Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to the methylene spacer and the P1' side chain. Enzyme inhibition and antibacterial activity data revealed that the optimum distance between the N-formyl hydroxylamine metal binding group and the P1' side chain is one unsubstituted methylene unit. Additionally, lipophilic P1' side chains that closely mimic the methionine residue in the substrate provided compounds with the best microbiological profile.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(03)00532-8 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Acceptance of Parents toward Hand-over-mouth Exercise and Other Behavior Management Techniques for Pediatric Dental Care in the 21st Century: A Systematic Review and Meta-analysis of Observational Studies.
Int J Clin Pediatr Dent
November 2024
Department of Pediatric and Preventive Dentistry, Bharati Vidyapeeth (Deemed to be University) Dental College and Hospital, Mumbai, Maharashtra, India.
Background: Hand-over-mouth exercise (HOME) is an aversive technique for child behavior management in a dental office. HOME has been omitted from various guidelines and certain teaching curricula due to legal and ethical issues. This systematic review meta-analysis (SRMA) was undertaken to understand the acceptance of parents toward HOME in comparison with that of other behavior management techniques (BMTs).
View Article and Find Full Text PDFImmune-related adverse events not associated with survival in advanced or metastatic gastroesophageal cancers.
J Chemother
January 2025
Department of Internal Medicine, Division of Hematology & Oncology, University of Virginia Health, Charlottesville, VA, USA.
Immune checkpoint inhibitors (ICIs) have shown promise in the treatment of gastric and oesophageal cancers (GEC). Despite their promising efficacy, ICIs have been associated with unique side effects known as immune-related adverse events (IRAEs). Several studies have shown improved treatment responses in patients with IRAEs compared to those without IRAEs in various cancer types such as melanoma and non-small cell lung cancer.
View Article and Find Full Text PDFPI-RADS 3 MRI lesions: Are biopsies still necessary?
Fr J Urol
January 2025
Department of Urology, North Hospital, AP-HM, Marseille, France.
Introduction: A significant proportion of newly diagnosed prostate cancer (PCa) cases are slow growing with a low risk of metastatic progression. There is a lack of data concerning the optimal biopsy regimen for improving diagnosis yield in PI-RADS3 lesions. This study aimed to assess the diagnostic value of current biopsy regimens in PI-RADS 3 lesions and identify clinical predictors to improve clinically significant PCa (csPCa) detection.
View Article and Find Full Text PDFDual Inhibitors of SARS-CoV-2 3CL Protease and Human Cathepsin L Containing Glutamine Isosteres Are Anti-CoV-2 Agents.
J Am Chem Soc
January 2025
Department of Biochemistry and Biophysics, Texas A&M University, 301 Old Main Drive, College Station, Texas 77845, United States.
SARS-CoV-2 3CL protease (Main protease) and human cathepsin L are proteases that play unique roles in the infection of human cells by SARS-CoV-2, the causative agent of COVID-19. Both proteases recognize leucine and other hydrophobic amino acids at the P position of a peptidomimetic inhibitor. At the P position, cathepsin L accepts many amino acid side chains, with a partial preference for phenylalanine, while 3CL-PR protease has a stringent specificity for glutamine or glutamine analogues.
View Article and Find Full Text PDFProlonged or perpetual growth of replacement teeth in the rock hyrax.
Anat Rec (Hoboken)
December 2024
Department of Anthropology, University of Florida, Gainesville, Florida, USA.
Tusks are ever-growing teeth present in mammals of the clade Paenungulata. Unlike the perpetually growing incisors of rodents, tusks are not used in mastication, and in at least some paenungulatans, the tusk is composed of dentin alone in adults. Few studies have provided tissue-level information on tusks of adult paenungulatans with embedding techniques that identify epithelial and other soft tissues.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!