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Items: 33

1.

A Novel Aldosterone Antagonist Limits Renal Injury in 5/6 Nephrectomy.

Fujihara CK, Kowala MC, Breyer MD, Sena CR, Rodrigues MV, Arias SCA, Fanelli C, Malheiros DM, Jadhav PK, Montrose-Rafizadeh C, Krieger JE, Zatz R.

Sci Rep. 2017 Aug 11;7(1):7899. doi: 10.1038/s41598-017-08383-2.

2.

ESR and X-ray Structure Investigations on the Binding and Mechanism of Inhibition of the Native State of Myeloperoxidase with Low Molecular Weight Fragments.

Chavali B, Masquelin T, Nilges MJ, Timm DE, Stout SL, Matter WF, Jin N, Jadhav PK, Deng GG.

Appl Magn Reson. 2015;46(8):853-873. Epub 2015 May 19.

3.

Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.

Jadhav PK, Schiffler MA, Gavardinas K, Kim EJ, Matthews DP, Staszak MA, Coffey DS, Shaw BW, Cassidy KC, Brier RA, Zhang Y, Christie RM, Matter WF, Qing K, Durbin JD, Wang Y, Deng GG.

ACS Med Chem Lett. 2014 Aug 27;5(10):1138-42. doi: 10.1021/ml500283g. eCollection 2014 Oct 9.

4.

(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.

Bell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK.

J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.

PMID:
18038968
5.

3,3-Bisaryloxindoles as mineralocorticoid receptor antagonists.

Neel DA, Brown ML, Lander PA, Grese TA, Defauw JM, Doti RA, Fields T, Kelley SA, Smith S, Zimmerman KM, Steinberg MI, Jadhav PK.

Bioorg Med Chem Lett. 2005 May 16;15(10):2553-7.

PMID:
15863315
6.

5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.

Qiao JX, Cheng X, Modi DP, Rossi KA, Luettgen JM, Knabb RM, Jadhav PK, Wexler RR.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):29-35.

PMID:
15582405
7.

5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.

Batt DG, Qiao JX, Modi DP, Houghton GC, Pierson DA, Rossi KA, Luettgen JM, Knabb RM, Jadhav PK, Wexler RR.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5269-73.

PMID:
15454209
8.

SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.

Smallheer JM, Alexander RS, Wang J, Wang S, Nakajima S, Rossi KA, Smallwood A, Barbera F, Burdick D, Luettgen JM, Knabb RM, Wexler RR, Jadhav PK.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5263-7.

PMID:
15454208
9.

Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.

Smallheer JM, Weigelt CA, Woerner FJ, Wells JS, Daneker WF, Mousa SA, Wexler RR, Jadhav PK.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):383-7.

PMID:
14698164
10.

Inhibition of human endogenous retrovirus-K10 protease in cell-free and cell-based assays.

Kuhelj R, Rizzo CJ, Chang CH, Jadhav PK, Towler EM, Korant BD.

J Biol Chem. 2001 May 18;276(20):16674-82. Epub 2001 Feb 21.

11.

Synthesis of cis and trans isomers of an isoxazoline ring-hydroxylated metabolite of roxifiban, a platelet glycoprotein IIb/IIIa receptor antagonist.

Batt DG, Houghton GC, Daneker WF, Jadhav PK.

J Org Chem. 2000 Nov 17;65(23):8100-4. No abstract available.

PMID:
11073629
12.

Inhibition of neointima formation by a nonpeptide alpha(v)beta(3) integrin receptor antagonist in a rabbit cuff model.

Racanelli AL, Gibbs SK, Schlingmann KL, Corjay MH, Jadhav PK, Reilly TM.

J Cell Biochem. 2000 Mar;77(2):213-20.

PMID:
10723088
13.

Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).

Batt DG, Petraitis JJ, Houghton GC, Modi DP, Cain GA, Corjay MH, Mousa SA, Bouchard PJ, Forsythe MS, Harlow PP, Barbera FA, Spitz SM, Wexler RR, Jadhav PK.

J Med Chem. 2000 Jan 13;43(1):41-58.

PMID:
10633037
14.

Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).

Pitts WJ, Wityak J, Smallheer JM, Tobin AE, Jetter JW, Buynitsky JS, Harlow PP, Solomon KA, Corjay MH, Mousa SA, Wexler RR, Jadhav PK.

J Med Chem. 2000 Jan 13;43(1):27-40.

PMID:
10633036
15.

Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.

Rockwell AL, Rafalski M, Pitts WJ, Batt DG, Petraitis JJ, DeGrado WF, Mousa S, Jadhav PK.

Bioorg Med Chem Lett. 1999 Apr 5;9(7):937-42.

PMID:
10230615
16.

Alphavbeta3 integrin binding affinity and specificity of SM256 in various species.

Mousa SA, Lorelli W, Mohamed S, Batt DG, Jadhav PK, Reilly TM.

J Cardiovasc Pharmacol. 1999 Apr;33(4):641-6.

PMID:
10218736
17.

The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.

Patel M, Kaltenbach RF 3rd, Nugiel DA, McHugh RJ Jr, Jadhav PK, Bacheler LT, Cordova BC, Klabe RM, Erickson-Viitanen S, Garber S, Reid C, Seitz SP.

Bioorg Med Chem Lett. 1998 May 5;8(9):1077-82.

PMID:
9871711
18.
19.

De novo design and discovery of cyclic HIV protease inhibitors capable of displacing the active-site structural water molecule.

De Lucca GV, Jadhav PK, Waltermire RE, Aungst BJ, Erickson-Viitanen S, Lam PY.

Pharm Biotechnol. 1998;11:257-84. Review. No abstract available.

PMID:
9760684
20.

Molecular recognition of cyclic urea HIV-1 protease inhibitors.

Ala PJ, DeLoskey RJ, Huston EE, Jadhav PK, Lam PY, Eyermann CJ, Hodge CN, Schadt MC, Lewandowski FA, Weber PC, McCabe DD, Duke JL, Chang CH.

J Biol Chem. 1998 May 15;273(20):12325-31.

21.

Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.

Han Q, Chang CH, Li R, Ru Y, Jadhav PK, Lam PY.

J Med Chem. 1998 Jun 4;41(12):2019-28.

PMID:
9622543
22.

Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.

Jadhav PK, Woerner FJ, Lam PY, Hodge CN, Eyermann CJ, Man HW, Daneker WF, Bacheler LT, Rayner MM, Meek JL, Erickson-Viitanen S, Jackson DA, Calabrese JC, Schadt M, Chang CH.

J Med Chem. 1998 Apr 23;41(9):1446-55.

PMID:
9554878
23.

Improved P1/P1' substituents for cyclic urea based HIV-1 protease inhibitors: synthesis, structure-activity relationship, and X-ray crystal structure analysis.

Nugiel DA, Jacobs K, Cornelius L, Chang CH, Jadhav PK, Holler ER, Klabe RM, Bacheler LT, Cordova B, Garber S, Reid C, Logue KA, Gorey-Feret LJ, Lam GN, Erickson-Viitanen S, Seitz SP.

J Med Chem. 1997 May 9;40(10):1465-74.

PMID:
9154969
24.

Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.

Jadhav PK, Ala P, Woerner FJ, Chang CH, Garber SS, Anton ED, Bacheler LT.

J Med Chem. 1997 Jan 17;40(2):181-91.

PMID:
9003516
25.

Direct Synthesis of [alpha-[(tert-Butoxycarbonyl)amino]alkyl]- boronates from (alpha-Haloalkyl)boronates.

Jadhav PK, Man HW.

J Org Chem. 1996 Nov 1;61(22):7951-7954. No abstract available.

PMID:
11667760
26.

Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.

Lam PY, Ru Y, Jadhav PK, Aldrich PE, DeLucca GV, Eyermann CJ, Chang CH, Emmett G, Holler ER, Daneker WF, Li L, Confalone PN, McHugh RJ, Han Q, Li R, Markwalder JA, Seitz SP, Sharpe TR, Bacheler LT, Rayner MM, Klabe RM, Shum L, Winslow DL, Kornhauser DM, Hodge CN, et al.

J Med Chem. 1996 Aug 30;39(18):3514-25.

PMID:
8784449
27.

Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors.

Nugiel DA, Jacobs K, Kaltenbach RF, Worley T, Patel M, Meyer DT, Jadhav PK, De Lucca GV, Smyser TE, Klabe RM, Bacheler LT, Rayner MM, Seitz SP.

J Med Chem. 1996 May 24;39(11):2156-69.

PMID:
8667359
28.

Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450.

Hodge CN, Aldrich PE, Bacheler LT, Chang CH, Eyermann CJ, Garber S, Grubb M, Jackson DA, Jadhav PK, Korant B, Lam PY, Maurin MB, Meek JL, Otto MJ, Rayner MM, Reid C, Sharpe TR, Shum L, Winslow DL, Erickson-Viitanen S.

Chem Biol. 1996 Apr;3(4):301-14.

29.

Stereoselective Synthesis of HIV-1 Protease Inhibitor, DMP 323.

Pierce ME, Harris GD, Islam Q, Radesca LA, Storace L, Waltermire RE, Wat E, Jadhav PK, Emmett GC.

J Org Chem. 1996 Jan 26;61(2):444-450.

PMID:
11666958
30.

Flexibility and function in HIV-1 protease.

Nicholson LK, Yamazaki T, Torchia DA, Grzesiek S, Bax A, Stahl SJ, Kaufman JD, Wingfield PT, Lam PY, Jadhav PK, et al.

Nat Struct Biol. 1995 Apr;2(4):274-80.

PMID:
7796263
31.
32.

Rational design of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors.

Lam PY, Jadhav PK, Eyermann CJ, Hodge CN, Ru Y, Bacheler LT, Meek JL, Otto MJ, Rayner MM, Wong YN, et al.

Science. 1994 Jan 21;263(5145):380-4.

PMID:
8278812
33.

In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitors of HIV type 1 protease.

Otto MJ, Garber S, Winslow DL, Reid CD, Aldrich P, Jadhav PK, Patterson CE, Hodge CN, Cheng YS.

Proc Natl Acad Sci U S A. 1993 Aug 15;90(16):7543-7.

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