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Page 1
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Bungard CJ, Williams PD, Schulz J, Wiscount CM, Holloway MK, Loughran HM, Manikowski JJ, Su HP, Bennett DJ, Chang L, Chu XJ, Crespo A, Dwyer MP, Keertikar K, Morriello GJ, Stamford AW, Waddell ST, Zhong B, Hu B, Ji T, Diamond TL, Bahnck-Teets C, Carroll SS, Fay JF, Min X, Morris W, Ballard JE, Miller MD, McCauley JA. Bungard CJ, et al. Among authors: stamford aw. ACS Med Chem Lett. 2017 Nov 13;8(12):1292-1297. doi: 10.1021/acsmedchemlett.7b00386. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259750 Free PMC article.
Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H, Macala MK, Hu Z, Mei H, Zhang H, Walsh P, Poirier M, Shi ZC, Xiao L, Agnihotri G, Baptista MA, Columbus J, Fell MJ, Hyde LA, Kuvelkar R, Lin Y, Mirescu C, Morrow JA, Yin Z, Zhang X, Zhou X, Chang RK, Embrey MW, Sanders JM, Tiscia HE, Drolet RE, Kern JT, Sur SM, Renger JJ, Bilodeau MT, Kennedy ME, Parker EM, Stamford AW, Nargund R, McCauley JA, Miller MW. Scott JD, et al. Among authors: stamford aw. J Med Chem. 2017 Apr 13;60(7):2983-2992. doi: 10.1021/acs.jmedchem.7b00045. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28245354
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Liu P, Hu Z, DuBois BG, Moyes CR, Hunter DN, Zhu C, Kar NF, Zhu Y, Garfunkle J, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Lamberson J, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Liu P, et al. ACS Med Chem Lett. 2015 Jul 10;6(8):936-41. doi: 10.1021/acsmedchemlett.5b00207. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288697 Free PMC article.
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Cumming J, Babu S, Huang Y, Carrol C, Chen X, Favreau L, Greenlee W, Guo T, Kennedy M, Kuvelkar R, Le T, Li G, McHugh N, Orth P, Ozgur L, Parker E, Saionz K, Stamford A, Strickland C, Tadesse D, Voigt J, Zhang L, Zhang Q. Cumming J, et al. Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20347593
Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.
Neelamkavil SF, Stamford AW, Kowalski T, Biswas D, Boyle C, Chackalamannil S, Xia Y, Jayne C, Neustadt B, Hao J, Liu H, Dai X, Baker H, Hawes B, O'Neill K, Tang H, Greenlee WJ. Neelamkavil SF, et al. Among authors: stamford aw. ACS Med Chem Lett. 2018 Apr 10;9(5):457-461. doi: 10.1021/acsmedchemlett.8b00073. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795759 Free PMC article.
Discovery of phenyl acetamides as potent and selective GPR119 agonists.
Zhu C, Wang L, Zhu Y, Guo ZZ, Liu P, Hu Z, Szewczyk JW, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Orr RK, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Zhu C, et al. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1124-1128. doi: 10.1016/j.bmcl.2017.01.091. Epub 2017 Feb 1. Bioorg Med Chem Lett. 2017. PMID: 28185720
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: stamford aw. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
DeMong D, Dai X, Hwa J, Miller M, Lin SI, Kang L, Stamford A, Greenlee W, Yu W, Wong M, Lavey B, Kozlowski J, Zhou G, Yang DY, Patel B, Soriano A, Zhai Y, Sondey C, Zhang H, Lachowicz J, Grotz D, Cox K, Morrison R, Andreani T, Cao Y, Liang M, Meng T, McNamara P, Wong J, Bradley P, Feng KI, Belani J, Chen P, Dai P, Gauuan J, Lin P, Zhao H. DeMong D, et al. J Med Chem. 2014 Mar 27;57(6):2601-10. doi: 10.1021/jm401858f. Epub 2014 Feb 26. J Med Chem. 2014. PMID: 24527772
60 results