Eleven new amino alcohol derivatives have been synthesized from reactions of lopinavir intermediate and heteroaromatic aldehyde in good yields. These compounds, the antiretrovirals (lopinavir and ritonavir) and lopinavir key intermediate were evaluated as antibacterial agents against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and their activity expressed as the minimum inhibitory concentration (MIC) in μM. Ten amino alcohols evaluated displayed significant activity (MIC between 6.15 and 108.4 μM) when compared to first-line drug ethambutol (MIC = 15.9 μM). Three of them showed more activity than ethambutol (MIC = 6.15; 6.21 and 13.4 μM). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti-TB compounds.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1111/j.1747-0285.2011.01244.x | DOI Listing |
Proc Natl Acad Sci U S A
January 2025
Helen Wills Neuroscience Institute, University of California Berkeley, Berkeley, CA 94720.
Norepinephrine in vertebrates and its invertebrate analog, octopamine, regulate the activity of neural circuits. We find that, when hungry, larvae switch activity in type II octopaminergic motor neurons (MNs) to high-frequency bursts, which coincide with locomotion-driving bursts in type I glutamatergic MNs that converge on the same muscles. Optical quantal analysis across hundreds of synapses simultaneously reveals that octopamine potentiates glutamate release by tonic type Ib MNs, but not phasic type Is MNs, and occurs via the G-coupled octopamine receptor (OAMB).
View Article and Find Full Text PDFCells
December 2024
Neuroscience Institute, Section of Padova, National Research Council (CNR), 35131 Padova, Italy.
Astrocytes from different brain regions respond with Ca elevations to the catecholamine norepinephrine (NE). However, whether this noradrenergic-mediated signaling is present in astrocytes from the ventral tegmental area (VTA), a dopaminergic circuit receiving noradrenergic inputs, has not yet been investigated. To fill in this gap, we applied a pharmacological approach along with two-photon microscopy and an AAV strategy to express a genetically encoded calcium indicator in VTA astrocytes.
View Article and Find Full Text PDFMicrobiology (Reading)
January 2025
Department of Microbiology and Molecular Genetics, Larner College of Medicine, University of Vermont, Burlington, USA.
Sphingoid bases, including sphingosine, are important components of the antimicrobial barrier at epithelial surfaces where they can cause growth inhibition and killing of susceptible bacteria. is a common opportunistic pathogen that is less susceptible to sphingosine than many Gram-negative bacteria. Here, we determined that the deletion of the operon reduced growth in the presence of sphingosine.
View Article and Find Full Text PDFBiomed Chromatogr
February 2025
Department of Chemistry, GITAM School of Science, GITAM Deemed to Be University, Hyderabad, India.
A simple LC method has been developed and validated for estimating budesonide (epimer B + A) and formoterol fumarate dihydrate in dry powder inhalation. The development results of this study make it very significant. The degradation and process impurities in EP and ChP were identified in addition to budesonide and formoterol fumarate.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Nephrology, Fujian Medical University Union Hospital, Fuzhou, 350001, China.
Glomerular endothelial cells (GECs) are pivotal in developing glomerular sclerosis disorders. The advancement of focal segmental glomerulosclerosis (FSGS) is intimately tied to disruptions in lipid metabolism. Sphingosine-1-phosphate (S1P), a molecule transported by high-density lipoproteins (HDL), exhibits protective effects on vascular endothelial cells by upregulating phosphorylated endothelial nitric oxide synthase (p-eNOS) and enhancing nitric oxide (NO) production.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!