Detail of "84532-72-9"

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N-[[5-(Trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]-N-methyl glycine (Tolrestat), a potent, orally active aldose reductase inhibitor

N-[[5-(Trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]-N-methyl glycine (Tolrestat), a potent, orally active aldose reductase inhibitor. Sestanj, Kazimir; Bellini, Francesco; Fung, Steven; Abraham, Nedumparambil; Treasurywala, Adi; Humber, Leslie; Simard-Dequesne, Nicole; Dvornik, Dushan (Chem. Dep., Ayerst Lab. Res. Inc., Princeton, NJ, USA). J. Med. Chem., 27(3), 255-6 (English) 1984. CODEN: JMCMAR. ISSN: 0022-2623. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 25 The chem., biochem., and pharmacol. of tolrestat (AY 27773)(I) [82964-04-3] is described. I was prepd. from 6-methoxy-5-(trifluoromethyl)naphthalene-1-carboxylic acid [84532-72-9] by treatment of its acid chloride with Me sarcosinate [5473-12-1], heating the resulting carboxamide [84533-46-0] formed with P2S5 to I Me ester [84533-04-0] followed by hydrolysis with KOH. I inhibited bovine lens aldose reductase [9028-31-3] showing an IC50 of 3.5 ′ 10-8M and decreased galactitol accumulation by 50% in the sciatic nerve in the galactosemic rat model after administration for 4 days in the diet at 7.3 mg/kg/day in rats rendered diabetic with streptozotocin, the dose of I that decreased sorbitol accumulation in the sciatic nerve by 50% after 3 wk administration in the diet was 2.4 mg/kg/day. Treatment of diabetic rats with I in the diet for 7 days at 1. 82964-04-3 is just another one chemical used in this study.8 mg/kg/day caused a reversal to normal red blood cell sorbitol levels. .

6-Alkoxy-5-trifluoromethyl-1-naphthoic acids

6-Alkoxy-5-trifluoromethyl-1-naphthoic acids.. Senaratne, K. Pushpananda A. (Ethyl Corp., USA). U.S.There are some reagents with their cas registry numbers 84532-72-9 and 103604-49-5 are used in this study. US 4629808 A 16 Dec 1986, 3 pp. (United States of America) CODEN: USXXAM. CLASS: ICM: C07C063-34. NCL: 562467000. APPLICATION: US 85-746768 20 Jun 1985. DOCUMENT TYPE: Patent CA Section: 25 (Benzene, Its Derivatives, and Condensed Benzenoid Compounds) Section cross-reference(s): 1 The title compds. I (R = COOH; R1 = alkyl), useful as intermediates for pharmaceuticals, were prepd. by hydrolysis of I (R = CN). Thus, treatment of 0.5 g I (R = CN, R1 = Me) in MeOH/H2O with 0.6 g KOH at 130° under 90-100 psi gave 98% I (R = COOH R1 = Me). .