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 …

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 …

An Iterative Approach Guides Discovery of the FabI Inhibitor Fabimycin, a Late-Stage Antibiotic Candidate with In Vivo Efficacy against Drug-Resistant Gram-Negative …

EN Parker, BN Cain, B Hajian, RJ Ulrich… - ACS Central …, 2022 - ACS Publications
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 …

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 …

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 …

Synthetic access to diverse thiazetidines via a one-pot microwave assisted telescopic approach and their interaction with biomolecules

RN Rao, S Das, K Jacob, MM Alam… - Organic & …, 2024 - pubs.rsc.org
A one-pot microwave assisted telescopic approach is reported for the chemo-selective
synthesis of substituted 1, 3-thiazetidines using readily available 2-aminopyridines …

Staphylococcus aureus utilizes host-derived lipoprotein particles as sources of fatty acids

PC Delekta, JC Shook, TA Lydic, MH Mulks… - Journal of …, 2018 - journals.asm.org
Methicillin-resistant Staphylococcus aureus (MRSA) is a threat to global health.
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

AZ Omar, NA Alshaye, TM Mosa, SK El-Sadany… - Molecules, 2022 - mdpi.com
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 …

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 …

The Staphylococcus aureus FASII bypass escape route from FASII inhibitors

C Morvan, D Halpern, G Kénanian, A Pathania… - Biochimie, 2017 - Elsevier
Antimicrobials targeting the fatty acid synthesis (FASII) pathway are being developed as
alternative treatments for bacterial infections. Emergence of resistance to FASII inhibitors …