トルシクラート
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/09/15 04:36:50」(JST)
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Tolciclate
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Clinical data |
AHFS/Drugs.com |
International Drug Names |
Identifiers |
CAS Number |
50838-36-3 Y |
ATC code |
D01AE19 (WHO) |
PubChem |
CID 5506 |
ChemSpider |
5305 N |
UNII |
T3TZ02X2AZ Y |
KEGG |
D01384 Y |
Chemical data |
Formula |
C20H21NOS |
Molar mass |
323.45 g/mol |
SMILES
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Cc1cccc(c1)N(C)C(=S)Oc2ccc3c(c2)C4CCC3C4
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InChI
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InChI=1S/C20H21NOS/c1-13-4-3-5-16(10-13)21(2)20(23)22-17-8-9-18-14-6-7-15(11-14)19(18)12-17/h3-5,8-10,12,14-15H,6-7,11H2,1-2H3 N
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Key:CANCCLAKQQHLNK-UHFFFAOYSA-N N
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NY (what is this?) (verify) |
Tolciclate is an antifungal.[1][2]
See also
References
- ^ Ryder, N. S.; Frank, I.; Dupont, M. C. (May 1986). "Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate". Antimicrobial Agents and Chemotherapy. 29 (5): 858–860. doi:10.1128/aac.29.5.858. PMC 284167. PMID 3524433.
- ^ Bianchi, A.; Monti, G.; de Carneri, I. (September 1977). "Tolciclate: further antimycotic studies". Antimicrobial Agents and Chemotherapy. 12 (3): 429–430. doi:10.1128/aac.12.3.429. PMC 429931. PMID 907333.
Antifungals (D01 and J02)
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Wall/
membrane |
Ergosterol
inhibitors |
Azoles
(lanosterol 14
alpha-demethylase inhibitors) |
Imidazoles |
- Topical: bifonazole‡
- butoconazole
- chlormidazole‡
- clotrimazole#
- croconazole‡
- econazole
- fenticonazole‡
- flutrimazole
- isoconazole‡
- ketoconazole
- luliconazole
- miconazole#
- neticonazole‡
- omoconazole‡
- oxiconazole
- sertaconazole
- sulconazole
- tioconazole
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|
Triazoles |
- Topical: efinaconazole
- fluconazole#
- fosfluconazole
- terconazole
- Systemic: fluconazole#
- hexaconazole‡
- isavuconazole
- itraconazole
- posaconazole
- voriconazole
- Unknown: albaconazole‡
- ravuconazole†
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Thiazoles |
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Polyene antimycotics
(ergosterol binding) |
- Topical: hamycin‡
- natamycin
- nystatin#
Systemic: amphotericin B#, hamycin‡
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Squalene monooxygenase
inhibitors |
Allylamines |
- Topical: naftifine
- terbinafine
Systemic: terbinafine
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Benzylamines |
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Others |
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β-glucan synthase
inhibitors |
- echinocandins (anidulafungin
- caspofungin
- micafungin)
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Intracellular |
Pyrimidine analogues/
thymidylate synthase inhibitors |
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Mitotic inhibitors |
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Aminoacyl tRNA synthetase inhibitors |
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Others |
- bromochlorosalicylanilide
- chlorophetanol
- chlorphenesin
- ciclopirox
- crystal violet
- dimazole
- ethylparaben
- haloprogin
- polynoxylin
- potassium iodide#
- salicylic acid
- selenium disulfide#
- sodium thiosulfate#
- sulbentine
- taurolidine
- ticlatone
- tolciclate
- tolnaftate
- tribromometacresol
- undecylenic acid
- Whitfield's ointment#
- citronella oil
- lemon grass
- lemon myrtle
- orange oil
- patchouli
- tea tree oil
- PCP: atovaquone
- dapsone
- pentamidine
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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English Journal
- Clinical Trichophyton rubrum strain exhibiting primary resistance to terbinafine.
- Mukherjee PK1, Leidich SD, Isham N, Leitner I, Ryder NS, Ghannoum MA.
- Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2003 Jan;47(1):82-6.
- The in vitro antifungal susceptibilities of six clinical Trichophyton rubrum isolates obtained sequentially from a single onychomycosis patient who failed oral terbinafine therapy (250 mg/day for 24 weeks) were determined by broth microdilution and macrodilution methodologies. Strain relatedness was
- PMID 12499173
- [Fungicidal activity of liranaftate against Trichophyton rubrum].
- Oku Y1, Sakuma K, Yokoyama K, Miyaji M.
- Nihon Ishinkin Gakkai zasshi = Japanese journal of medical mycology.Nihon Ishinkin Gakkai Zasshi.2002;43(3):181-7.
- The fungicidal activities of thiocarbamate antifungal agent liranaftate were studied by determining the MIC and the MCC against Trichophyton rubrum with the Milliflex -100 Test System and by determining the time-kill curve in comparison to that of six reference agents. Liranaftate and lanoconazole b
- PMID 12145634
- Characterization of squalene epoxidase activity from the dermatophyte Trichophyton rubrum and its inhibition by terbinafine and other antimycotic agents.
- Favre B1, Ryder NS.
- Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.1996 Feb;40(2):443-7.
- Squalene epoxidase (SE) is the primary target of the allylamine antimycotic agents terbinafine and naftifine and also of the thiocarbamates. Although all of these drugs are employed primarily in dermatological therapy, SE from dermatophyte fungi has not been previously investigated. We report here t
- PMID 8834895
Japanese Journal
- Trichophyton rubrumに対するliranaftateの殺菌活性
- 奥 幸夫,佐久間 慶太,横山 耕治,宮治 誠
- 日本医真菌学会雑誌 43(3), 181-187, 2002
- … 用9日目以降小さくなりはじめ, 作用14日目のMCC値は0.039μg/mlであった.TolciclateのMCC値も作用9日目以降小さくなったが, amorolfine, lanoconazole, neticonazole, clotrimazoleおよびbifonazoleのMCC値は作用14日目まで全く低下しなかった.この結果は発芽分生子に対しても大きな差が認められなかった.<BR>Time-killcurveの検討では, liranaftateおよびtolciclateは2~32×MICで作用7~9日目に生菌数が測定限界以下となった.Amorolfineは …
- NAID 130003672040
- モルモットの実験的白せんに対する新チオカルバミン酸系抗真菌剤Liranaftate(M‐732)の治療効果
- 井上 恒男,奥 幸夫,高瀬 宗章,横山 耕治,加治 晴夫,西村 和子,宮治 誠
- 日本医真菌学会雑誌 34(2), 193-197, 1993
- … piritetrate) クリーム剤の治療効果について対照薬剤に1% tolciclateクリームを用いて比較検討した結果, 以下の成績を得た.<BR>1%および2% liranaftateクリーム剤を菌接種3日目より感染部位に1日1回14日間連日塗布した結果, 症状の著しい改善と組織内の菌消滅効果を示した. …
- NAID 130003671710
- 新チオカルバミン酸系抗真菌剤Liranaftate(M‐732)のin vitro抗菌活性
- 奥 幸夫,井上 恒男,高瀬 宗章,横山 耕治,加治 晴夫,西村 和子,宮治 誠
- 日本医真菌学会雑誌 34(2), 185-192, 1993
- … piritetrate) の外用抗真菌剤としての有用性を評価する前提として, 諸種病原真菌, <I>Nocardia</I>属その他の細菌に対する<I>in vitro</I>抗菌活性を対照薬剤にtolciclateとbifonazoleを用い, 寒天平板希釈法により比較検討した.<BR>Liranaftateは皮膚糸状菌に対して最も強力な抗菌活性を示した. … Liranaftateの抗菌活性は総じてtolciclateより優れ, 抗菌スペクトルも広域であった. …
- NAID 130003671709
Related Links
- Tolciclate is an antifungal. [edit] References. ^ Ryder, N. S.; Frank, I.; Dupont, M. C. (May 1986). "Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate". Antimicrobial Agents and Chemotherapy 29 ...
- Title: Tolciclate. CAS Registry Number: 50838-36-3. CAS Name: Methyl(3- methylphenyl)carbamothioic acid O-(1,2,3,4-tetrahydro-1,4-methanonaphthalen- 6-yl) ester. Additional Names: O-(1,4-methano-1,2,3 ...