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N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat.
Kalgutkar AS, Frederick KS, Chupka J, Feng B, Kempshall S, Mireles RJ, Fenner KS, Troutman MD. Kalgutkar AS, et al. Among authors: frederick ks. J Pharm Sci. 2009 Dec;98(12):4914-27. doi: 10.1002/jps.21756. J Pharm Sci. 2009. PMID: 19373887
Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human.
Kalgutkar AS, Feng B, Nguyen HT, Frederick KS, Campbell SD, Hatch HL, Bi YA, Kazolias DC, Davidson RE, Mireles RJ, Duignan DB, Choo EF, Zhao SX. Kalgutkar AS, et al. Among authors: frederick ks. Drug Metab Dispos. 2007 Nov;35(11):2111-8. doi: 10.1124/dmd.107.016162. Epub 2007 Aug 8. Drug Metab Dispos. 2007. PMID: 17686907
Pharmacokinetics, disposition and lipid-modulating activity of 5-{2-[4-(3,4-difluorophenoxy)-phenyl]-ethylsulfamoyl}-2-methyl-benzoic acid, a potent and subtype-selective peroxisome proliferator-activated receptor alpha agonist in preclinical species and human.
Frederick KS, Maurer TS, Kalgutkar AS, Royer LJ, Francone OL, Winter SM, Terra SG, Chen D, Gao X. Frederick KS, et al. Xenobiotica. 2009 Oct;39(10):766-81. doi: 10.1080/00498250903121796. Xenobiotica. 2009. PMID: 19622022
Elucidation of the biochemical basis for a clinical drug-drug interaction between atorvastatin and 5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid (CP-778875), a subtype selective agonist of the peroxisome proliferator-activated receptor alpha.
Kalgutkar AS, Chen D, Varma MV, Feng B, Terra SG, Scialis RJ, Rotter CJ, Frederick KS, West MA, Goosen TC, Gosset JR, Walsky RL, Francone OL. Kalgutkar AS, et al. Among authors: frederick ks. Xenobiotica. 2013 Nov;43(11):963-72. doi: 10.3109/00498254.2013.791004. Epub 2013 Apr 30. Xenobiotica. 2013. PMID: 23631744
Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.
Kalgutkar AS, Frederick KS, Hatch HL, Ambler CM, Perry DA, Garigipati RS, Chang GC, Lefker BA, Clark RW, Morehouse LA, Francone O, Hu X. Kalgutkar AS, et al. Among authors: frederick ks. Xenobiotica. 2014 Jul;44(7):591-605. doi: 10.3109/00498254.2013.874611. Epub 2013 Dec 31. Xenobiotica. 2014. PMID: 24380613
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists.
Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, DiBrinno J, Zawistoski MP, Bagley SW, Li J, Zeng Y, Santucci S, Oliver R, Corbett M, Olson T, Chen C, Li M, Paralkar VM, Riccardi KA, Healy DR, Kalgutkar AS, Maurer TS, Nguyen HT, Frederick KS. Didiuk MT, et al. Among authors: frederick ks. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4555-9. doi: 10.1016/j.bmcl.2009.07.004. Epub 2009 Jul 8. Bioorg Med Chem Lett. 2009. PMID: 19625189
Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.
Kalgutkar AS, Griffith DA, Ryder T, Sun H, Miao Z, Bauman JN, Didiuk MT, Frederick KS, Zhao SX, Prakash C, Soglia JR, Bagley SW, Bechle BM, Kelley RM, Dirico K, Zawistoski M, Li J, Oliver R, Guzman-Perez A, Liu KK, Walker DP, Benbow JW, Morris J. Kalgutkar AS, et al. Among authors: frederick ks. Chem Res Toxicol. 2010 Jun 21;23(6):1115-26. doi: 10.1021/tx100137n. Chem Res Toxicol. 2010. PMID: 20507089
18 results