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Items: 1 to 20 of 36

1.

Impacting Global Health Through Equipment Repurposing: Measurable Progress Through the Accumulation of Many Tiny Victories.

Buist NL, Minnihan EC, Young K, Yang L.

J Pharm Sci. 2018 Mar;107(3):788-793. doi: 10.1016/j.xphs.2017.10.016. Epub 2017 Oct 24.

PMID:
29074379
2.

Linking High-Throughput Screens to Identify MoAs and Novel Inhibitors of Mycobacterium tuberculosis Dihydrofolate Reductase.

Santa Maria JP Jr, Park Y, Yang L, Murgolo N, Altman MD, Zuck P, Adam G, Chamberlin C, Saradjian P, Dandliker P, Boshoff HIM, Barry CE 3rd, Garlisi C, Olsen DB, Young K, Glick M, Nickbarg E, Kutchukian PS.

ACS Chem Biol. 2017 Sep 15;12(9):2448-2456. doi: 10.1021/acschembio.7b00468. Epub 2017 Aug 29.

3.

Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.

Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24.

PMID:
27839686
4.

Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.

Tang H, Zhu Y, Teumelsan N, Walsh SP, Shahripour A, Priest BT, Swensen AM, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Pai LY, Hampton C, Corona A, Hernandez M, Metzger J, Forrest M, Zhou X, Owens K, Tong V, Parmee E, Roy S, Kaczorowski GJ, Yang L, Alonso-Galicia M, Garcia ML, Pasternak A.

ACS Med Chem Lett. 2016 May 12;7(7):697-701. doi: 10.1021/acsmedchemlett.6b00122. eCollection 2016 Jul 14.

5.

Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.

Walsh SP, Shahripour A, Tang H, de Jesus RK, Teumelsan N, Zhu Y, Frie J, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A.

Bioorg Med Chem Lett. 2016 May 1;26(9):2339-43. doi: 10.1016/j.bmcl.2016.03.035. Epub 2016 Mar 12.

PMID:
27017115
6.

Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

Lin S, Malkani S, Lombardo M, Yang L, Mills SG, Chapman K, Thompson JE, Zhang WX, Wang R, Cubbon RM, O'Neill EA, Hale JJ.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5402-8. doi: 10.1016/j.bmcl.2015.09.016. Epub 2015 Sep 8.

PMID:
26403928
7.

The role of anthropogenic and natural factors in shaping the geochemical evolution of groundwater in the Subei Lake basin, Ordos energy base, Northwestern China.

Liu F, Song X, Yang L, Han D, Zhang Y, Ma Y, Bu H.

Sci Total Environ. 2015 Dec 15;538:327-40. doi: 10.1016/j.scitotenv.2015.08.057. Epub 2015 Aug 24.

PMID:
26312407
8.

Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.

Walsh SP, Shahripour A, Tang H, Teumelsan N, Frie J, Zhu Y, Priest BT, Swensen AM, Liu J, Margulis M, Visconti R, Weinglass A, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Alonso-Galicia M, Zhou X, Pai LY, Corona A, Hampton C, Hernandez M, Bentley R, Chen J, Shah K, Metzger J, Forrest M, Owens K, Tong V, Ha S, Roy S, Kaczorowski GJ, Yang L, Parmee E, Garcia ML, Sullivan K, Pasternak A.

ACS Med Chem Lett. 2015 May 7;6(7):747-52. doi: 10.1021/ml500440u. eCollection 2015 Jul 9.

9.

Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl)ethyl)isobenzofuran-1(3H)-one.

Tang H, de Jesus RK, Walsh SP, Zhu Y, Yan Y, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5829-32. doi: 10.1016/j.bmcl.2013.08.104. Epub 2013 Sep 6.

PMID:
24075732
10.

The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.

He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK.

ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14.

11.

Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.

Tang H, Walsh SP, Yan Y, de Jesus RK, Shahripour A, Teumelsan N, Zhu Y, Ha S, Owens KA, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest BT, Bailey T, Brochu R, Alonso-Galicia M, Kaczorowski GJ, Roy S, Yang L, Mills SG, Garcia ML, Pasternak A.

ACS Med Chem Lett. 2012 Mar 28;3(5):367-72. doi: 10.1021/ml3000066. eCollection 2012 May 10.

12.

Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.

Pasternak A, Feng Z, de Jesus R, Ye Z, He S, Dobbelaar P, Bradley SA, Chicchi GG, Tsao KL, Trusca D, Eiermann GJ, Li C, Feng Y, Wu M, Shao Q, Zhang BB, Nargund R, Mills SG, Howard AD, Yang L, Zhou YP.

ACS Med Chem Lett. 2012 Feb 27;3(4):289-93. doi: 10.1021/ml200272z. eCollection 2012 Apr 12.

13.

3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.

Walsh SP, Severino A, Zhou C, He J, Liang GB, Tan CP, Cao J, Eiermann GJ, Xu L, Salituro G, Howard AD, Mills SG, Yang L.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3390-4. doi: 10.1016/j.bmcl.2011.03.114. Epub 2011 Apr 8.

PMID:
21514824
14.

Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.

Zhou C, Garcia-Calvo M, Pinto S, Lombardo M, Feng Z, Bender K, Pryor KD, Bhatt UR, Chabin RM, Geissler WM, Shen Z, Tong X, Zhang Z, Wong KK, Roy RS, Chapman KT, Yang L, Xiong Y.

J Med Chem. 2010 Oct 14;53(19):7251-63. doi: 10.1021/jm101013m.

PMID:
20857914
15.

Dual targeting of CCR2 and CX3CR1 in an arterial injury model of vascular inflammation.

Jerath MR, Liu P, Struthers M, Demartino JA, Peng R, Peterson LB, Cumiskey AM, Yang L, Rojas M, Patel DD, Fong AM.

Thromb J. 2010 Sep 13;8:14. doi: 10.1186/1477-9560-8-14.

16.

Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.

Tang H, Yan Y, Feng Z, de Jesus RK, Yang L, Levorse DA, Owens KA, Akiyama TE, Bergeron R, Castriota GA, Doebber TW, Ellsworth KP, Lassman ME, Li C, Wu MS, Zhang BB, Chapman KT, Mills SG, Berger JP, Pasternak A.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6088-92. doi: 10.1016/j.bmcl.2010.08.047. Epub 2010 Aug 20.

PMID:
20832306
17.

Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.

Zhou C, Tang C, Chang E, Ge M, Lin S, Cline E, Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger J, Howard AD, Thornberry N, Mills SG, Yang L.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1298-301. doi: 10.1016/j.bmcl.2009.10.052. Epub 2009 Oct 15.

PMID:
20064714
18.

Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.

Pasternak A, Goble SD, deJesus RK, Hreniuk DL, Chung CC, Tota MR, Mazur P, Feighner SD, Howard AD, Mills SG, Yang L.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6237-40. doi: 10.1016/j.bmcl.2009.08.076. Epub 2009 Aug 26.

PMID:
19767208
19.

Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

Lin S, Lombardo M, Malkani S, Hale JJ, Mills SG, Chapman K, Thompson JE, Zhang WX, Wang R, Cubbon RM, O'Neill EA, Luell S, Carballo-Jane E, Yang L.

Bioorg Med Chem Lett. 2009 Jun 15;19(12):3238-42. doi: 10.1016/j.bmcl.2009.04.088. Epub 2009 Apr 24.

PMID:
19423344
20.

Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists.

Sakamoto T, Moriya M, Haga Y, Takahashi T, Shibata T, Okamoto O, Nonoshita K, Kitazawa H, Hidaka M, Gomori A, Iwaasa H, Ishihara A, Kanatani A, Fukami T, Gao YD, Macneil DJ, Yang L.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1564-8. doi: 10.1016/j.bmcl.2009.02.035. Epub 2009 Feb 12.

PMID:
19243937

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