The design and syntheses of new fluoroquinolone antibacterial agents having pyrrolidine ring at C-7 position are described. The pyrrolidine ring is optically active and possesses methyloxime functional group. Two of them have excellent in vitro antibacterial activities and pharmacokinetic profiles.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2003.12.044 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Effectiveness of dolutegravir-based regimens compared to raltegravir-, elvitegravir-, bictegravir, and darunavir-based regimens among older adults with HIV in the Veterans Aging Cohort Study (VACS).
AIDS Res Ther
December 2024
Veterans Affairs (VA) Connecticut Healthcare System Cooperative Studies Program Clinical Epidemiology Research Center (CSP-CERC), 950 Campbell Avenue, West Haven, CT, 06516-2770, USA.
Background: Real-world data on treatment patterns and clinical outcomes for newer drugs, including integrase strand transfer inhibitors, among older people with human immunodeficiency virus (PWH) are limited.
Methods: This cohort study included PWH enrolled in the Veterans Aging Cohort Study (VACS) who were prescribed a standard 3-drug antiretroviral therapy (ART) regimen containing dolutegravir (DTG), bictegravir (BIC), cobicistat boosted elvitegravir (EVG), raltegravir (RAL), or darunavir/ritonavir (DRV) plus 2 nucleoside reverse transcriptase inhibitors between January 1, 2014, and March 31, 2020, and who were ≥50 years at regimen initiation. The association between regimen and virologic effectiveness or discontinuation was assessed using logistic regression models with inverse probability of treatment weights.
Generation and Application of All Possible Conformations of Cyclic Tryptophan within and beyond Post-translational Modification.
J Org Chem
December 2024
Department of Organic and Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Isoprenylation of the indole C3-position of tryptophan accompanied by cyclization (c-Trp) is one of the most attractive post-translational modifications because of C-C bond formation and drastic conformational alteration. As the modification generates two stereoisomers of the 6/5/5-fused ring system and consequently, a mixture of four possible conformations as considered in proline, it is expected to influence the biological activity in quorum sensing pheromone ComX containing the c-Trp residue. In this study, the simultaneous control of the amide equilibrium and pyrrolidine ring puckering was achieved by utilizing an N-carbamoylated and α-methylated 6/5/5-fused ring system.
View Article and Find Full Text PDFMultigram Synthesis of 3,3-Spiro-α-prolines.
J Org Chem
December 2024
Enamine Ltd., 78 Winston Churchill Street, 02094 Kyiv, Ukraine.
A series of novel spirocyclic α-proline building blocks with a spiro conjunction in position 3 of the pyrrolidine ring was prepared to employ two convenient and practical synthetic approaches. Both alternative routes utilize simple and readily available starting materials─cyclic ketones and esters─and comprise 6 and 7 steps, respectively. The methodologies feature distinct advantages, using routine organic chemistry transformations, and are suitable for producing multigram amounts of the target prolines.
View Article and Find Full Text PDFHeterocyclic pseudoguaianolide oligomers and seco-pseudoguaianolide derivatives from the inflorescence of Ambrosia artemisiifolia.
Phytochemistry
December 2024
College of Plant Protection, Hunan Agricultural University, Changsha, 410128, China. Electronic address:
Two heterocyclic sesquiterpenoid oligomers (1, 2) and four previously undescribed seco-pseudoguaianolide derivatives (3-6) were isolated from the inflorescence of Ambrosia artemisiifolia. Ambrosiadimer A (1) is an unprecedented dimer featuring a hexahydropyrrolizine core scaffold and two pseudoguaianolide units. Ambrosiatrimer A (2) is a trimer formed from three pseudoguaianolide units via a pyrrolidine ring.
View Article and Find Full Text PDFα-Pyrrolidinooctanophenone facilitates activation of human microglial cells via ROS/STAT3-dependent pathway.
Forensic Toxicol
December 2024
Laboratory of Bioinformatics, Gifu Pharmaceutical University, Gifu, 502-8585, Japan.
Purpose: Pyrrolidinophenone derivatives (PPs) are amphetamine-like designer drugs containing a pyrrolidine ring, and their adverse effects resemble those of methamphetamine (METH). Microglial activation has been recently suggested as a key event in eliciting the adverse effects against dysfunction of the central nervous system. The aim of this study is to clarify the mechanisms of microglial activation induced by PPs.
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!