Search Results - "Marcopulos, Nicholas"

4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists by Cheung, Adrian Wai-Hing, Brinkman, John, Firooznia, Fariborz, Flohr, Alexander, Grimsby, Joseph, Gubler, Mary Lou, Guertin, Kevin, Hamid, Rachid, Marcopulos, Nicholas, Norcross, Roger D., Qi, Lida, Ramsey, Gwendolyn, Tan, Jenny, Wen, Yang, Sarabu, Ramakanth

“…7-N-Acetamide-4-methoxy-2-aminobenzothiazole 4-fluorobenzamide (compound 1) was chosen as a drug-like and non-xanthine based starting point for the discovery…”
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Application of 5-lithiotetrazoles in organic synthesis by Satoh, Yoshitaka, Marcopulos, Nicholas

“…Lithiation of 1-benzyl and 1- p-methoxybenzyltetrazole at the 5-position with n-butyllithium followed by treatment with electrophiles gave functionalized…”
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Enantioselective synthesis of 4-substituted phenylalanines by cross-coupling reactions by Firooznia, Fariborz, Gude, Candido, Chan, Kenneth, Marcopulos, Nicholas, Satoh, Yoshitaka

“…The enantiomerically enriched BOC-protected (4-pinacolylborono)phenylalanine methyl ester ( 8) is produced via enzymatic resolution of the racemic material, or…”
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Design and Synthesis of Potent, Selective Inhibitors of Endothelin-Converting Enzyme by Wallace, Eli M, Moliterni, John A, Moskal, Michael A, Neubert, Alan D, Marcopulos, Nicholas, Stamford, Lisa B, Trapani, Angelo J, Savage, Paula, Chou, Mary, Jeng, Arco Y

“…Endothelin-1 is the most potent peptidic vasoconstrictor discovered to date. The final step of posttranslational processing of this peptide is the conversion…”
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Discovery of Orally Active Carboxylic Acid Derivatives of 2-Phenyl-5-trifluoromethyloxazole-4-carboxamide as Potent Diacylglycerol Acyltransferase-1 Inhibitors for the Potential Treatment of Obesity and Diabetes by Qian, Yimin, Wertheimer, Stanley J, Ahmad, Mushtaq, Cheung, Adrian Wai-Hing, Firooznia, Fariborz, Hamilton, Matthew M, Hayden, Stuart, Li, Shiming, Marcopulos, Nicholas, McDermott, Lee, Tan, Jenny, Yun, Weiya, Guo, Liang, Pamidimukkala, Anjula, Chen, Yingsi, Huang, Kuo-Sen, Ramsey, Gwendolyn B, Whittard, Toni, Conde-Knape, Karin, Taub, Rebecca, Rondinone, Cristina M, Tilley, Jefferson, Bolin, David

“…Diacylglycerol acyltransferase-1 (DGAT-1) is the enzyme that catalyzes the final and committed step of triglyceride formation, namely, the acylation of…”
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7-Phenyl-pyrido[2,3-d]pyrimidine-2,4-diamines: Novel and highly selective protein tyrosine phosphatase 1B inhibitors by Cheung, Adrian Wai-Hing, Banner, Bruce, Bose, Jolly, Kim, Kyungjin, Li, Shiming, Marcopulos, Nicholas, Orzechowski, Lucja, Sergi, Joseph A., Thakkar, Kshitij C., Wang, Bing-Bing, Yun, Weiya, Zwingelstein, Catherine, Berthel, Steven, Olivier, Andrée R.

“…High throughput screening of the Roche compound collection led to the identification of diaminopyrroloquinazoline series as a novel class of PTP1B inhibitors…”
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Synthesis and selective class III antiarrhythmic activity of novel N-heteroaralkyl-substituted 1-(aryloxy)-2-propanolamine and related propylamine derivatives by Butera, John A, Spinelli, Walter, Anantharaman, Viji, Marcopulos, Nicholas, Parsons, Roderick W, Moubarak, Issam F, Cullinan, Catherine, Bagli, Jehan F

“…The synthesis and biological evaluation of a series of novel 1-(aryloxy)-2-propanolamines and several related deshydroxy analogues are described. Compounds…”
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Discovery of benzothiazole-based adenosine A₂B receptor antagonists with improved A₂A selectivity by Firooznia, Fariborz, Cheung, Adrian Wai-Hing, Brinkman, John, Grimsby, Joseph, Gubler, Mary Lou, Hamid, Rachid, Marcopulos, Nicholas, Ramsey, Gwendolyn, Tan, Jenny, Wen, Yang, Sarabu, Ramakanth

“…The highly potent but modestly selective N-(2-amino-4-methoxy-benzothiazol-7-yl)-N-ethyl-acetamide derivative 2 was selected as the starting point for the…”
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Discovery of benzothiazole-based adenosine A sub(2B receptor antagonists with improved A) sub(2)A selectivity by Firooznia, Fariborz, Cheung, Adrian Wai-Hing, Brinkman, John, Grimsby, Joseph, Gubler, Mary Lou, Hamid, Rachid, Marcopulos, Nicholas, Ramsey, Gwendolyn, Tan, Jenny, Wen, Yang, Sarabu, Ramakanth

“…The highly potent but modestly selective N-(2-amino-4-methoxy-benzothiazol-7-yl)-N-ethyl-acetamide derivative 2 was selected as the starting point for the…”
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Discovery of benzothiazole-based adenosine A 2B receptor antagonists with improved A 2A selectivity by Firooznia, Fariborz, Cheung, Adrian Wai-Hing, Brinkman, John, Grimsby, Joseph, Gubler, Mary Lou, Hamid, Rachid, Marcopulos, Nicholas, Ramsey, Gwendolyn, Tan, Jenny, Wen, Yang, Sarabu, Ramakanth

“…The highly potent but modestly selective N-(2-amino-4-methoxy-benzothiazol-7-yl)- N-ethyl-acetamide derivative 2 was selected as the starting point for the…”
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4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A sub(2B) adenosine receptor antagonists by Cheung, Adrian Wai-Hing, Brinkman, John, Firooznia, Fariborz, Flohr, Alexander, Grimsby, Joseph, Gubler, Mary Lou, Guertin, Kevin, Hamid, Rachid, Marcopulos, Nicholas, Norcross, Roger D, Qi, Lida, Ramsey, Gwendolyn, Tan, Jenny, Wen, Yang, Sarabu, Ramakanth

“…7-N-Acetamide-4-methoxy-2-aminobenzothiazole 4-fluorobenzamide (compound 1) was chosen as a drug-like and non-xanthine based starting point for the discovery…”
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Perhydroquinolylbenzamides as Novel Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 by Coppola, Gary M, Kukkola, Paivi J, Stanton, James L, Neubert, Alan D, Marcopulos, Nicholas, Bilci, Natalie A, Wang, Hua, Tomaselli, Hollis C, Tan, Jenny, Aicher, Thomas D, Knorr, Douglas C, Jeng, Arco Y, Dardik, Beatriz, Chatelain, Ricardo E

“…High-throughput screening identified 5 as a weak inhibitor of 11β-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some with…”
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Perhydroquinolylbenzamides as novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by Coppola, Gary M, Kukkola, Paivi J, Stanton, James L, Neubert, Alan D, Marcopulos, Nicholas, Bilci, Natalie A, Wang, Hua, Tomaselli, Hollis C, Tan, Jenny, Aicher, Thomas D, Knorr, Douglas C, Jeng, Arco Y, Dardik, Beatriz, Chatelain, Ricardo E

“…High-throughput screening identified 5 as a weak inhibitor of 11beta-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some…”
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Synthesis of tetrazole analogs of α-amino acids by alkylation of a Schiff base of α-aminomethyltetrazole by Satoh, Yoshitaka, De Lombaert, Stéphane, Marcopulos, Nicholas, Moliterni, John, Moskal, Michael, Tan, Jenny, Wallace, Eli

“…A benzophenone imine of N-1 protected α-aminomethyltetrazoles was found to undergo alkylation with organic halides in good yields. Deprotection afforded…”
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Diels-Alder reactions of dieno-pyranosides. Anomeric vs allylic stereoselection by GIULIANO, R. M, BUZBY, J. H, MARCOPULOS, N, SPRINGER, J. P

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Diels-Alder reactions of dieno-pyranosides. Anomeric versus allylic stereoselection by Giuliano, Robert M, Buzby, John H, Marcopulos, Nicholas, Springer, James P

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