シクログアニル。パモ酸シクログアニル
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/21 07:37:05」(JST)
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Cycloguanil
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| Systematic (IUPAC) name |
| 1-(4-chlorophenyl)-6,6-dimethyl-1,3,5-triazine-2,4-diamine |
| Clinical data |
| Legal status |
? |
| Identifiers |
| CAS number |
516-21-2 |
| ATC code |
P01BB02 |
| PubChem |
CID 9049 |
| ChemSpider |
8697 Y |
| UNII |
26RM326WVN Y |
| ChEMBL |
CHEMBL747 Y |
| Chemical data |
| Formula |
C11H14ClN5 |
| Mol. mass |
251.715 g/mol |
SMILES
- Clc1ccc(cc1)N2C(=N/C(=N\C2(C)C)N)\N
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InChI
-
InChI=1S/C11H14ClN5/c1-11(2)16-9(13)15-10(14)17(11)8-5-3-7(12)4-6-8/h3-6H,1-2H3,(H4,13,14,15,16) Y
Key:QMNFFXRFOJIOKZ-UHFFFAOYSA-N Y
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| Y (what is this?) (verify) |
Cycloguanil is a dihydrofolate reductase inhibitor,[1] and is a metabolite of the antimalarial drug proguanil; its formation in vivo has been thought to be primarily responsible for the antimalarial activity of proguanil.[2] However, more recent work has indicated that, while proguanil is synergistic with the drug atovaquone (as in the combination Malarone), cycloguanil is in fact antagonistic to the effects of atovaquone, suggesting that, unlike cycloguanil, proguanil may have an alternative mechanism of antimalarial action besides dihydrofolate reductase inhibition.[3]
Although cycloguanil is not currently in general use as an antimalarial, the continuing development of resistance to current antimalarial drugs has led to renewed interest in studying the use of cycloguanil in combination with other drugs.[4]
References
- ^ Srivastava IK, Vaidya AB (June 1999). "A mechanism for the synergistic antimalarial action of atovaquone and proguanil". Antimicrob. Agents Chemother. 43 (6): 1334–9. PMC 89274. PMID 10348748.
- ^ Watkins, W. S. (Jun 1984). "The activity of proguanil and its metabolites, cycloguanil and p-chlorophenylbiguanide, against Plasmodium falciparum in vitro" (Free full text). Annals of Tropical Medicine and Parasitology 78 (3): 273–278. ISSN 0003-4983. PMID 6385887. edit
- ^ Thapar, M. G.; Gupta, S.; Spindler, C.; Wernsdorfer, W. H.; Björkman, A. (May 2003). "Pharmacodynamic interactions among atovaquone, proguanil and cycloguanil against Plasmodium falciparum in vitro". Transactions of the Royal Society of Tropical Medicine and Hygiene 97 (3): 331–337. doi:10.1016/S0035-9203(03)90162-3. ISSN 0035-9203. PMID 15228254. edit
- ^ Walzer, P. ; F.; Foy, J.; Steele, P.; White, M. (Jul 1993). "Synergistic combinations of Ro 11-8958 and other dihydrofolate reductase inhibitors with sulfamethoxazole and dapsone for therapy of experimental pneumocystosis". Antimicrobial Agents and Chemotherapy 37 (7): 1436–1443. doi:10.1128/AAC.37.7.1436. ISSN 0066-4804. PMC 187990. PMID 8363372. edit
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Antiparasitics – antiprotozoal agents – Chromalveolate antiparasitics (P01)
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Alveo-
late |
Apicom-
plexa |
Conoidasida/
(Coccidiostats) |
| Cryptosporidiosis |
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| Isosporiasis |
- trimethoprim/sulfamethoxazole#
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| Toxoplasmosis |
- pyrimethamine
- sulfadiazine
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| Aconoidasida |
| Malaria |
Individual
agents |
Hemozoin
inhibitors |
| aminoquinolines |
- (4-): amodiaquine#
- chloroquine#
- (8-): primaquine#
- pamaquine
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| 4-methanolquinolines |
- mefloquine#
- quinine#
- quinidine
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| Other |
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| Antifolates |
DHFR inhibitors
(antifols) |
- proguanil#
- chlorproguanil
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| Sulfonamides |
- sulfadoxine
- sulfamethoxypyrazine
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| Coformulation |
- sulfadoxine/pyrimethamine (SP)#
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Sesquiterpene
lactones |
- artemether#
- artesunate#
- dihydroartemisinin
- artemotil
- artemisinin
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| Other |
- atovaquone (with proguanil as Malarone)
- tetracycline
- doxycycline#
- clindamycin
- pyronaridine
- piperaquine
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Combi-
nations |
| Fixed-dose (coformulated) ACTs |
- artemether/lumefantrine#
- artesunate/amodiaquine (ASAQ)
- artesunate/mefloquine (ASMQ)
- dihydroartemisinin/piperaquine
- artesunate/pyronaridine
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Other combinations
(not co-formulated) |
- artesunate/SP
- artesunate/mefloquine
- quinine/tetracycline
- quinine/doxycycline
- quinine/clindamycin
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| Babesiosis |
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Cilio-
phora |
- Balantidiasis: Tetracycline
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Hetero-
kont |
- Blastocystosis: Metronidazole
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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UpToDate Contents
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English Journal
- [Contribution of molecular genetics to the understanding of chemoresistance of Plasmodium falciparum].
- Le Bras J1, Basco LK, Cremer G, Charmot G.
- Bulletin de la Societe de pathologie exotique (1990).Bull Soc Pathol Exot.1992;85(2):146-9.
- PMID 1356539
- Activities of respository preparations of cycloguanil pamoate and 4,4'-diacetyldiaminodiphenylsulfone, alone and in combination, against infections with Plasmodium cynomolgi in rhesus monkeys.
- Schmidt LH, Rossan RN.
- Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.1984 Nov;26(5):611-42.
- The studies summarized in this report were concerned with the capacities of repository preparations of cycloguanil pamoate (CGT-P) to protect rhesus monkeys against infections with drug-susceptible and pyrimethamine-resistant strains of Plasmodium cynomolgi. Administered intramuscularly as a suspens
- PMID 6393864
- Long-acting, repository antimalarial agents. Duration of protection in mice and monkeys following administration of pyrimethamine pamoate.
- Werbel LM, Jacobs RL, Steinkampf RW, Worth DF.
- The American journal of tropical medicine and hygiene.Am J Trop Med Hyg.1984 Jul;33(4):526-33.
- The duration of protection from blood-stage malarial challenge following single injections of pyrimethamine pamoate was assessed in mice and monkeys. This duration was dose-related and ranged from several weeks in mice to over 4 months in the monkeys. Comparisons with the previously reported reposit
- PMID 6236702
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- Cycloguanil embonate - chemical information, properties, structures, articles, patents and more chemical data. ... 2-Naphthalenecarboxylic acid, 4,4'-methylenebis(3-hydroxy-, compd. with 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-1 ...
Related Pictures
★リンクテーブル★
[★]
- 英
- cycloguanil
- 化
- パモ酸シクログアニル, cycloguanil embonate
抗マラリア薬。ビグアナイド系
参考
- http://en.wikipedia.org/wiki/Cycloguanil
- 2. [charged] 抗マラリア剤：概要 - uptodate [1]
- 3. [charged] アトバコンおよびプログアニル：医薬品情報 - uptodate [2]
- 4. [charged] アトバコンおよびプログアニル：小児用医薬品情報 - uptodate [3]
[★]
シクログアニル。cycloguanil embonate