Synthesis, Antimicrobial Activity and Molecular Docking Study of Thiazole Derivatives

Abstract

in Wiley Online Library (wileyonlinelibrary.com).The reaction of 4-thiochromane thiocarbohydrazone with a series of hydrazonoyl halides in dioxane in the presence of triethylamine afforded novel thiochromane derivatives incorporating 1,3-thiazole moiety. The structure of the latter compounds was established by elemental analysis and spectral technique and by their chemical transformation. Moreover, the antimicrobial activity of the newly synthesized compounds was screened and the results showed that some compounds have higher activity than the applied fungicide and bactericide. The antimicrobial activity of the most active compounds was interpreted by molecular docking study.

Design, Synthesis, DNA Binding, and Docking Studies of Thiazoles and Thiazole‐Containing Triazoles as Antibacterials

“…Eight out of ten biologically active substances contains heterocyclic compounds. Among them, Thiazole and [1, 2,4] triazole derivatives are one of the important classes of heterocyclic compounds which has various biological activities and has been found applications in drug development for the treatment of inflammation, bacterial, HIV infection, anti‐Alzheimer, anti‐oxidant, antimicrobial, antiviral, anticancer, and antimalarial etc. In the current study two series of compounds, 4 a‐g and 5 a‐f were synthesized, series 4 a‐g contains thiazole derivatives with low molecular mass and small structure compared to the other series 5 a‐f incorporating thiazole and triazole in a single molecular framework.…”

“…In the current study two series of compounds, 4 a‐g and 5 a‐f were synthesized, series 4 a‐g contains thiazole derivatives with low molecular mass and small structure compared to the other series 5 a‐f incorporating thiazole and triazole in a single molecular framework. Since thiazole and triazole derivatives are widely used in the treatment of bacterial infections ,. A well‐established target for antibacterial action is bacterial cell wall peptidoglycan synthesis which is a common feature present in gram positive and gram negative bacteria .…”

Review of the synthesis and biological activity of thiazoles

“…Reacting of thiochroman-4-thiocarbohydrazone 175 with hydrazonoyl chlorides derivatives 165 gaves thiazole compounds 177 (Scheme 40). [65] In the same way, using different types of hydrazonoyl chlorides 178, reacted with thiochroman-4-thiocarbohydrazone 175 to give the compounds 180 (Scheme 41). [65] 3-(4-(Dimethylamino)benzylidene)thiochroman-4-one 181 was reacted with thiosemcarbazide 74 to give 3-(4-(dimethylamino)phenyl)-3,4-dihydrothiochromeno[4,3-c] pyrazole-2(1H)-carbothioamide 182.…”

“…[65] In the same way, using different types of hydrazonoyl chlorides 178, reacted with thiochroman-4-thiocarbohydrazone 175 to give the compounds 180 (Scheme 41). [65] 3-(4-(Dimethylamino)benzylidene)thiochroman-4-one 181 was reacted with thiosemcarbazide 74 to give 3-(4-(dimethylamino)phenyl)-3,4-dihydrothiochromeno[4,3-c] pyrazole-2(1H)-carbothioamide 182. The last carbothioamide derivative 184 reacted with hydrazonoyl chlorides 165 and 178 to provide the thiazole derivatives 183 and 184, respectively (Scheme 42).…”

Synthesis of new thiazole and thiazolyl derivatives of medicinal significant-a short review

“…Synthesis procedureFarghaly et al13 described the synthesis of new thiazole derivatives. The thiocroman-4-thiocarbohydrazone was used in this work as starting material for synthesis of new series of thiochromanes incorporating thiazole moiety by its reaction with a variety of hydrazonoyl chlorides using triethylamine as a catalyst(Figure 4).…”