Article
Chemistry, Medicinal
Yi Zhang, Ting-jian Zhang, Xin-yang Li, Jing-wei Liang, Shun Tu, Hai-li Xu, Wen-han Xue, Xin-hua Qian, Zhen-hao Zhang, Xu Zhang, Fan-hao Meng
Summary: In this study, a series of potential Hsp90 inhibitors were designed and synthesized, among which 14t exhibited excellent antiproliferative and Hsp90α inhibitory activities, inducing apoptosis, cell cycle arrest, and inhibiting cell migration. Moreover, 14t significantly repressed tumor growth in a xenograft mouse model.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Jun Xu, Tianjiao Yang, Jiayi Wang, Gonghua Song
Summary: Novel compounds derived from 5-HT3 receptor antagonists were synthesized through isocyanide insertion reaction, showing good lethality and serious nervous effects against nematodes. These compounds have potential anti-nematode activities.
CHEMISTRY OF HETEROCYCLIC COMPOUNDS
(2021)
Article
Chemistry, Multidisciplinary
Krishnaji Tadiparthi, Pragya Anand, Raghavendra Sakirolla, T. Prakash Gupta, Krishna A. Jadhav, Sukant Kishore Das, Jhillu Singh Yadav
Summary: The use of dimethyl-8-oxa-bicyclo[3.2.1]oct-6-en-3-ol as a synthon has been explored for the synthesis of various natural products over the past three decades, allowing for the construction of multiple stereo centers during asymmetric synthesis. By desymmetrizing this starting material through hydroboration, different chiral centers can be obtained, enabling the synthesis of natural products through protection, deprotection, and C-C bond formation steps.
Article
Chemistry, Multidisciplinary
Krishnaji Tadiparthi, Pragya Anand, Raghavendra Sakirolla, T. Prakash Gupta, Krishna A. Jadhav, Sukant Kishore Das, Jhillu Singh Yadav
Summary: The paragraph discusses the synthesis of various natural products using dimethyl-8-oxa-bicyclo[3.2.1]oct-6-en-3-ol as a synthon, with focus on asymmetric synthesis to create multiple stereocenters at once. This approach provides a key foundation for the preparation of biologically active natural products.
Review
Chemistry, Organic
Sandra Rodriguez, Uxue Uria, Efraim Reyes, Liher Prieto, Marta Rodriguez-Rodriguez, Luisa Carrillo, Jose L. Vicario
Summary: The 8-azabicyclo[3.2.1]octane scaffold is the central core of tropane alkaloids with diverse biological activities. Research focuses on preparing this structure stereoselectively, with some approaches achieving stereochemical control directly in the same transformation process.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Article
Chemistry, Organic
Cheng Yuan, Sheng Sun, Gangqiang Wang, Shaofa Sun, Jian Wang
Summary: In this study, a unique and operationally simple method was reported for assembling 8-azabicyclo[3,2,1]octanes using oxidopyridinium ions and maleimides as synthons. Good to high yields and good functional group tolerance are achieved regularly under mild conditions. It is noteworthy that oxidopyridinium ions undergo a [3 + 2] cycloaddition on their C2 and C6 positions.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Ludmila A. Bulygina, Natalya S. Khrushcheva, Konstantin A. Lyssenko, Alexander S. Peregudov
Summary: A new bicyclic unsymmetrical CNN palladium 5,6-membered pincer complex was synthesized and showed high catalytic activity in Suzuki cross-coupling reactions between aryl bromides and phenylboronic acid.
MENDELEEV COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Arun K. Ghosh, Monika Yadav
Summary: The study focused on the base mediated asymmetric intramolecular oxidopyrylium-alkene [5 + 2]-cycloaddition reaction to synthesize functionalized tricyclic ring systems with an 8-oxabicyclo[3.2.1]octane core. The intramolecular cycloaddition resulted in the construction of two new rings, three new stereogenic centers, and high diastereoselectivity in the isolated yield. The size of alkyl groups and alkene tether length were found to affect the diastereoselectivity of the cycloadduct.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Hsin-Yen Cho, Tzu-Hsien Chuang, Sheng-Nan Wu
Summary: Solifenacin enhances M-type K+ current by interacting with K-M channels in electrically excitable cells, independent of its antagonistic activity on muscarinic receptors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Organic
Peter S. Radulov, Ivan A. Yaremenko, Alexander O. Terent'ev
Summary: The title compound, 1-(2-Benzyl-1,5-dimethyl-6,7,8-trioxabicyclo[3.2.1]octan-2-yl)ethan-1-ol, was synthesized for the first time by selectively reducing keto ozonide using the strong reducing agent LiAlH4. The product was characterized by NMR, IR, HRMS, and elemental analysis.
Article
Chemistry, Medicinal
Sanjay Kumar, Purvi Shah, Siddharth K. Tripathi, Shabana I. Khan, Inder Pal Singh
Summary: This study synthesized and evaluated hydrazonomethylquinolin-8-ol and pyrazol-3-yl-quinolin-8-ol derivatives for antifungal, antibacterial, and antimalarial activity. The results showed that most compounds exhibited good antifungal activity against various strains, indicating their potential as leads for further development of antifungal agents.
MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Larisa N. Grigor'eva, Alexsei Ya Tikhonov, Konstantin A. Lomanovich, Dmitrii G. Mazhukin
Summary: Bicyclic nitroxyl radicals have gained attention as selective catalysts for the oxidation of alcohols and amines, and the development of new synthetic methods for functional bicyclic nitroxides is an important issue. A novel stable nitroxyl bicyclic radical derived from imidazo[1,2-b]isoxazoles can be formed by oxidation with lead dioxide in acetone.
Article
Chemistry, Organic
Yoshihiko Yamamoto, Yuya Nakazato, Ryu Tadano, Takeshi Yasui
Summary: This study reports the trifluoromethylation of furfural followed by photo-Achmatowicz reaction to obtain 6-hydroxy-2-(trifluoromethyl)-2H-pyran-3(6H)-one. The acetylated product, 6-acetoxy-2-(trifluoromethyl)-2H-pyran-3(6H)-one, was then transformed into various 1-(trifluoromethyl)-8-oxabicyclo[3.2.1]oct-3-en-2-one derivatives through a base-mediated oxidopyrylium [5 + 2] cycloaddition. The reactivity and selectivity of the 2-trifluoromethylated oxidopyrylium species were analyzed using density functional theory calculations.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Takahito Uemura, Motohiro Sonoda, Shinji Tanimori
Summary: 5-Hydroxyequol, a biologically active isoflavone metabolite, was synthesized from 3-(2,4,6-trimethoxyphenyl)propanal using MacMillans' asymmetric alpha-arylation protocol. Enantiomerically pure (S)- and (R)-5-Hydroxyequols were obtained with high enantiomeric excess. Additionally, unnatural equol isomers were also synthesized with high enantiomeric excess for the first time.
RESULTS IN CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Liliana Mazur, Renata Lyszczek, Malgorzata Sztanke, Krzysztof Sztanke
Summary: For the first time, single crystal X-ray diffraction data of the potential pharmaceutical compound C15H18N4O have been reported, revealing its unique structural features and discussing its intermolecular and intramolecular interactions as well as crystal structure. The study found a lack of strong hydrogen bonds in the crystal but the presence of weak C-H···O/N/··· hydrogen bonds facilitated by multiple hydrogen bond acceptors and highly polarized C-H groups.
ACTA POLONIAE PHARMACEUTICA
(2022)
Article
Multidisciplinary Sciences
Guy Griebel, Philippe Pichat, Denis Boulay, Vanessa Naimoli, Lisa Potestio, Robert Featherstone, Sukhveen Sahni, Henry Defex, Christophe Desvignes, Franck Slowinski, Xavier Vige, Olivier E. Bergis, Rosy Sher, Raymond Kosley, Sathapana Kongsamut, Mark D. Black, Geoffrey B. Varty
SCIENTIFIC REPORTS
(2016)
Article
Chemistry, Medicinal
Dong Xiao, Cheng Wang, Anandan Palani, Hon-Chung Tsui, Gregory Reichard, Sunil Paliwal, Neng-Yang Shih, Robert Aslanian, Ruth Duffy, Jean Lachowicz, Geoffrey Varty, Cynthia Morgan, Fei Liu, Amin Nomeir
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2010)
Article
Pharmacology & Pharmacy
Robbie L. McLeod, Deen B. Tulshian, Donald C. Bolser, Geoffrey B. Varty, Marco Baptista, Xiomara Fernandez, Leonard E. Parra, Jennifer C. Zimmer, Christine H. Erickson, Ginny D. Ho, Yanlin Jia, Fay W. Ng, Walter Korfmacher, Xiaoying Xu, John Veals, April Smith-Torhan, Samuel Wainhaus, Ahmad B. Fawzi, Theodore M. Austin, Margaret van Heek, John A. Hey
EUROPEAN JOURNAL OF PHARMACOLOGY
(2010)
Article
Pharmacology & Pharmacy
Sherry X. Lu, Guy A. Higgins, Robert A. Hodgson, Lynn A. Hyde, Robert A. Del Vecchio, Donald H. Guthrie, Tatiana Kazdoba, Martha F. McCool, Cynthia A. Morgan, Ana Bercovici, Ginny D. Ho, Deen Tulshian, Eric M. Parker, John C. Hunter, Geoffrey B. Varty
EUROPEAN JOURNAL OF PHARMACOLOGY
(2011)
Article
Pharmacology & Pharmacy
Robert A. Hodgson, Deborra Mullins, Sherry X. Lu, Mario Guzzi, Xiaoping Zhang, Carina J. Bleickardt, Jack D. Scott, Michael W. Miller, Andrew W. Stamford, Eric M. Parker, Geoffrey B. Varty
EUROPEAN JOURNAL OF PHARMACOLOGY
(2014)
Article
Pharmacology & Pharmacy
Michel R. Corboz, Maria A. Rivelli, Kevin D. McCormick, Yuntao Wan, Himanshu Shah, Shelby Umland, Gisela Lieber, Yanlin Jia, Robbie L. McLeod, Cynthia Morgan, Geoffrey B. Varty, Jie Wu, Kung-I Feng, Christopher W. Boyce, Robert G. Aslanian, Jai Palamanda, Amin A. Nomeir, Walter Korfmacher, John C. Hunter, John C. Anthes, John A. Hey
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2011)
Article
Behavioral Sciences
Nancy Rogacki, Matilde Lopez-Grancha, Vanessa Naimoli, Lisa Potestio, Rachel J. Stevens, Philippe Pichat, Olivier E. Bergis, Caroline Cohen, Geoffrey B. Varty, Guy Griebel
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2011)
Article
Behavioral Sciences
Robert A. Hodgson, Lynn A. Hyde, Donald H. Guthrie, Mary E. Cohen-Williams, Prescott T. Leach, Tatiana M. Kazdoba, Carina J. Bleickardt, Sherry X. Lu, Eric M. Parker, Geoffrey B. Varty
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2011)
Article
Behavioral Sciences
Guy Griebel, Philippe Pichat, Marie-Pierre Pruniaux, Sandra Beeske, Mati Lopez-Grancha, Elisabeth Genet, Jean-Paul Terranova, Antonio Castro, Juan Antonio Sanchez, Mark Black, Geoffrey B. Varty, Ina Weiner, Michal Arad, Segev Barak, Amaya De Levie, Etienne Guillot
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2012)
Article
Behavioral Sciences
Ruth A. Duffy, Cynthia Morgan, Robert Naylor, Guy A. Higgins, Geoffrey B. Varty, Jean E. Lachowicz, Eric M. Parker
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2012)
Article
Neurosciences
Mark D. Black, Rachel J. Stevens, Nancy Rogacki, Robert E. Featherstone, Yaw Senyah, Odessa Giardino, Beth Borowsky, Jeanne Stemmelin, Caroline Cohen, Philippe Pichat, Michal Arad, Segev Barak, Amaya De Levie, Ina Weiner, Guy Griebel, Geoffrey B. Varty
PSYCHOPHARMACOLOGY
(2011)
Article
Neurosciences
Steven M. Grauer, Raul Sanoja, Dominic Poulin, Harunor Rashid, Nina Jochnowitz, Michael Calhoun, Daniel Zwilling, Geoffrey B. Varty, Thomas W. Rosahl, Hamid Meziane, Christopher Mittlelhaeuser, Robert Mazzola, John Morrow, Sean M. Smith, Darrell Henze, Jacob Marcus
Meeting Abstract
Neurosciences
Amir Inamdar, Michael Morgan, Joan Krakowsky, Amy Reichelt, Clinton Canal, Tina Mueller, Ken Avery, Pradip Pathare, Joshua Hartsel, Alex Nivorozhkin, Geoffrey Varty, Michael Palfreyman
NEUROPSYCHOPHARMACOLOGY
(2022)
Meeting Abstract
Neurosciences
Michael Palfreyman, Joan Krakowsky, Michael Morgan, Clinton Canal, Pradip Pathare, Ken Avery, Amy Reichelt, Joshua Hartsel, Alex Nivorozhkin, Amir Inamder, Geoffrey Varty
NEUROPSYCHOPHARMACOLOGY
(2022)
Meeting Abstract
Chemistry, Multidisciplinary
Anthony Roecker, Mark Layton, Michael Kelly, Joseph Pero, Thomas Greshock, Ting Zhang, Richard Kraus, Yuxing Li, Christopher Daley, Aneta Jovanovska, Becky Klein, Michelle Clements, Jixin Wang, Darrell Henze, Geoffrey Varty, Jeanine Ballard, Deping Wang, Fuqiang Zhao, Christopher Regan, Hillary Regan, Leo Joyce, Edward Sherer, Christopher John, Xuanjia Peng, Xiu Wang, Haiyan Sun, Andrea Houghton, Christopher Burgey
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2018)