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Items: 1 to 20 of 105

1.

Property-based design in the optimisation of benzamide glucokinase activators: from hit to clinic.

McKerrecher D, Waring MJ.

Prog Med Chem. 2013;52:1-43. doi: 10.1016/B978-0-444-62652-3.00001-6. Review. No abstract available.

PMID:
23384665
2.

Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators.

Mao W, Ning M, Liu Z, Zhu Q, Leng Y, Zhang A.

Bioorg Med Chem. 2012 May 1;20(9):2982-91. doi: 10.1016/j.bmc.2012.03.008. Epub 2012 Mar 8.

PMID:
22459213
3.

Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase.

Zhang L, Li H, Zhu Q, Liu J, Chen L, Leng Y, Jiang H, Liu H.

Bioorg Med Chem. 2009 Oct 15;17(20):7301-12. doi: 10.1016/j.bmc.2009.08.045. Epub 2009 Aug 24.

PMID:
19758809
4.

Metabolic activation of N-thiazol-2-yl benzamide as glucokinase activators: Impacts of glutathione trapping on covalent binding.

Iino T, Hashimoto N, Hasegawa T, Chiba M, Eiki J, Nishimura T.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1619-22. doi: 10.1016/j.bmcl.2010.01.041. Epub 2010 Jan 20.

PMID:
20138764
5.

Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus.

Park K, Lee BM, Kim YH, Han T, Yi W, Lee DH, Choi HH, Chong W, Lee CH.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):537-42. doi: 10.1016/j.bmcl.2012.11.018. Epub 2012 Nov 16.

PMID:
23218712
6.

Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H-pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus.

Park K, Lee BM, Hyun KH, Lee DH, Choi HH, Kim H, Chong W, Kim KB, Nam SY.

Bioorg Med Chem. 2014 Apr 1;22(7):2280-93. doi: 10.1016/j.bmc.2014.02.009. Epub 2014 Feb 17.

PMID:
24588963
7.

Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs.

Eiki J, Nagata Y, Futamura M, Sasaki-Yamamoto K, Iino T, Nishimura T, Chiba M, Ohyama S, Yoshida-Yoshimioto R, Fujii K, Hosaka H, Goto-Shimazaki H, Kadotani A, Ohe T, Lin S, Langdon RB, Berger JP.

Mol Pharmacol. 2011 Dec;80(6):1156-65. doi: 10.1124/mol.111.074401. Epub 2011 Sep 21.

8.

Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators.

Iino T, Tsukahara D, Kamata K, Sasaki K, Ohyama S, Hosaka H, Hasegawa T, Chiba M, Nagata Y, Eiki J, Nishimura T.

Bioorg Med Chem. 2009 Apr 1;17(7):2733-43. doi: 10.1016/j.bmc.2009.02.038. Epub 2009 Feb 25.

PMID:
19282189
9.

Design, synthesis and SAR of novel glucokinase activators.

Cheruvallath ZS, Gwaltney SL 2nd, Sabat M, Tang M, Feng J, Wang H, Miura J, Guntupalli P, Jennings A, Hosfield D, Lee B, Wu Y.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2166-71. doi: 10.1016/j.bmcl.2013.01.093. Epub 2013 Feb 4.

PMID:
23434031
10.

Small molecule glucokinase activators as novel anti-diabetic agents.

Leighton B, Atkinson A, Coghlan MP.

Biochem Soc Trans. 2005 Apr;33(Pt 2):371-4. Review.

PMID:
15787609
11.

Novel glucokinase activators: a patent review (2008 - 2010).

Sarabu R, Berthel SJ, Kester RF, Tilley JW.

Expert Opin Ther Pat. 2011 Jan;21(1):13-33. doi: 10.1517/13543776.2011.542413. Epub 2010 Dec 15. Review.

PMID:
21155690
12.

Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators.

Nishimura T, Iino T, Mitsuya M, Bamba M, Watanabe H, Tsukahara D, Kamata K, Sasaki K, Ohyama S, Hosaka H, Futamura M, Nagata Y, Eiki J.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1357-60. doi: 10.1016/j.bmcl.2009.01.053. Epub 2009 Jan 21.

PMID:
19188063
13.

Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life.

Pike KG, Allen JV, Caulkett PW, Clarke DS, Donald CS, Fenwick ML, Johnson KM, Johnstone C, McKerrecher D, Rayner JW, Walker RP, Wilson I.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3467-70. doi: 10.1016/j.bmcl.2011.03.093. Epub 2011 Apr 7.

PMID:
21515051
14.

[Advances in the study of glucokinase and small molecule glucokinase activators].

Li YQ, Feng ZQ, Song HR, Guo YS, Guo ZR.

Yao Xue Xue Bao. 2006 May;41(5):390-4. Review. Chinese. No abstract available.

PMID:
16848312
15.

Targeting glucokinase activation for the treatment of type 2 diabetes--a status review.

Sarabu R, Grimsby J.

Curr Opin Drug Discov Devel. 2005 Sep;8(5):631-7. Review.

PMID:
16159025
16.

Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy.

Iino T, Hashimoto N, Sasaki K, Ohyama S, Yoshimoto R, Hosaka H, Hasegawa T, Chiba M, Nagata Y, Eiki J, Nishimura T.

Bioorg Med Chem. 2009 Jun 1;17(11):3800-9. doi: 10.1016/j.bmc.2009.04.040. Epub 2009 Apr 24.

PMID:
19427223
17.

[Salicylic acid derivatives as simplified and novel GK small molecule activators].

Huo LC, Zhang YL, Lei L, Liu SN, Shen ZF, Wang YL, Song HR, Feng ZQ.

Yao Xue Xue Bao. 2013 Apr;48(4):514-20. Chinese.

PMID:
23833938
18.

Identification of YH-GKA, a novel benzamide glucokinase activator as therapeutic candidate for type 2 diabetes mellitus.

Park K.

Arch Pharm Res. 2012 Dec;35(12):2029-33. doi: 10.1007/s12272-012-1201-9. Review.

PMID:
23263798
19.

Glucokinase. Preface.

Lawton G, Witty DR.

Prog Med Chem. 2013;52:v-vii. doi: 10.1016/B978-0-444-62652-3.10000-6. No abstract available.

PMID:
23384669
20.

SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1.

Bertram LS, Black D, Briner PH, Chatfield R, Cooke A, Fyfe MC, Murray PJ, Naud F, Nawano M, Procter MJ, Rakipovski G, Rasamison CM, Reynet C, Schofield KL, Shah VK, Spindler F, Taylor A, Turton R, Williams GM, Wong-Kai-In P, Yasuda K.

J Med Chem. 2008 Jul 24;51(14):4340-5. doi: 10.1021/jm8003202. Epub 2008 Jun 28.

PMID:
18588279
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