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Sharon Sadowski

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Laura C Meurer; Paul E Finke; Karen Owens; Nancy N Tsou; Richard G Ball; Sander G Mills; Malcolm MacCoss; Sharon Sadowski; Margaret A Cascieri; Kwei-Lan Tsao; Gary G Chicchi; Linda A Egger; Silvi Luell; Joseph M Metzger; D Euan MacIntyre; Nadia M J Rupniak; Angela R Williams; Richard Hargreaves
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Paul E Finke; Laura C Meurer; Dorothy A Levorse; Sander G Mills; Malcolm MacCoss; Sharon Sadowski; Margaret A Cascieri; Kwei-Lan Tsao; Gary G Chicchi; Joseph M Metzger; D Euan MacIntyre
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Eileen M Seward; Emma Carlson; Timothy Harrison; Karen R Haworth; Richard Herbert; Fintan J Kelleher; Marc M Kurtz; Jonathan Moseley; Simon N Owen; Andrew P Owens; Sharon Sadowski; Christopher J Swain; Brian J Williams
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.

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All Publications

2006: Laura C Meurer; Paul E Finke; Karen Owens; Nancy N Tsou; Richard G Ball; Sander G Mills; Malcolm MacCoss; Sharon Sadowski; Margaret A Cascieri; Kwei-Lan Tsao; Gary G Chicchi; Linda A Egger; Silvi Luell; Joseph M Metzger; D Euan MacIntyre; Nadia M J Rupniak; Angela R Williams; Richard Hargreaves
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Bioorganic & medicinal chemistry letters 2006;16(17):4504-11.
2006: Paul E Finke; Laura C Meurer; Dorothy A Levorse; Sander G Mills; Malcolm MacCoss; Sharon Sadowski; Margaret A Cascieri; Kwei-Lan Tsao; Gary G Chicchi; Joseph M Metzger; D Euan MacIntyre
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Bioorganic & medicinal chemistry letters 2006;16(17):4497-503.
2002: Eileen M Seward; Emma Carlson; Timothy Harrison; Karen R Haworth; Richard Herbert; Fintan J Kelleher; Marc M Kurtz; Jonathan Moseley; Simon N Owen; Andrew P Owens; Sharon Sadowski; Christopher J Swain; Brian J Williams
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
Bioorganic & medicinal chemistry letters 2002;12(18):2515-8.
2002: Christopher A Willoughby; Steven M Hutchins; Keith G Rosauer; Madhumeeta J Dhar; Kevin Chapman; Gary G Chicchi; Sharon Sadowski; David Weinberg; Smita Patel; Lorraine Malkowitz; Jerry Di Salvo; Stephen G Pacholok; Kang Cheng
Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors.
Bioorganic & medicinal chemistry letters 2002;12(1):93-6.
2001: Timothy Harrison; Andrew P Owens; Brian J Williams; Christopher J Swain; A Williams; Emma J Carlson; Wayne Rycroft; F David Tattersall; Margaret A Cascieri; Gary G Chicchi; Sharon Sadowski; Nadia M J Rupniak; Richard Hargreaves
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
Journal of medicinal chemistry 2001;44(24):4296-9.
2001: Maria A Bednarek; Scott Feighner; Donna L Hreniuk; Oksana C Palyha; Nancy R Morin; Sharon Sadowski; Douglas J MacNeil; Andrew D Howard; Lex H T Van Der Ploeg
Short segment of human melanin-concentrating hormone that is sufficient for full activation of human melanin-concentrating hormone receptors 1 and 2.
Biochemistry 2001;40(31):9379-86.
2001: Andreas W Sailer; Hideki Sano; Zhizhen Zeng; Terrence P McDonald; Jie Pan; Sheng-Shung Pong; Scott Feighner; Carina P Tan; Takehiro Fukami; Hisashi Iwaasa; Donna L Hreniuk; Nancy R Morin; Sharon Sadowski; Masahiko Ito; M Ito; A Bansal; Betty Ky; David Figueroa; Q Jiang; Christopher P Austin; Douglas J MacNeil; Akane Ishihara; Masaki Ihara; Akio Kanatani; Lex H T Van Der Ploeg; Andrew D Howard; Qingyun Liu
Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(13):7564-9.
2000: Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; C P Dorn; Paul E Finke; Richard J Budhu; R A Reamer; Su-Er W Huskey; D Luffer-Atlas; Brian J Dean; Erin McGowan; William P Feeney; Shuet-Hing Lee Chiu; Margaret A Cascieri; Gary G Chicchi; Marc M Kurtz; Sharon Sadowski; E Ber; F David Tattersall; Nadia M J Rupniak; Angela R Williams; Wayne Rycroft; Richard Hargreaves; Joseph M Metzger; D Euan MacIntyre
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
Journal of medicinal chemistry 2000;43(6):1234-41.
2000: F David Tattersall; Wayne Rycroft; Michael J Cumberbatch; Glenn Mason; S Tye; David J Williamson; Jeffrey J Hale; Sander G Mills; Paul E Finke; Malcolm MacCoss; Sharon Sadowski; E Ber; Margaret A Cascieri; Raymond G Hill; D Euan MacIntyre; Richard Hargreaves
The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets.
Neuropharmacology 2000;39(4):652-63.
1999: Margaret A Cascieri; Greg E Koch; E Ber; Sharon Sadowski; D Louizides; Stephen E de Laszlo; C Hacker; William K Hagmann; Malcolm MacCoss; Gary G Chicchi; Pasquale P Vicario
Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
The Journal of biological chemistry 1999;274(13):8694-7.
1998: GI Stevenson; Ian T Huscroft; Angus M MacLeod; Christopher J Swain; Margaret A Cascieri; Gary G Chicchi; M I Graham; Timothy Harrison; Fintan J Kelleher; Marc M Kurtz; Tammy Ladduwahetty; Kevin J Merchant; Joseph M Metzger; D Euan MacIntyre; Sharon Sadowski; Bindi Sohal; Andrew P Owens
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.
Journal of medicinal chemistry 1998;41(23):4623-35.
1998: Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; Paul E Finke; Margaret A Cascieri; Sharon Sadowski; E Ber; Gary G Chicchi; Marc M Kurtz; J Metzger; G Eiermann; Nancy N Tsou; F David Tattersall; Nadia M J Rupniak; Angela R Williams; Wayne Rycroft; Richard Hargreaves; D Euan MacIntyre
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Journal of medicinal chemistry 1998;41(23):4607-14.
1998: Mark S Kramer; N Cutler; J Feighner; R Shrivastava; J Carman; J J Sramek; Scott A Reines; G Liu; Duane Snavely; E Wyatt-Knowles; Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; Christopher J Swain; Timothy Harrison; Raymond G Hill; Franz Hefti; Edward M Scolnick; Margaret A Cascieri; Gary G Chicchi; Sharon Sadowski; Angela R Williams; Louise Hewson; David Smith; Emma J Carlson; Richard Hargreaves; Nadia M J Rupniak
Distinct mechanism for antidepressant activity by blockade of central substance P receptors.
Science (New York, N.Y.) 1998;281(5383):1640-5.
1998: Hongbo Qi; Shrenik K Shah; Margaret A Cascieri; Sharon Sadowski; Malcolm MacCoss
L-tryptophan urea amides as NK1/NK2 dual antagonists.
Bioorganic & medicinal chemistry letters 1998;8(16):2259-62.
1998: Jason M Elliott; Howard B Broughton; Margaret A Cascieri; Gary G Chicchi; Ian T Huscroft; Marc M Kurtz; Angus M MacLeod; Sharon Sadowski; GI Stevenson
Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.
Bioorganic & medicinal chemistry letters 1998;8(14):1851-6.
1998: Jason M Elliott; Margaret A Cascieri; Gary G Chicchi; S Davies; Fintan J Kelleher; Marc M Kurtz; Tammy Ladduwahetty; Richard T Lewis; Angus M MacLeod; Kevin J Merchant; Sharon Sadowski; GI Stevenson
Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.
Bioorganic & medicinal chemistry letters 1998;8(14):1845-50.
1998: Timothy Harrison; M P Korsgaard; Christopher J Swain; Margaret A Cascieri; Sharon Sadowski; Guy R Seabrook
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Bioorganic & medicinal chemistry letters 1998;8(11):1343-8.
1998: Andrew P Owens; Timothy Harrison; J D Moseley; Christopher J Swain; Sharon Sadowski; Margaret A Cascieri
High affinity phenylglycinol-based NK1 receptor antagonists.
Bioorganic & medicinal chemistry letters 1998;8(1):51-6.
1997: Nadia M J Rupniak; F David Tattersall; Angela R Williams; Wayne Rycroft; Emma J Carlson; Margaret A Cascieri; Sharon Sadowski; E Ber; Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; Eileen M Seward; Ian T Huscroft; S Owen; Christopher J Swain; Raymond G Hill; Richard Hargreaves
In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonists.
European journal of pharmacology 1997;326(2-3):201-9.
1997: Margaret A Cascieri; E Ber; Tung M Fong; Jeffrey J Hale; F Tang; LL Shiao; Sander G Mills; Malcolm MacCoss; Sharon Sadowski; Michael R Tota; Catherine D Strader
Characterization of the binding and activity of a high affinity, pseudoirreversible morpholino tachykinin NK1 receptor antagonist.
European journal of pharmacology 1997;325(2-3):253-61.
1996: Tammy Ladduwahetty; R Baker; Margaret A Cascieri; M S Chambers; K Haworth; L E Keown; D Euan MacIntyre; Joseph M Metzger; S Owen; Wayne Rycroft; Sharon Sadowski; E M Seward; Sara Shepheard; Christopher J Swain; F David Tattersall; Alan P Watt; D W Williamson; Richard Hargreaves
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Journal of medicinal chemistry 1996;39(15):2907-14.
1996: Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; S K Shah; H Qi; D J Mathre; Margaret A Cascieri; Sharon Sadowski; Catherine D Strader; D Euan MacIntyre; Joseph M Metzger
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Journal of medicinal chemistry 1996;39(9):1760-2.
1995: GI Stevenson; Angus M MacLeod; Ian T Huscroft; Margaret A Cascieri; Sharon Sadowski; R Baker
4,4-Disubstituted piperidines: a new class of NK1 antagonist.
Journal of medicinal chemistry 1995;38(8):1264-6.
1995: Margaret A Cascieri; LL Shiao; Sander G Mills; Malcolm MacCoss; Christopher J Swain; H Yu; E Ber; Sharon Sadowski; M T Wu; Catherine D Strader
Characterization of the interaction of diacylpiperazine antagonists with the human neurokinin-1 receptor: identification of a common binding site for structurally dissimilar antagonists.
Molecular pharmacology 1995;47(4):660-5.
1995: R T Lewis; Angus M MacLeod; Kevin J Merchant; F Kelleher; I Sanderson; R H Herbert; Margaret A Cascieri; Sharon Sadowski; R G Ball; K Hoogsteen
Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.
Journal of medicinal chemistry 1995;38(6):923-33.
1995: Angus M MacLeod; Margaret A Cascieri; Kevin J Merchant; Sharon Sadowski; S Hardwicke; R T Lewis; D Euan MacIntyre; Joseph M Metzger; Tung M Fong; Sara Shepheard
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
Journal of medicinal chemistry 1995;38(6):934-41.
1994: Angus M MacLeod; Kevin J Merchant; F Brookfield; F Kelleher; G Stevenson; Andrew P Owens; Christopher J Swain; M A Casiceri; Sharon Sadowski; E Ber
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
Journal of medicinal chemistry 1994;37(9):1269-74.
1994: Margaret A Cascieri; Angus M MacLeod; D Underwood; LL Shiao; E Ber; Sharon Sadowski; H Yu; Kevin J Merchant; Christopher J Swain; Catherine D Strader
Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor.
The Journal of biological chemistry 1994;269(9):6587-91.
1993: Angus M MacLeod; Kevin J Merchant; Margaret A Cascieri; Sharon Sadowski; E Ber; Christopher J Swain; R Baker
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
Journal of medicinal chemistry 1993;36(14):2044-5.
1993: Sharon Sadowski; Ruey-Ruey C Huang; Tung M Fong; O Marko; Margaret A Cascieri
Characterization of the binding of [125I-iodo-histidyl, methyl-Phe7] neurokinin B to the neurokinin-3 receptor.
Neuropeptides 1993;24(6):317-9.
1992: Margaret A Cascieri; E Ber; Tung M Fong; Sharon Sadowski; A Bansal; Christopher J Swain; E Seward; B Frances; D Burns; Catherine D Strader
Characterization of the binding of a potent, selective, radioiodinated antagonist to the human neurokinin-1 receptor.
Molecular pharmacology 1992;42(3):458-63.
1992: Margaret A Cascieri; Ruey-Ruey C Huang; Tung M Fong; A H Cheung; Sharon Sadowski; E Ber; Catherine D Strader
Determination of the amino acid residues in substance P conferring selectivity and specificity for the rat neurokinin receptors.
Molecular pharmacology 1992;41(6):1096-9.