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Items: 1 to 20 of 165

1.

(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.

Yeh TK, Tsai TY, Hsu T, Cheng JH, Chen X, Song JS, Shy HS, Chiou MC, Chien CH, Tseng YJ, Huang CY, Yeh KC, Huang YL, Huang CH, Huang YW, Wang MH, Tang HK, Chao YS, Chen CT, Jiaang WT.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3596-600. doi: 10.1016/j.bmcl.2010.04.124. Epub 2010 May 17.

PMID:
20483603
2.

Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.

Tsai TY, Hsu T, Chen CT, Cheng JH, Chiou MC, Huang CH, Tseng YJ, Yeh TK, Huang CY, Yeh KC, Huang YW, Wu SH, Wang MH, Chen X, Chao YS, Jiaang WT.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1908-12. doi: 10.1016/j.bmcl.2009.02.061. Epub 2009 Feb 21.

PMID:
19269819
3.

3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.

Coumar MS, Chang CN, Chen CT, Chen X, Chien CH, Tsai TY, Cheng JH, Wu HY, Han CH, Wu SH, Huang YW, Hsu T, Hsu LJ, Chao YS, Hsieh HP, Jiaang WT.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1274-9. Epub 2006 Dec 12.

PMID:
17194587
4.

(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.

Ammirati MJ, Andrews KM, Boyer DD, Brodeur AM, Danley DE, Doran SD, Hulin B, Liu S, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soglia CB, Treadway JL, VanVolkenburg MA, Wilder DC, Piotrowski DW.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1991-5. doi: 10.1016/j.bmcl.2009.02.041. Epub 2009 Feb 13.

PMID:
19275964
5.

2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.

Tsu H, Chen X, Chen CT, Lee SJ, Chang CN, Kao KH, Coumar MS, Yeh YT, Chien CH, Wang HS, Lin KT, Chang YY, Wu SH, Chen YS, Lu IL, Wu SY, Tsai TY, Chen WC, Hsieh HP, Chao YS, Jiaang WT.

J Med Chem. 2006 Jan 12;49(1):373-80.

PMID:
16392822
6.

1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.

Villhauer EB, Brinkman JA, Naderi GB, Dunning BE, Mangold BL, Mone MD, Russell ME, Weldon SC, Hughes TE.

J Med Chem. 2002 Jun 6;45(12):2362-5.

PMID:
12036346
7.

(2S,4S)-4-Fluoro-1-{[(2-hydroxy-1,1-dimethylethyl)amino]acetyl}-pyrrolidine-2-carbonitrile monobenzenesulfonate (TS-021) is a selective and reversible dipeptidyl peptidase IV inhibitor.

Tajima A, Yamamoto K, Kozakai A, Okumura-Kitajima L, Mita Y, Kitano K, Jingu S, Nakaike S.

Eur J Pharmacol. 2011 Mar 25;655(1-3):99-107. doi: 10.1016/j.ejphar.2011.01.010. Epub 2011 Jan 22.

PMID:
21262219
8.

Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.

Wang L, Zhang B, Ji J, Li B, Yan J, Zhang W, Wu Y, Wang X.

Eur J Med Chem. 2009 Aug;44(8):3318-22. doi: 10.1016/j.ejmech.2009.03.021. Epub 2009 Mar 26.

PMID:
19375196
9.

Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.

Tsai TY, Hsu T, Chen CT, Cheng JH, Yeh TK, Chen X, Huang CY, Chang CN, Yeh KC, Hsieh SH, Chien CH, Chang YW, Huang CH, Huang YW, Huang CL, Wu SH, Wang MH, Lu CT, Chao YS, Jiaang WT.

Bioorg Med Chem. 2009 Mar 15;17(6):2388-99. doi: 10.1016/j.bmc.2009.02.020. Epub 2009 Feb 20.

PMID:
19261480
10.

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM.

J Med Chem. 2006 Oct 19;49(21):6416-20.

PMID:
17034148
11.

Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile).

Brandt I, Joossens J, Chen X, Maes MB, Scharpé S, De Meester I, Lambeir AM.

Biochem Pharmacol. 2005 Jul 1;70(1):134-43.

PMID:
15907807
12.

1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.

Villhauer EB, Brinkman JA, Naderi GB, Burkey BF, Dunning BE, Prasad K, Mangold BL, Russell ME, Hughes TE.

J Med Chem. 2003 Jun 19;46(13):2774-89.

PMID:
12801240
13.

ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity.

Matsuyama-Yokono A, Tahara A, Nakano R, Someya Y, Nagase I, Hayakawa M, Shibasaki M.

Biochem Pharmacol. 2008 Jul 1;76(1):98-107. doi: 10.1016/j.bcp.2008.03.021. Epub 2008 Apr 6.

PMID:
18468582
14.

Antihyperglycemic effects of ASP8497 in streptozotocin-nicotinamide induced diabetic rats: comparison with other dipeptidyl peptidase-IV inhibitors.

Tahara A, Matsuyama-Yokono A, Nakano R, Someya Y, Hayakawa M, Shibasaki M.

Pharmacol Rep. 2009 Sep-Oct;61(5):899-908.

15.

cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.

Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, McClure LD, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soeller WC, Soglia CB, Treadway JL, VanVolkenburg MA, Wang H, Wilder DC, Olson TV.

J Med Chem. 2006 Jun 1;49(11):3068-76.

PMID:
16722626
16.

7-But-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin-8-one is a novel competitive and selective inhibitor of dipeptidyl peptidase IV with an antihyperglycemic activity.

Yamazaki K, Yasuda N, Inoue T, Nagakura T, Kira K, Shinoda M, Saeki T, Tanaka I.

J Pharmacol Exp Ther. 2006 Dec;319(3):1253-7. Epub 2006 Sep 15.

17.

Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.

Fukushima H, Hiratate A, Takahashi M, Mikami A, Saito-Hori M, Munetomo E, Kitano K, Chonan S, Saito H, Suzuki A, Takaoka Y, Yamamoto K.

Bioorg Med Chem. 2008 Apr 1;16(7):4093-106. doi: 10.1016/j.bmc.2008.01.016. Epub 2008 Jan 16.

PMID:
18243000
18.

Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.

Senten K, Van der Veken P, De Meester I, Lambeir AM, Scharpé S, Haemers A, Augustyns K.

J Med Chem. 2003 Nov 6;46(23):5005-14.

PMID:
14584950
19.

Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys.

Lee B, Shi L, Kassel DB, Asakawa T, Takeuchi K, Christopher RJ.

Eur J Pharmacol. 2008 Jul 28;589(1-3):306-14. doi: 10.1016/j.ejphar.2008.04.047. Epub 2008 Apr 26.

PMID:
18538760
20.

Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.

Nordhoff S, Cerezo-Gálvez S, Deppe H, Hill O, López-Canet M, Rummey C, Thiemann M, Matassa VG, Edwards PJ, Feurer A.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4201-3. doi: 10.1016/j.bmcl.2009.05.109. Epub 2009 May 30.

PMID:
19515557

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