Category: 3818-50-6

Musdal, Yaman published the artcileFDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1, HPLC of Formula: 3818-50-6, the publication is Chemico-Biological Interactions (2013), 205(1), 53-62, database is CAplus and MEDLINE.

Glutathione transferase P1-1 (GST P1-1) is often overexpressed in tumor cells and is regarded as a contributor to their drug resistance. Inhibitors of GST P1-1 are expected to counteract drug resistance and may therefore serve as adjuvants in the chemotherapy of cancer by increasing the efficacy of cytostatic drugs. Finding useful inhibitors among compounds used for other indications would be a shortcut to clin. applications and a search for GST P1-1 inhibitors among approved drugs and other compounds was therefore conducted. We tested 1040 FDA-approved compounds as inhibitors of the catalytic activity of purified human GST P1-1 in vitro. We identified chlorophyllide, merbromine, hexachlorophene, and ethacrynic acid as the most effective GST P1-1 inhibitors with IC₅₀ values in the low micromolar range. For comparison, these compounds were even more potent in the inhibition of human GST A3-3, an enzyme implicated in steroid hormone biosynthesis. In distinction from the other inhibitors, which showed conventional inhibition patterns, the competitive inhibitor ethacrynic acid elicited strong kinetic cooperativity in the glutathione saturation of GST P1-1. Apparently, ethacrynic acid serves as an allosteric inhibitor of the enzyme. In their own right, the compounds investigated are less potent than desired for adjuvants in cancer chemotherapy, but the structures of the most potent inhibitors could serve as leads for the synthesis of more efficient adjuvants.

Chemico-Biological Interactions published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, HPLC of Formula: 3818-50-6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Mutalik, G. S. published the artcileComparative clinical trial of bitoscanate, bephenium hydroxynaphthoate, and tetrachlorethylene in hookworm infection, COA of Formula: C28H29NO4, the publication is Indian Journal of Medical Sciences (1972), 26(11), 718-22, database is CAplus and MEDLINE.

Bitoscanate (I) [4044-65-9] (200-300 mg/day) decreased fecal egg counts by 98% and cured 15 of 23 patients with hookworm whereas bephenium hydroxynaphthoate [3818-50-6] (2.4 g) decreased fecal egg count by 76% and cured 3 of 23 patients and tetrachloroethylene [127-18-4] (3 mL) decreased egg counts by 89% and cured 5 of 23 patients. Mild and transient gastrointestinal reactions were obsd with all 3 drugs but most frequently with bitoscanate.

Indian Journal of Medical Sciences published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, COA of Formula: C28H29NO4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Katiyar, R. D. published the artcileThiabendazole as an anthelmintic of outstanding efficiency, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Indian Veterinary Journal (1964), 41(12), 803-9, database is CAplus.

Four trials are described in which thiabendazole [2-(4-thiazolyl)benzimidazole] (I) efficiency is tested against nematodes. Frantin (bephenium hydroxynaphthoate) (II), Promintic (Methrydine) (III), and phenothiazine (IV) were used as comparisons. Lambs naturally parasitized with Haemonchus, Trichostrongyles, Ostertagia, Nematodirus, Oesophagostomum, Cooperia, and Bunostomum spp. were treated with I (50 mg./kg. body weight), II (4 g./lamb), III (200 mg./kg. body weight), IV (600 mg./kg.) and no treatment. The reductions in egg counts were 95.7, 82.1, 78.7, 76.2, and 39.2%, resp. Against individual nematode species in sheep, I was 85-100% effective. It was 97.7% effective against nematodes causing gastroenteritis in crossbred Angora kids, while IV was only 76.5% effective. Romney Marsh rams with a heavy infestation of Strongloides papillosus were treated with IV with no effect, while treatment with I reduced the ova count by 91-95% over 15 days. In all trials, treatment with I increased the body weight

Indian Veterinary Journal published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Blagov, N A published the artcile[Microparasitocenosis of the intestines and the activity of intestinal enzymes in patients with trichocephaliasis during treatment]., Safety of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Meditsinskaia parazitologiia i parazitarnye bolezni (1989), 49-53, database is MEDLINE.

Results of the studies of large intestine microflora, enterokinase and alkaline phosphatase activity in the feces of 298 children and adults suffering from trichocephaliasis are presented. Intestinal dysbacteriosis was observed in 51.7% cases, increased enterokinase activity, in 57.6% cases and increased alkaline phosphatase activity, in 55% cases. Enteric enzyme activity relation to the state of enteric microflora is demonstrated. Specific bephenium hydroxynaphthoate and mebendazole treatment was followed by increased dysbacteriosis and higher intestinal enzyme activity, especially in case of bephenium hydroxynaphthoate treatment. Normalization of the above-mentioned parameters was observed 90-120 days after the end of the treatment.

Meditsinskaia parazitologiia i parazitarnye bolezni published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Safety of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cortinas de Nava, C. published the artcileMutagenicity of antiamebic and anthelmintic drugs in the Salmonella typhimurium microsomal test system, Product Details of C28H29NO4, the publication is Mutation Research, Genetic Toxicology Testing (1983), 117(1-2), 79-91, database is CAplus and MEDLINE.

Amebicides (chloroquine (I) [54-05-7], diiodohydroxyquin  [83-73-8], iodochlorohydroxyquin  [130-26-7] and dehydroemetine  [4914-30-1]) and anthelmintics (bephenium hydroxynaphthoate  [3818-50-6], 4-hexylresorcinol  [136-77-6], mebendazole  [31431-39-7], niclosamide  [50-65-7], pyrantel pamoate  [22204-24-6] and pyrvinium pamoate  [3546-41-6]) were tested for mutagenicity in the S. typhimurium microsomal test system. Frameshift mutations were induced by dehydroemetine and niclosamide following activation by microsomal enzymes, while pyrvinium pamoate induced both frameshift and base-pair substitution mutations with or without metabolic activation. The urine of mice treated with dehydroemetine or pyrvinium pamoate showed no mutagenic activity. However, urine obtained from mice treated with niclosamide was mutagenic in strains TA98 and TA1538. The fluctuation assay showed I to be mutagenic in TA1537, a strain which detects frameshift mutations.

Mutation Research, Genetic Toxicology Testing published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Product Details of C28H29NO4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Arriaga Alba, M. published the artcileMutagenicity of products generated by the reaction between several antiparasitic drugs and nitrite, HPLC of Formula: 3818-50-6, the publication is Environmental and Molecular Mutagenesis (1988), 12(1), 65-73, database is CAplus and MEDLINE.

Drugs containing secondary aliphatic amines, heterocyclic N, or secondary aliphatic amido groups (chloroquine, dihydroemetine, mebendazole, and piperazine) and pyrimidine derivatives such as pyrantel pamoate were reacted in vitro with NaNO₂ at pH 3.7 and became mutagenic for Salmonella typhimurium strain TA1535. The products derived from the nitrosation of chloroquine and dehydroemetine required metabolic activation by mammalian hepatic S9 to be mutagenic. The N-nitroso derivatives of mebendazole, piperazine, and pyrantel pamoate were mutagenic with and without S9, although more activity was noted in the presence of S9 with the nitrosated compounds formed from mebendazole and piperazine. Under identical conditions, no mutagenic products were detected from quaternary ammonium salts such as bephenium hydroxynaphthoate or drugs containing tertiary heterocyclic amino groups, such as iodochlorhydroxyquin.

Environmental and Molecular Mutagenesis published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, HPLC of Formula: 3818-50-6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Arriaga Alba, M. published the artcileMutagenicity of urine from mice exposed orally to nitrite and various aminated antiparasitic drugs, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Environmental and Molecular Mutagenesis (1989), 14(1), 13-19, database is CAplus and MEDLINE.

The mutagenic activity of mouse urine was determined after oral administration of sodium nutrite and pyrantel pamoate, chloroquine, piperazine, dehydroemetine, iodochlorhydroxyquin, and bephenium hydroxynaphthoate. The simultaneous administration of piperazine or chloroquine with sodium nitrite produced urinary mutagens that appeared conjugated as glucuronides, whereas pyrantel pamoate and dehydroemetine in the presence of nitrite caused only slight mutagenic urine. No mutagenic activity was detected in the urine of mice to which halogenated derivatives of tertiary amines (iodochlorhydroxyquin) or quaternary ammonium salts (bephenium hydroxynaphthoate) were administered together with nitrite.

Environmental and Molecular Mutagenesis published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Brody, Gerald published the artcileComparative activity of 29 known anthelmintics under standarized drug-diet and gavage medication regimens against four helminth species in mice, Recommanded Product: N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Journal of Parasitology (1971), 57(5), 1068-77, database is CAplus and MEDLINE.

Of 29 reference anthelmintics (21 aromatic-heterocyclic and 8 organophosphate compounds) tested at an initial concentration of 1000 ppm in the diet of mice for 18 days against 4 mouse helminths, parbendazole (I) [14255-87-9] was the only compound exhibiting activity against all 4 helminths and the effectiveness of I was .sim.100% against the 4 helminths. However, in experiments using the 29 compounds at an initial dose of 200 mg/kg/day by gavage for 3 days, significant differences were observed in the effectiveness of a number of the anthelmintics in the 2 different medication regimens. The data below refers to the effectiveness of the compounds when given in the diet. Against Nematospiroides dubius, I, pyrantel (II) [15686-83-6], dl-tetramisole [5036-02-2], l-tetramisole (III) [14769-73-4], and thiabendazole (IV) [148-79-8] were the most effective. Against Hymenolepis nana (tapeworm), I and Ro-2-9009 (1,4-bis(2-diethylaminoethoxy)anthraquinone-2HCl (V) [18272-48-5] were the most effective. Against Syphacia obvelata, I, II, III, IV, V, dithiazanine (VI) [7187-55-5] (at 250 ppm), pyrvinium (VII) [7187-62-4], stilbazium (VIII) [3784-99-4], coumaphos (IX) [56-72-4], haloxon (X) [321-55-1], mercaptophos (XI) [55-38-9], and Ruelene (XII) [299-86-5] were the most effective. Against Aspiculuris tetraptera, I, II, VI, VII, VIII, IX, X, XI, XII, and dichlorvos [62-73-7] were the most effective.

Journal of Parasitology published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Recommanded Product: N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Busev, A. I. published the artcileSpectroscopic study of the reaction products of Rhodamine 6Zh with naftamon during extraction by benzene, Product Details of C28H29NO4, the publication is Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya (1974), 17(9), 1367-70, database is CAplus.

Reaction products of the dye Rhodamine 6Zh (I) [7325-85-1] with Naftamon (II) [3818-50-6], and the dye itself were extracted with C6H6, and the spectra obtained from the extracts in the region 17,000-22,000 cm-1 were split into gauss constituents. Four gauss peaks were found in the extract corresponding to monomeric and dimeric forms of ionic associates of I with II and traces of the dye.

Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Product Details of C28H29NO4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Coles, G. C. published the artcileMechanism of action of the anthelmintic levamisole, SDS of cas: 3818-50-6, the publication is General Pharmacology (1975), 6(4), 309-13, database is CAplus.

In a solution of levamisole-HCl (I) [16595-80-5], the small round worm Nippostrongylus brasiliensis became paralyzed, but recovered on being left in the solution Both the rates of paralysis and recovery increased with increasing concentration of I. A small percentage of Ascaris suum also resumed movement in I, and were then protected against the effects of the anthelmintics bephenium hydroxynaphthoate [3818-50-6], methyridine [114-91-0], and pyrantel tartrate [33401-94-4]. The autonomic blocking agents mecamylamine and pempidine blocked I contractions in normal A. suum, and the results suggested that all 4 anthelmintics acted in a similar way.

General Pharmacology published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, SDS of cas: 3818-50-6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts