Development of a high-throughput dual-stream liquid chromatography-tandem mass spectrometry method to screen for inhibitors of glutamate carboxypeptidase II.

Rationale: Glutamate carboxypeptidase II (GCPII) catalyzes the hydrolysis of N-acetylaspartylglutamate (NAAG) to yield glutamate (Glu) and N-acetylaspartate (NAA). Inhibition of GCPII has been shown to remediate the neurotoxicity of excess Glu in a variety of cell and animal disease models. A robust high-throughput liquid chromatography-tandem mass spectrometry (LC/MS/MS) method was needed to quantify GCPII enzymatic activity in a biochemical high-throughput screening assay.

Noscapine-Amino Acid Conjugates Suppress the Progression of Cancer Cells.

Lung cancer is the leading cause of cancer deaths globally; 1 in 16 people are diagnosed with lung cancer in their lifetime. Microtubules, a critical cytoskeletal assembly, have an essential role in cell division. Interference with the microtubule assembly leads to genetic instability during mitosis and cancer cell death.

Repurposing of FDA Approved Drugs Against SARS-CoV-2 Papain-Like Protease: Computational, Biochemical, and Studies.

The pandemic caused by SARS-CoV-2 (SCoV-2) has impacted the world in many ways and the virus continues to evolve and produce novel variants with the ability to cause frequent global outbreaks. Although the advent of the vaccines abated the global burden, they were not effective against all the variants of SCoV-2. This trend warrants shifting the focus on the development of small molecules targeting the crucial proteins of the viral replication machinery as effective therapeutic solutions.

Computational investigations on the potential role of hygrophorones as quorum sensing inhibitors against LasR protein of .

is a gram negative, rod shape bacterium that infects people with compromised immune systems, such as those suffering from AIDS, organ transplantation and cancer. This bacterium is responsible for diseases like cystic fibrosis, chronic lung infection, and ulcerative keratitis. It is diagnosed in most of the patients who were on prolonged ventilation with long term critical care stay.

Stereoselective total synthesis of (-)-hygrophorone A and 4-epi-2,3-dihydrohygrophorone H.

Stereoselective total synthesis of anti-fungal cyclopentenone (-)-hygrophorone A and cyclopentanone 4-epi-2,3-dihydrohygrophorone H were achieved in high overall yields from d-ribose. An aqueous KOH mediated diastereoselective formation of β-hydroxy ketone with three contiguous chiral centres served as a key step in this synthesis.

Stereoselective total syntheses of (-)-hygrophorone A, 4--acetyl-hygrophorone A and (+)-hygrophorone B.

Total syntheses of anti-fungal cyclopentenones (-)-hygrophorone A12, 4-O-acetyl-hygrophorone A12 and (+)-hygrophorone B12 were achieved in high overall yields from d-(-)-tartaric acid. The key feature of these syntheses is the aqueous KOH-mediated diastereoselective intramolecular aldol reaction to form β-hydroxy ketone with three contiguous chiral centres, which was further elaborated to (-)-hygrophorone A12 and (+)-hygrophorone B12. The synthetic route reported here is operationally simple and highly diastereoselective and is amenable for the synthesis of several analogues of hygrophorones.

Identification and analysis of organic explosives from post-blast debris by nuclear magnetic resonance.

The growing threat of terrorism has triggered an urgent need to find effective ways to improve the analysis of explosives. This will aid forensic scientists in analysing the post-blast debris, which in turn helps the law enforcement agencies to frame suitable regulations. Analysis of post-blast debris is challenging as it hosts a massive amount of complexity.