Synthesis of N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B

The linkage between dopamine D2 receptors and PDE activity via cAMP prompted us to design a series of novel N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B. The target compounds were conveniently prepared by using a simple and inexpensive method involving Pd/C-mediated CC bond forming reaction under Sonogashira conditions. A number of compounds were synthesized by using this strategy in good yields. Some of the compounds showed promising inhibition of PDE4B when tested in vitro that was supported by the docking studies

4-[(4-Methyl­benz­yl)amino]-3-[(4-methyl­benz­yl)imino­meth­yl]-2H-chromen-2-one

The title compound, C26H24N2O2, was prepared from the reaction of 4-chloro-3-formyl­coumarin with p-methyl­benzyl­amine. Even though there are no strong and specific inter­actions in the crystal structure, the translationally related mol­ecules form chains along the b axis. The coumarin moieties are stacked through π–π inter­actions [centroid–centroid distance = 3.5275 (7) Å], forming layers perpendicular to the stacking direction

Iodine-Mediated Neutral and Selective N

A simple, efficient, and alternative method has been developed for the N-Boc deprotection of structurally diverse protected amines. Selective removal of N-Boc groups was achieved with excellent yields under a solvent-free condition or in a solvent using iodine as a catalyst. The methodology involving the first use of iodine for N-Boc deprotection of protected amines represents an effective and useful alternative to the previously reported methods

Research for practice in small human service organisations: doing and disseminating smallscale research

A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I2-mediated Biginelli reaction followed by Cu-free Sonogashira coupling. Some of them showed promising inhibitory activities when tested at 30 μM. One compound showed dose dependent inhibition of CM with IC50 value of 14.76 ± 0.54 μM indicating o-alkynylphenyl substituted DHPM as a new scaffold for the discovery of promising inhibitors of CM

Overview of Chatbots with special emphasis on artificial intelligence-enabled ChatGPT in medical science

The release of ChatGPT has initiated new thinking about AI-based Chatbot and its application and has drawn huge public attention worldwide. Researchers and doctors have started thinking about the promise and application of AI-related large language models in medicine during the past few months. Here, the comprehensive review highlighted the overview of Chatbot and ChatGPT and their current role in medicine. Firstly, the general idea of Chatbots, their evolution, architecture, and medical use are discussed. Secondly, ChatGPT is discussed with special emphasis of its application in medicine, architecture and training methods, medical diagnosis and treatment, research ethical issues, and a comparison of ChatGPT with other NLP models are illustrated. The article also discussed the limitations and prospects of ChatGPT. In the future, these large language models and ChatGPT will have immense promise in healthcare. However, more research is needed in this direction

Cu-Catalyzed ligand-free synthesis of rosuvastatin based novel indole derivatives as potential anticancer agents

Rosuvastatin based novel indole derivatives designed as potential anti-cancer agents were synthesized via a newly developed ligand-free, simple, straightforward and inexpensive one-pot method. The methodology involved a Cu-catalyzed coupling-cyclization of a rosuvastatin based alkyne with o-iodoanilides in the presence of CuI and K2CO3 in PEG-400. Three of the synthesized compounds showed promising anti-proliferative activities against cancer cell lines and an increase of p21 mRNA expression and apoptotic effects in zebrafish embryos/larvae.Peer reviewe