare mikronükleus testi ayrca oral yoldan uygulanan 150 mg / kg maksimum tolere edilen doza (MTD) kadar mutajenik olmadn gösterir. In vivo / in vitro planlanmam DNA sentezi deneyinde Klimbazol, oral yoldan 200 mg / kg MTD’ye kadar olan dozlarda sçanlarn karacierlerinde DNA hasar kant göstermez. [14C] -Klimbazol (150 mg / kg) oral uygulamasyla farelerde toksikokinetik bir çalma yaplmtr. Radyoaktivite (20.42 μg-edeeri / g plazma), [14C] -Climbazol (Klimbazol) ‘un oral uygulamasndan 15 dakika sonra tespit edilir ve dozlamadan 8 saat sonra tepe konsantrasyon 62.96 μg-edeeri / g plazma’dr. seboreik dermatitin bir semptomu olarak kepek patogenezinde önemli bir rol oynamak. Klimbazol, P. ovale’ye kar yüksek in vitro ve in vivo etkinlie sahip bir antimikotik ajandr. Sunulan çalmada, 30 gönüllünün seboreik dermatiti üzerindeki Klimbazol% 0.65 ampuannn etkililiini ve güvenliini aratrdk. Deneklere kafa derisinde orta ila iddetli seboreik dermatit tehisi kondu. 1 haftalk bir arnma ve 4 haftalk bir tedaviden sonra klinik deerlendirme, gönüllülerin% 80’inde kepek, cilt kzarkl ve kantda baarl bir azalma ve gönüllülerin% 20’sinde hafif bir iyileme gösterdi. Kozmetik kabul edilebilirlik çounluk tarafndan çok iyiydi. Test edilen formülasyonun orta ve iddetli kepek tedavisinde etkili olduu sonucuna varlmtr.Kiisel bakm ürünleri gibi ortaya çkan kirleticiler, atk su artma tesisleri (AAT) ve çürütülmü çamurlardan çevreye ulaabilmektedir. Ksa bir süre önce, kepek önleyici ajan ve antimikotik Klimbazol, 0,5 µg / L’ye varan konsantrasyonlarda bir AAT atk suyunda ilk kez tespit edildi. C14-demetilaz inhibitörü (DMI) fungisit olarak etki ekline ve dolaysyla mantarlara kar yüksek etkinliine ramen, potansiyel çevresel etkisine ilikin bilgi eksiktir. Bu nedenle, bu çalmann amac, hem sucul hem de karasal kompartmandan farkl trofik seviyeleri temsil eden organizmalarla standart biyotestler gerçekletirerek Klimbazol ‘un ekotoksisitesini karakterize etmektir. Climbazole’un (Klimbazol) toksisitesinin çounlukla dier DMI fungisitlerininkine benzer olduu, ancak birincil üreticilere kar özellikle toksik olduu kantlanmtr. En düük medyan etki konsantrasyonlar (EC50), 0.013 mg / L (biyokütle verimi) ile Lemna minör için ve 18.5 mg / kg (-) toprak kuru arl (d.w.) (sürgün biyokütlesi) ile Avena sativa için belirlenmitir. Su mercimeklerinde yaprak boyutunun ve daha yüksek bitkilerde sürgün uzunluunun azaltlmas, Climbazole’un (Klimbazol) ek, bitki büyümesini geciktirici bir etki modu önerdi. Ek olarak, burada Klimbazol gibi iyonize edilebilir bir bileik için toprak pH’snn fitotoksisite üzerinde önemli bir etkiye sahip olabilecei gösterilmitir. Environ Toxicol Chem © 2013 SETAC.