Results 181 to 190 of about 9,317 (205)

HIV‐1 Protease Inhibitors with Picomolar Potency Against PI‐Resistant HIV‐1 by Modification of the P₁′ Substituent.

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Joseph L. Duffy, et al. et al.
openaire   +1 more source

Molecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency

Journal of Medicinal Chemistry, 2013
The design and preliminary SAR of a new series of 1H-quinazolin-4-one (QAZ) allosteric HCV NS5B thumb pocket 2 (TP-2) inhibitors was recently reported. To support optimization efforts, a molecular dynamics (MD) based modeling workflow was implemented, providing information on QAZ binding interactions with NS5B.
Oliver, Hucke, René, Coulombe, Pierre, Bonneau, Mégan, Bertrand-Laperle, Christian, Brochu, James, Gillard, Marc-André, Joly, Serge, Landry, Olivier, Lepage, Montse, Llinàs-Brunet, Marc, Pesant, Martin, Poirier, Maude, Poirier, Ginette, McKercher, Martin, Marquis, George, Kukolj, Pierre L, Beaulieu, Timothy A, Stammers   +17 more
openaire   +2 more sources

1,3-Oxazole-based selective picomolar inhibitors of cytosolic human carbonic anhydrase II alleviate ocular hypertension in rabbits: Potency is supported by X-ray crystallography of two leads

Bioorganic & Medicinal Chemistry, 2017
Two lead 1,3-oxazole-based carbonic anhydrase inhibitors (CAIs) earlier identified as selective, picomolar inhibitors of hCA II (a cytosolic target for treatment of glaucoma) have been investigated further. Firstly, they were found to be conveniently synthesized on multigram scale, which enables further development.
Ferraroni, Marta, Lucarini, Laura, Masini, Emanuela, Korsakov, Mikhail, Scozzafava, Andrea, Supuran, Claudiu T., Krasavin, Mikhail   +6 more
openaire   +3 more sources

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis

Bioorganic & Medicinal Chemistry Letters, 2008
Conformational analysis of trans-1,2-disubstituted cyclohexane CCR3 antagonist 2 revealed that the cyclohexane linker could be replaced by an acyclic syn-alpha-methyl-beta-hydroxypropyl linker. Synthesis and biological evaluation of mono- and disubstituted propyl linkers support this conformational correlation.
Joseph B, Santella, Daniel S, Gardner, Wenqing, Yao, Chongsheng, Shi, Prabhakar, Reddy, Andrew J, Tebben, George V, DeLucca, Dean A, Wacker, Paul S, Watson, Patricia K, Welch, Eric A, Wadman, Paul, Davies, Kimberly A, Solomon, Dani M, Graden, Swamy, Yeleswaram, Sandhya, Mandlekar, Ilona, Kariv, Carl P, Decicco, Soo S, Ko, Percy H, Carter, John V, Duncia   +20 more
openaire   +2 more sources

ChemInform Abstract: From Rigid Cyclic Templates to Conformationally Stabilized Acyclic Scaffold. Part 1. The Discovery of CCR3 Antagonist Development Candidate BMS‐639623 with Picomolar Inhibition Potency Against Eosinophil Chemotaxis.

ChemInform, 2008
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
John V. Duncia, et al. et al.
openaire   +1 more source

Toxic potency-adjusted control of air pollution for solid fuel combustion

Nature Energy, 2022
Haotian Zheng, Qing Li, Ling Jin
exaly  

Preclinical assessment of capsid assembly modulators (CAMs) of varying potency revealed a novel class of picomolar-acting CAMs inducing neither significant HBcAg cytoplasmic retention nor adverse interactions with HBcAg-specific adaptive immunity

Journal of Hepatology, 2020
Romano Di Fabio, Leda Bencheva, Raffaele De Francesco, Lorena Donnici, Vincenzo Summa, Edith Monteagudo, Matteo Iannacone, Luca Guidotti   +7 more
openaire   +2 more sources

Designing spatial and temporal control of vaccine responses

Nature Reviews Materials, 2021
Shih Hao Ou, Wei Luo, Bali Pulendran
exaly  

Tailoring Aggregation Extent of Photosensitizers to Boost Phototherapy Potency for Eliciting Systemic Antitumor Immunity

Advanced Materials, 2022
Hao Zhao, Jiabao Xu, Lin Bao
exaly  

Induction of Bleb Structures in Lipid Nanoparticle Formulations of mRNA Leads to Improved Transfection Potency

Advanced Materials, 2023
Pieter Cullis
exaly