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Author Report for: Djuric SW

Title: 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 and Trevillyan JM <21 more author(s)> 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 (- 21)
Ref: Journal of Medicinal Chemistry, 49:6416, 2006 : PubMed
Abstract


ESTHER: Madar_2006_J.Med.Chem_49_6416
PubMedSearch: Madar 2006 J.Med.Chem 49 6416
PubMedID: 17034148
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: ABT-279

Abstract

Dipeptidyl peptidase-IV (DPP-IV) inhibitors are poised to be the next major drug class for the treatment of type 2 diabetes. Structure-activity studies of substitutions at the C5 position of the 2-cyanopyrrolidide warhead led to the discovery of potent inhibitors of DPP-IV that lack activity against DPP8 and DPP9. Further modification led to an extremely potent (Ki(DPP)(-)(IV) = 1.0 nM) and selective (Ki(DPP8) > 30 microM; Ki(DPP9) > 30 microM) clinical candidate, ABT-279, that is orally available, efficacious, and remarkably safe in preclinical safety studies.



        

Title: Synthesis and antibacterial activity of 6-O-arylpropargyl-9-oxime-11,12-carbamate ketolides
Beebe X, Yang F, Bui MH, Mitten MJ, Ma Z, Nilius AM, Djuric SW
Ref: Bioorganic & Medicinal Chemistry Lett, 14:2417, 2004 : PubMed
Abstract


ESTHER: Beebe_2004_Bioorg.Med.Chem.Lett_14_2417
PubMedSearch: Beebe 2004 Bioorg.Med.Chem.Lett 14 2417
PubMedID: 15109624

Abstract

A series of novel 6-O-arylpropargyl-9-oxime-ketolides was synthesized and evaluated against various pathogens. These new compounds show promising in vitro antibacterial potency and in vivo efficacy against macrolide resistant strains.



        

Title: Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Malecha JW, Miyashiro JM, Russell MA, Askonas LJ and Smith WG <8 more author(s)> Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Malecha JW, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG (- 8)
Ref: Bioorganic & Medicinal Chemistry Lett, 13:1137, 2003 : PubMed
Abstract


ESTHER: Penning_2003_Bioorg.Med.Chem.Lett_13_1137
PubMedSearch: Penning 2003 Bioorg.Med.Chem.Lett 13 1137
PubMedID: 12643929

Abstract

The synthesis and biological evaluation of a series of heterocyclic analogues of the previously reported LTA(4) hydrolase inhibitor 1b are described. Imidazopyridine and purine analogues are specifically highlighted with several demonstrating excellent potency in our in vitro assays, as well as good oral activity in a mouse ex vivo assay.



        

Title: Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ and Smith WG <8 more author(s)> Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG (- 8)
Ref: Bioorganic & Medicinal Chemistry Lett, 12:3383, 2002 : PubMed
Abstract


ESTHER: Penning_2002_Bioorg.Med.Chem.Lett_12_3383
PubMedSearch: Penning 2002 Bioorg.Med.Chem.Lett 12 3383
PubMedID: 12419366

Abstract

The synthesis and biological evaluation of a series of functionalized pyrrolidine- and piperidine-containing analogues of our lead LTA(4) hydrolase inhibitor, SC-57461A, is described. A number of compounds showed excellent potency in our in vitro screens and several demonstrated good oral activity in a mouse ex vivo assay. These efforts led to the identification of SC-56938 (14) as a potent, orally active inhibitor of LTA(4) hydrolase.



        

Title: Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase
Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA and Smith WG <16 more author(s)> Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA, Miyashiro JM, Russell MA, Yu SS, Corley DG, Durley RC, Kilpatrick BF, Parnas BL, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Krivi GG, Villani-Price D, Pyla EY, Smith WG (- 16)
Ref: Journal of Medicinal Chemistry, 43:721, 2000 : PubMed
Abstract


ESTHER: Penning_2000_J.Med.Chem_43_721
PubMedSearch: Penning 2000 J.Med.Chem 43 721
PubMedID: 10691697

Abstract

Leukotriene B(4) (LTB(4)) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA(4) hydrolase is the rate-limiting step for LTB(4) production, this enzyme represents an attractive pharmacological target for the suppression of LTB(4) production. From an in-house screening program, SC-22716 (1, 1-[2-(4-phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA(4) hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA(4) hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.