Literature DB >> 31699608

Green chemistry appended synthesis, metabolic stability and pharmacokinetic assessment of medicinally important chromene dihydropyrimidinones.

Ashutosh K Dash1, Debaraj Mukherjee2, Abhijeet Dhulap3, Saqlain Haider4, Deepak Kumar5.   

Abstract

A green chemistry approach has been developed for the synthesis of chromene dihydropyrimidinone (CDHPM) using recyclable Fe/Al pillared clay catalyst. Pharmacokinetic parameters like aqueous solubility, lipophilicity, P-glycoprotein (P-gp) ATPase activity, permeability, plasma protein binding, red blood cell (RBC) partitioning, metabolic stability in liver microsomes and in silico computations have been studied for the most potent anticancer chromene dihydropyrimidinone hybrid 1. This compound exhibited low solubility, optimum lipophilicity, no P-gp inhibitory activity, intermediate permeability, high plasma protein binding, low RBC partitioning, acceptable metabolic stability in rat liver microsomes (RLM) as well as human liver microsomes (HLM) with transitional hepatic extraction ratio.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Chromene dihydropyrimidinone; Green chemistry; In silico studies; Pharmacokinetic studies

Year:  2019        PMID: 31699608     DOI: 10.1016/j.bmcl.2019.126750

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Catalytic Performance of One-Pot Synthesized Fe-MWW Layered Zeolites (MCM-22, MCM-36, and ITQ-2) in Selective Catalytic Reduction of Nitrogen Oxides with Ammonia.

Authors:  Agnieszka Szymaszek-Wawryca; Urbano Díaz; Bogdan Samojeden; Monika Motak
Journal:  Molecules       Date:  2022-05-06       Impact factor: 4.927

2.  Novel Dihydropyrimidinone Derivatives as Potential P-Glycoprotein Modulators.

Authors:  Sabera Bijani; Faraz Shaikh; Sheefa Mirza; Shirley Weng In Siu; Nayan Jain; Rakesh Rawal; Nigel G J Richards; Anamik Shah; Ashish Radadiya
Journal:  ACS Omega       Date:  2022-05-02
  2 in total

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