Search Results - "PALOVICH, Michael"

Quality guidelines for oral drug candidates: dose, solubility and lipophilicity by Bayliss, Martin K., Butler, James, Feldman, Paul L., Green, Darren V.S., Leeson, Paul D., Palovich, Michael R., Taylor, Anthony J.

“…[Display omitted] •Experimental properties of GSK's oral portfolio were compared with marketed drugs.•Properties were dose, solubility and the property…”
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Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases by Salmon, Michael, Luttmann, Mark A, Foley, James J, Buckley, Peter T, Schmidt, Dulcie B, Burman, Miriam, Webb, Edward F, DeHaas, Christopher J, Kotzer, Charles J, Barrett, Victoria J, Slack, Robert J, Sarau, Henry M, Palovich, Michael R, Lainé, Dramane I, Hay, Douglas W P, Rumsey, William L

“…Activation of muscarinic subtype 3 (M3) muscarinic cholinergic receptors (mAChRs) increases airway tone, whereas its blockade improves lung function and…”
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Discovery of Novel 1-Azoniabicyclo[2.2.2]octane Muscarinic Acetylcholine Receptor Antagonists by Lainé, Dramane I, McCleland, Brent, Thomas, Sonia, Neipp, Christopher, Underwood, Brian, Dufour, Jeremy, Widdowson, Katherine L, Palovich, Michael R, Blaney, Frank E, Foley, James J, Webb, Edward F, Luttmann, Mark A, Burman, Miriam, Belmonte, Kristen, Salmon, Michael

“…A novel 4-hydroxyl(diphenyl)methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure−activity…”
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Tyrosine urea muscarinic acetylcholine receptor antagonists: Achiral quaternary ammonium groups by Jin, Qi, Davis, Roderick S., Bullion, Ann M., Jin, Jian, Wang, Yonghui, Widdowson, Katherine L., Palovich, Michael R., Foley, James J., Schmidt, Dulcie B., Buckley, Peter T., Webb, Edward F., Salmon, Michael, Belmonte, Kristen E., Sarau, Henry M., Busch-Petersen, Jakob

“…Novel tyrosine-based, long-acting inhaled muscarinic antagonists: preparation, SAR and biological evaluation. Tyrosine ureas had been identified as potent…”
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Design, synthesis and structure–activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists by Lainé, Dramane I., Yan, Hongxing, Xie, Haibo, Davis, Roderick S., Dufour, Jeremy, Widdowson, Katherine L., Palovich, Michael R., Wan, Zehong, Foley, James J., Schmidt, Dulcie B., Hunsberger, Gerald E., Burman, Miriam, Bacon, Alicia M., Webb, Edward F., Luttmann, Mark A., Salmon, Michael, Sarau, Henry M., Umbrecht, Sandra T., Landis, Philip S., Peck, Brian J., Busch-Petersen, Jakob

“…Novel tropane-based, ultra long-acting inhaled muscarinic antagonists: preparation, biological evaluation and developability. A novel series of N-substituted…”
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Comparison of N, N′-diarylsquaramides and N, N′-diarylureas as antagonists of the CXCR2 chemokine receptor by McCleland, Brent W., Davis, Roderick S., Palovich, Michael R., Widdowson, Katherine L., Werner, Michelle L., Burman, Miriam, Foley, James J., Schmidt, Dulcie B., Sarau, Henry M., Rogers, Martin, Salyers, Kevin L., Gorycki, Peter D., Roethke, Theresa J., Stelman, Gary J., Azzarano, Leonard M., Ward, Keith W., Busch-Petersen, Jakob

“…N, N′-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2…”
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Design, Synthesis, and Structure−Activity Relationship of Tropane Muscarinic Acetylcholine Receptor Antagonists by Lainé, Dramane I, Wan, Zehong, Yan, Hongxing, Zhu, Chongjie, Xie, Haibo, Fu, Wei, Busch-Petersen, Jakob, Neipp, Christopher, Davis, Roderick, Widdowson, Katherine L, Blaney, Frank E, Foley, James, Bacon, Alicia M, Webb, Edward F, Luttmann, Mark A, Burman, Miriam, Sarau, Henry M, Salmon, Michael, Palovich, Michael R, Belmonte, Kristen

“…Novel tropane derivatives were characterized as muscarinic acetylcholine receptor antagonists (mAChRs). Through optimization of the structure−activity…”
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3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists by Wang, Yonghui, Busch-Petersen, Jakob, Wang, Feng, Ma, Lanping, Fu, Wei, Kerns, Jeffrey K, Jin, Jian, Palovich, Michael R, Shen, Jing-Kang, Burman, Miriam, Foley, James J, Schmidt, Dulcie B, Hunsberger, Gerald E, Sarau, Henry M, Widdowson, Katherine L

“…A series of 3-arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides were prepared and shown to be novel and selective antagonists of the CXCR2 receptor…”
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Fluorescent styryl dyes FM1-43 and FM2-10 are muscarinic receptor antagonists: intravital visualization of receptor occupancy by Mazzone, Stuart B., Mori, Nanako, Burman, Miriam, Palovich, Michael, Belmonte, Kristen E., Canning, Brendan J.

“…The fluorescent styryl dyes FM1-43 and FM2-10 have been used to visualize the endocytic and exocytic processes involved in neurotransmission in a variety of…”
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N, N′-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors by Nie, Hong, Widdowson, Katherine L., Palovich, Michael R., Fu, Wei, Elliott, John D., Bryan, Deborah L., Burman, Miriam, Schmidt, Dulcie B., Foley, James J., Sarau, Henry M., Busch-Petersen, Jakob

“…A series of N-(2-hydroxy-3-sulfonamidobenzene)- N′-arylcyanoguanidines was prepared. In general, these compounds proved to be potent antagonists of CXCR2 while…”
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Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists by Lainé, Dramane I., Xie, Haibo, Buffet, Noémie, Foley, James J., Buckley, Peter, Webb, Edward F., Widdowson, Katherine L., Palovich, Michael R., Belmonte, Kristen E.

“…In the course of our research program to develop novel muscarinic receptor antagonists for the treatment of COPD, new tropane carbamate derivatives were…”
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Discovery of (3- endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD by Wan, Zehong, Laine, Dramane I., Yan, Hongxing, Zhu, Chongjie, Widdowson, Katherine L., Buckley, Peter T., Burman, Miriam, Foley, James J., Sarau, Henry M., Schmidt, Dulcie B., Webb, Edward F., Belmonte, Kristen E., Palovich, Michael

“…Design and syntheses of a novel series of muscarinic antagonists are reported. These efforts have culminated in the discovery of (3-…”
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Call for Papers: Exploring the Use of AI/ML Technologies in Medicinal Chemistry and Drug Discovery by Palovich, Michael, Adams, Ashley, Chibale, Kelly

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Discovery of potent and orally bioavailable N, N′-diarylurea antagonists for the CXCR2 chemokine receptor by Jin, Qi, Nie, Hong, McCleland, Brent W., Widdowson, Katherine L., Palovich, Michael R., Elliott, John D., Goodman, Richard M., Burman, Miriam, Sarau, Henry M., Ward, Keith W., Nord, Melanie, Orr, Bonnie M., Gorycki, Peter D., Busch-Petersen, Jakob

“…A series of 3-substituted N, N′-diarylureas was prepared and CXCR2 receptor affinities as well as pharmacokinetic properties were examined. A series of…”
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M3 muscarinic acetylcholine receptor antagonists : SAR and optimization of bi-aryl amines by BUDZIK, Brian, YONGHUI WANG, SARAU, Henry M, MORROW, Dwight M, MOORE, Michael L, RIVERO, Ralph A, PALOVICH, Michael, SALMON, Michael, BELMONTE, Kristen E, LAINE, Dramane I, JIAN JIN, DONGCHUAN SHI, FENG WANG, HAIBO XIE, ZEHONG WAN, CHONGYE ZHU, FOLEY, James J, NUTHULAGANTI, Parvathi, KALLAL, Lorena A

“…Exploration of multiple regions of a bi-aryl amine template led to the identification of highly potent M(3) muscarinic acetylcholine receptor antagonists such…”
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Synthesis of Stereopentad Subunits of Zincophorin and Rifamycin-S through Use of Chiral Allenyltin Reagents by Marshall, James A, Palovich, Michael R

“…The anti,anti adduct 3, from addition of the allenic stannane (P)-2 to the α-methyl-β-OBn aldehyde (S)-1 promoted by SnCl4, was converted to the stereopentad 6…”
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Radical Cyclizations of Acylgermanes. New Reagent Equivalents of the Carbonyl Radical Acceptor Synthon by Curran, Dennis P, Diederichsen, Ulf, Palovich, Michael

“…An in depth study of the capability of acylgermanes to function as acceptors in radical cyclizations is reported. Radicals add to acylgermanes, and rapid…”
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Comparative Studies on the Synthesis of an anti,syn Stereotriad with Chiral Allenylstannane and Allenylindium Reagents by Marshall, James A, Palovich, Michael R

“…Addition of the chloroallenylstannane derived from the Bu3Sn allene (S)-2 and SnCl4 to nonracemic α-methyl-β-oxygenated aldehyde 1a afforded mixtures of…”
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Enantioselective and Diastereoselective Additions of Allylic Stannanes to Aldehydes Promoted by a Chiral (Acyloxy)borane Catalyst by Marshall, James A, Palovich, Michael R

“…A modified Yamamoto Lewis acid (CAB), prepared from the 2,6-dimethoxybenzoic ester of (R,R)-tartaric acid, and 1.5 equiv of BH3·THF was employed in additions…”
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Discovery of Novel Cyanamide-Based Inhibitors of Cathepsin C by Lainé, Dramane, Palovich, Michael, McCleland, Brent, Petitjean, Emilie, Delhom, Isabelle, Xie, Haibo, Deng, Jianghe, Lin, Guoliang, Davis, Roderick, Jolit, Anais, Nevins, Neysa, Zhao, Baoguang, Villa, Jim, Schneck, Jessica, McDevitt, Patrick, Midgett, Robert, Kmett, Casey, Umbrecht, Sandra, Peck, Brian, Davis, Alicia Bacon, Bettoun, David

“…The discovery of potent and selective cyanamide-based inhibitors of the cysteine protease cathepsin C is detailed. Optimization of the template with regard to…”
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