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Journals and Conferences
The synthesis of a novel gut selective MTP inhibitor, 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), and its in vitro and in vivo profile are described. Dirlotapide (3) demonstrated excellent potency against MTP enzyme in HepG2 cells and canine hepatocytes. This novel MTP inhibitor… (More)
The medical records of 17 horses that were evaluated and treated because of colic caused by pedunculated lipomas between 1983 and 1990 were reviewed. The mean age of the horses was 16.6 +/- 3.9 years (range, 10 to 26 years), which was significantly greater than that of the population of horses evaluated because of colic (control population) during the same… (More)
Seventeen Thoroughbred horses with moderate to severe gastric ulceration were purchased from a race track within 10 days of racing and were treated once daily with either omeprazole (9 horses) or vehicle (8 horses) and evaluated gastroscopically for ulcer healing. Horses were administered omeprazole (1.5 mg/kg bwt/day) or vehicle by nasogastric tube once… (More)
A single preoperative dose of antibiotic proved as effective as a preoperative and 7-day postoperative course in reducing complications following rumenotomy in cattle. Exploratory rumenotomy was performed on 29 healthy Angus steers, which were allotted to the following treatment groups: (1) no antibiotic therapy, (2) single-dose, preoperative, antibiotic… (More)
Structure-activity relationship (SAR) studies of novel 5-alkyl and 5-aryl/heteroaryl substituted 1,2,4-triazoles are described. The in vitro activity is compared to the pyrazole class of compounds with analogous side chains to delineate the contribution of the triazole ring nitrogen in binding to the active site. Both series are quite potent and selective… (More)
Structure-activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine… (More)
We have successfully identified a number of novel MTP inhibitors with single digit nanomolar potency. Analogues 10aq and 10dq demonstrated in vivo efficacy in a murine gut retention assay.
Twenty-one cases of urolithiasis in small ruminants were examined to evaluate the efficacy of various surgical treatments. Of 21 cases, all but 1 had multiple calculi. Urethral process amputation and medical therapy either did not relieve the obstruction or provided only temporary relief (< 36 hours) in 14 of 16 cases. In 2 cases, obstruction recurred in 1… (More)
Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COX enzymes are described. The studies led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats.