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1Pyrrolizidine Esters and Amides As 5-HT4 Receptor Agonists and Antagonists

DP Becker,DL Flynn,AE Moormann,R Nosal,CI Villamil,R Loeffler,GW Gullikson,C Moummi,DC Yang

A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT(4) and 5-HT(3) receptor binding, 5-HT(4) receptor agonism in the rat tunica muscularis mucosae (TMM) assay, and for 5-HT(3) receptor-mediated functional antagonism in the Bezold-Jarisch reflex assay. Several pyrrolizidine derivatives were identified with high affinity for the 5-HT(4) receptor, including benzamide 12a (SC-53116), a potent and selective 5-HT(4) partial agonist that exhibits efficacy in promoting antral contractions and activity in promoting gastric emptying in canine models. Also discovered were 5-HT(4) receptor antagonists, including imidazopyridine amide 12h (SC-53606), which is a potent and selective 5-HT(4) receptor antagonist with a pA(2) value of 8.13 in the rat TMM assay. N-Methyl indole ester 13d was identified as a potent 5-HT(4) antagonist with a pA(2) value of 8.93. High selectivity was observed for these pyrrolizidine derivatives versus other monoamine receptors, including 5-HT(1), 5-HT(2), D(1), D(2), alpha(1), alpha(2), and beta receptors.

2006JOURNAL OF MEDICINAL CHEMISTRY（2006）引用：44

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2Synthesis and Structure-Activity Relationships of Beta- and Alpha-Piperidine Sulfone Hydroxamic Acid Matrix Metalloproteinase Inhibitors with Oral Antitumor Efficacy.

Daniel P Becker,Clara I Villamil,Thomas E Barta,Louis J Bedell,Terri L Boehm,Gary A Decrescenzo,John N Freskos,Daniel P Getman,Susan Hockerman, Robert Heintz,Susan Carol Howard,Madeleine H Li,

alpha-Piperidine-beta-sulfone hydroxamate derivatives were explored that are potent for matrix metalloproteinases (MMP)-2, -9, and -13 and are sparing of MMP-1. The investigation of the beta-sulfones subsequently led to the discovery of hitherto unknown alpha-sulfone hydroxamates that are superior to the corresponding beta-sulfones in potency for target MMPs, selectivity vs MMP-1, and exposure when dosed orally. alpha-Piperidine-alpha-sulfone hydroxamate 35f (SC-276) was advanced through antitumor and antiangiogenesis assays and was selected for development. Compound 35f demonstrates excellent antitumor activity vs MX-1 breast tumor in mice when dosed orally as monotherapy or in combination with paclitaxel.

2005Journal of medicinal chemistry（2005）引用：71

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3Bridgehead-methyl Analog of SC-53116 As a 5-HT4 Agonist.

DP Becker,DL Flynn,CI Villamil

Pyrrolizidine benzamide (+/-)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (+/-)-2 has an EC50 of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116. (C) 2004 Elsevier Ltd. All rights reserved.

2004Bioorganic & Medicinal Chemistry Letters（2004）引用：22

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4Design and Synthesis of Potent and Selective 4,4-Substituted Alpha-Sulphones Hydroxamates As Mmp Inhibitors.

CI Villamil,DP Becker,TE Barta,LJ Bedell,JJ Talley,SL Hockerman,GE Munie, SY Boyce, CA Swearinger,CL Funckes-Shippy,GA DeCrescenzo,MI Heron,

2002ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（2002）

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5Design And Synthesis Of 4,4-Disubstituted Piperidine Alpha-Sulphone Hydroxamates As Potent And Selective Mmp Inhibitors: The Discovery Of Sc-77964.

Ci Villamil,Te Barta,Dp Becker,Lj Bedell,G Decrescenzo,Jn Freskos,Dp Getman,Cl Funckes-Shippy,Sl Hockerman,Mh Li,Pp Mehta,Ge Munie,

2001ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（2001）

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6Serotonin 5-Ht4 Agonist Activity of A Series of Meso-Azanoradamantane Benzamides

DP Becker,R Nosal,CI Villamil,G Gullikson,C Moummi,DC Yang,DL Flynn

A series of meso-amino(methyl)azanoradamantane benzamides has been prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis mucosae (TMM) assay. Compound 8i is the most potent 5-HT4 agonist in the series, with an EC50 of 217 nM. (C) 1997 Elsevier Science Ltd.

1997BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1997）引用：6

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7Antagonists To The Serotonin 5-Ht4 Receptor Which Are Based On A Pyrrolizidine Scaffold

Dl Flynn,Dp Becker, Dp Spangler,R Nosal,Ci Villamil,Gw Gullikson,Dc Yang

1993ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（1993）

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81,3,4-Trisubstituted Pyrrolidinones As Scaffolds for Construction of Peptidomimetic Cholecystokinin Antagonists

DL FLYNN,CI VILLAMIL,DP BECKER,GW GULLIKSON,C MOUMMI,DC YANG

A new series of cholecystokinin (CCK) antagonists are described which utilizes a new 1,3,4-trisubstituted pyrrolidinone as a scaffold for appending specific amino acid R group mimics (Figure 1). Compound 1A and 1E (SC-50998) exhibit potent nanomolar IC50 values in a CCK-A receptor binding assay. Compound 1E behaves as a competitive antagonist in vitro and is orally active.

1992Bioorganic & Medicinal Chemistry Letters（1992）引用：21

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9Novel Purine Ribosides As Gastrointestinal Prokinetic Agents