Results 41 to 50 of about 53,373 (308)

Breakthrough Design of Highly Potent Antivirals Against Wild‐Type HIV‐1 and Lenacapavir‐Resistant M66I Variant

Angewandte Chemie, EarlyView.
Lenacapavir, the first‐in‐class drug targeting HIV‐1 capsid, is a breakthrough drug in HIV‐1 treatment and prophylaxis. However, a single M66I mutation confers complete viral resistance to lenacapavir. We report herein the design and synthesis of innovative R2 analogs demonstrating low nM potency against HIV‐1 M66I and excellent pharmacokinetics in ...
Nicolas Jamey, D. M. Nirosh Udayanga, Huanchun Zhang, Roshan Katekar, Wei Xie, Shreya M. Ravichandran, Xinyong Cai, Zachary C. Lorson, William M. McFadden, Won Hee Ryu, Jiashu Xie, Karen A. Kirby, Stefan G. Sarafianos, Zhengqiang Wang   +13 more
wiley   +2 more sources

Novel Regioselective Synthesis of 1,3,4,5-Tetrasubstituted Pyrazoles and Biochemical Valuation on F₁F_O-ATPase and Mitochondrial Permeability Transition Pore Formation

Pharmaceutics, 2023
An efficient, eco-compatible, and very cheap method for the construction of fully substituted pyrazoles (Pzs) via eliminative nitrilimine-alkene 1,3-dipolar cycloaddition (ENAC) reaction was developed in excellent yield and high regioselectivity ...
Vincenzo Algieri, Cristina Algieri, Paola Costanzo, Giulia Fiorani, Antonio Jiritano, Fabrizio Olivito, Matteo Antonio Tallarida, Fabiana Trombetti, Loredana Maiuolo, Antonio De Nino, Salvatore Nesci   +10 more
doaj   +1 more source

Cobalt‐Catalyzed C─N Bond Formation via Metal‐Hydride Hydrogen Atom Transfer (MHAT)

Angewandte Chemie, EarlyView.
Cobalt‐catalyzed metal‐hydride hydrogen atom transfer (Co‐MHAT) converts simple alkenes into C─N bonds under mild, near‐neutral conditions. A shared Co─H‐initiated radical/organocobalt intermediate is channeled into radical trapping, radical‐polar crossover, or radical ligand transfer, unifying hydroamination, hydroazidation, hydroamidation, and remote
Arman Khosravi, Ming‐Yu Ngai
wiley   +2 more sources

Regeneration‐Optimized Chemisorbents: Evaluating Hybrid Coordination Networks for Atmospheric Water Harvesting

Angewandte Chemie, EarlyView.
Atmospheric water harvesting (AWH) under arid conditions requires desiccants that load water below 30% RH and regenerate below 60°C, a performance regime traditionally limited to physisorbents. Here, we show that the inherent hydrolytic instability of M′FSIX‐25‐M coordination networks enable regeneration‐optimized chemisorbents (ROCs) with projected ...
Xiang‐Jing Kong, Asif Raza, Lilia Croitor, Andrey Bezrukov, Xia Li, Angela Shipman, William Morris, Carlos J. Solanilla‐Salinas, Adam Hogan, Brian Space, Volodymyr Bon, Stefan Kaskel, Soumya Mukherjee, Alan C. Eaby, Tao He, Michael J. Zaworotko   +15 more
wiley   +2 more sources

Order versus disorder in two isomorphous pyrazolone-substituted diethyl propanedioates prepared using a three-component one-pot reaction under solvent-free conditions

Acta Crystallographica Section E: Crystallographic Communications, 2020
Two new substituted propanedioate esters have been synthesized using a three-component solvent-free thermal reaction between diethyl propanedioate (diethyl malonate), 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde and an aryl azide, forming two ...
Tharangini K. Shreekanth, Hemmige S. Yathirajan, Balakrishna Kalluraya, Sabine Foro, Christopher Glidewell   +4 more
doaj   +1 more source

Cobalt‐Catalyzed [2σ+2π] Cycloaddition via Site‐Selective Capture of Bicyclobutane Diradical

Angewandte Chemie, EarlyView.
We report a Co(II)‐catalyzed strategy that combines thermal activation of bicyclo[1.1.0]butane (BCBs) with site‐selective radical capture to furnish head‐to‐head fused bicyclo[2.1.1]hexanes via [2σ+2π] cycloaddition with indoles. Detailed mechanistic studies (31P NMR, EPR, CV, and DFT) support the catalytic pathway, while phosphine‐oxide trapping and X‐
Tanmayee Nanda, Alexander Umanzor, Julia Gartzke, Jeremy T. Maddigan‐Wyatt, Philipp Thielert, Stefan Weber, Sabine Richert, Shuming Chen, Daniel B. Werz   +8 more
wiley   +2 more sources

Synthesis of tetrasubstituted pyrazoles containing pyridinyl substituents

Beilstein Journal of Organic Chemistry, 2017
A synthesis of tetrasubstituted pyrazoles containing two, three or four pyridinyl substituents is described. Hence, the reaction of 1,3-dipyridinyl-1,3-propanediones with 2-hydrazinopyridine or phenylhydrazine, respectively, affords the corresponding 1,3,
Josef Jansa, Ramona Schmidt, Ashenafi Damtew Mamuye, Laura Castoldi, Alexander Roller, Vittorio Pace, Wolfgang Holzer   +6 more
doaj   +1 more source

Rhodium(III)-Catalyzed Oxidative Coupling of 5-Aryl-1H-pyrazoles with Alkynes and Acrylates

, 2011
Rhodium(III)-Catalyzed Oxidative Coupling of 5-Aryl-1H-pyrazoles with Alkynes and Acrylates[RhCp*Cl(2)](2)-catalyzed oxidative coupling of 5-aryl-1H-pyrazoles with alkynes and acrylates has been achieved using Cu(OAc)(2) as an oxidant.
李兴伟, Zhao, Miao, Li, Xingwei
core   +1 more source

Thermal rearrangements of 3H-pyrazoles, 4H-pyrazoles, and cyclopentadienes

, 1992
3H-Pyrazoles generally undergo thermal rearrangement by concerted [1,5]-sigmatropic migrations. It has been discovered that 3H-pyrazoles 111a-e undergo thermal rearrangement by an alterative mechanism.
Jefferson, Anne Elizabeth
core   +1 more source

Enantiomeric-Enriched Ferrocenes: Synthesis, Chiral Resolution, and Mathematic Evaluation of CD-chiral Selector Energies with Ferrocene-Conjugates

Molecules, 2017
Enantiomeric-enriched ferrocene-modified pyrazoles were synthesized via the reaction of the ferrocene alcohol, (S)-FcCH(OH)CH3 (Fc = ferrocenyl), with various pyrazoles in acidic conditions at room temperature within several minutes.
Lubov V. Snegur, Yurii A. Borisov, Yuliya V. Kuzmenko, Vadim A. Davankov, Mikhail M. Ilyin, Mikhail M. Ilyin, Dmitry E. Arhipov, Alexander A. Korlyukov, Sergey S. Kiselev, Alexander A. Simenel   +9 more
doaj   +1 more source