New 5-Thiazolyl-carbohydrazon-n-allyl-thiazolines Synthesis, characterization and antioxidant activity

Abstract

In an effort to obtain new NSAIDs, that act as COX-2 selective inhibitors with simultaneous iNOS inhibition properties and direct antioxidant activity, we designed a series of 8 new compounds bearing the 5-thiazolyl-carbohydrazon-N-allyl-thiazoline scaffold. The synthesized compounds were physicochemically characterized by: 1H-NMR, MS and elemental analysis. An initial, in vitro, free radical scavenging assay (DPPH bleaching) test showed that most compounds are superior to standard antioxidants Trolox and BHT.

Clean Grinding Technique: A Facile Synthesis and In Silico Antiviral Activity of Hydrazones, Pyrazoles, and Pyrazines Bearing Thiazole Moiety against SARS-CoV-2 Main Protease (Mpro)

“…An initial endeavor was to investigate the condensation reactions under solid-state conditions. Thus, grinding of 3-acetyl-7-amino-1-aryl-[1,2,4]triazolo [4,3- a ]pyrimidin-5(1 H )-one ( 1 ) [ 35 ] and 4-methyl-2-phenylthiazole -5-carbohydrazide ( 2 ) [ 36 ], in the presence of a few drops of acetic acid at room temperature, gave the condensation products N ’-[1-(7-amino-5-oxo-1-aryl-1,5-dihydro-[1,2,4] triazolo[4,3- a ]pyrimidin-3-yl)ethylidene]-4-methyl-2-phenylthiazole-5-carbohydrazides ( 3a – c ) ( Scheme 1 ).…”