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Put a ring on it: application of small aliphatic rings in medicinal chemistry
MR Bauer, P Di Fruscia, SCC Lucas… - RSC Medicinal …, 2021 - pubs.rsc.org
Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …
Facilitating compound entry as a means to discover antibiotics for gram-negative bacteria
KA Muñoz, PJ Hergenrother - Accounts of chemical research, 2021 - ACS Publications
Conspectus It has been over half a century since the last class of antibiotics active against
the most problematic Gram-negative bacteria was approved by the Food and Drug …
the most problematic Gram-negative bacteria was approved by the Food and Drug …
An Iterative Approach Guides Discovery of the FabI Inhibitor Fabimycin, a Late-Stage Antibiotic Candidate with In Vivo Efficacy against Drug-Resistant Gram-Negative …
Genomic studies and experiments with permeability-deficient strains have revealed a variety
of biological targets that can be engaged to kill Gram-negative bacteria. However, the …
of biological targets that can be engaged to kill Gram-negative bacteria. However, the …
Implementation of permeation rules leads to a FabI inhibitor with activity against Gram-negative pathogens
EN Parker, BS Drown, EJ Geddes, HY Lee… - Nature …, 2020 - nature.com
Gram-negative bacterial infections are a significant public health concern, and the lack of
new drug classes for these pathogens is linked to the inability of most drug leads to …
new drug classes for these pathogens is linked to the inability of most drug leads to …
3.08-Furans and their Benzo Derivatives: Applications
BA Keay, JM Hopkins, PW Dibble - … Heterocyclic Chemistry III, 2008 - hero.epa.gov
This chapter provides an overview of literature from 1996 on the applications of various
furan and benzofuran containing compounds. In addition to compounds that contain a furan …
furan and benzofuran containing compounds. In addition to compounds that contain a furan …
Synthetic access to diverse thiazetidines via a one-pot microwave assisted telescopic approach and their interaction with biomolecules
A one-pot microwave assisted telescopic approach is reported for the chemo-selective
synthesis of substituted 1, 3-thiazetidines using readily available 2-aminopyridines …
synthesis of substituted 1, 3-thiazetidines using readily available 2-aminopyridines …
Staphylococcus aureus utilizes host-derived lipoprotein particles as sources of fatty acids
Methicillin-resistant Staphylococcus aureus (MRSA) is a threat to global health.
Consequently, much effort has focused on the development of new antimicrobials that target …
Consequently, much effort has focused on the development of new antimicrobials that target …
[HTML][HTML] Synthesis and Antimicrobial Activity Screening of Piperazines Bearing N,N′-Bis(1,3,4-thiadiazole) Moiety as Probable Enoyl-ACP Reductase Inhibitors
A new N, N′-disubstituted piperazine conjugated with 1, 3, 4-thiadiazole and 1, 2, 4-triazole
was prepared and the chemical structures were identified by IR, NMR and elemental …
was prepared and the chemical structures were identified by IR, NMR and elemental …
The Drug Discovery and Development Industry in India—Two Decades of Proprietary Small‐Molecule R&D
E Differding - ChemMedChem, 2017 - Wiley Online Library
This review provides a comprehensive survey of proprietary drug discovery and
development efforts performed by Indian companies between 1994 and mid‐2016. It is …
development efforts performed by Indian companies between 1994 and mid‐2016. It is …
The Staphylococcus aureus FASII bypass escape route from FASII inhibitors
Antimicrobials targeting the fatty acid synthesis (FASII) pathway are being developed as
alternative treatments for bacterial infections. Emergence of resistance to FASII inhibitors …
alternative treatments for bacterial infections. Emergence of resistance to FASII inhibitors …