Shankaraiah G. Konda

Rapid and selective deallylation of allyl ethers and esters using iodine in polyethylene glycol-400

A simple and selective deallylation of allyl ethers and esters using iodine (10 mol%) in polyethylene glycol-400 as a green reaction solvent is described. The reaction was performed at room temperature with various aryl/alkyl allyl ethers and esters in good to excellent yields. The present methodology includes inexpensive catalyst, easy work-up, benign reaction conditions and high selectivity.

Eco-friendly polyethylene glycol-400: a rapid and efficient recyclable reaction medium for the synthesis of thiazole derivatives

Abstract An efficient and convenient procedure for the synthesis of thiazole derivatives from α-haloketone, thiourea and substituted acetophenones using polyethylene glycol-400 as a green and recyclable solvent is described. Significant rate enhancement and improved yields have been observed.

Synthesis and biological activity of pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidin-4-one derivatives: in silico approach.

Xanthine oxidase (XO) is responsible for the pathological condition called gout. Inhibition of XO activity by various pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidine-4-one derivatives was assessed and compared with the standard inhibitor allopurinol. Out of 10 synthesized compounds, two compounds, viz. 3-amino-6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidin-4-one (3b) and 3-amino-6-(4-chloro-2-hydroxy-5-methylphenyl)-1H-pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidin-4-one (3g) were found to have promising XO inhibitory activity of the same order as allopurinol. Both compounds and allopurinol inhibited competitively with comparable Ki (3b: 3.56 µg, 3g: 2.337 µg, allopurinol: 1.816 µg) and IC50 (3b: 4.228 µg, 3g: 3.1 µg, allopurinol: 2.9 µg) values. The enzyme–ligand interaction was studied by molecular docking using Autodock in BioMed Cache V. 6.1 software. The results revealed a significant dock score for 3b (−84.976 kcal/mol) and 3g (−90.921 kcal/mol) compared with allopurinol (−55.01 kcal/mol). The physiochemical properties and toxicity of the compounds were determined in silico using online computational tools. Overall, in vitro and in silico study revealed 3-amino-6-(4-chloro-2-hydroxy-5-methylphenyl)-1H-pyrazolo[3,4-d]thiazolo[3,2–a]pyrimidin-4-one (3g) as a potential lead compound for the design and development of XO inhibitors.

An improved procedure for synthesis of some new 1,3-diaryl-2-propen-1-ones using PEG-400 as a recyclable solvent and their antimicrobial evaluation

An improved procedure for synthesis of some new 1,3-diaryl-2-propen-1-ones using PEG-400 as a recyclable solvent and their antimicrobial evaluation A simple and convenient route is described for the synthesis of novel hetero 1,3-diaryl-2-propen-1-ones (chalcones) by using recyclable PEG-400 as an alternative reaction solvent. The reaction is clean with excellent yield, shorter reaction time and reduces the use of volatile organic compounds (VOCs). All the synthesized compounds were evaluated for their antimicrobial activities against several pathogenic representatives. Poboljšan postupak sinteze nekih novih 1,3-diaril-2-propen-1-ona koristeći PEG-400 kao reciklirajuće otapalo i njihovo antimikrobno vrednovanje Opisana je jednostavna i pogodna metoda sinteze novih hetero 1,3-diaril-2-propen-1-ona (kalkona) koristeći poli(etilenglikol) (PEG-400) kao alternativno otapalo. Reakcija je jednoznačna, a uporaba hlapljivih organskih otapala je smanjena. Iskorištenja na produktima su visoka, a reakcijska vremena kraća. Svi sintetizirani spojevi testirani su na antimikrobno djelovanje na nekoliko patogenih mikroorganizama.

Multicomponent One-Pot Synthesis of Substituted Hantzsch Thiazole Derivatives Under Solvent Free Conditions

Thiazole derivatives were prepared by one-pot procedure by the reaction of α-haloketones, thiourea and substituted o-hydroxybenzaldehyde under environmentally solvent free conditions.