Synthesis and HIV-1 Reverse Transcriptase Inhibitor Activity of Some 2,5,6-Substituted Benzoxazole, Benzimidazole, Benzothiazole and Oxazolo(4,5-b)pyridine Derivatives

Abstract

In this study, the synthesis of some benzoxazoles and their analogues were described and their antiviral activities were studied together with the previously synthesized 2,5,6-trisubstituted benzoxazole, benzothiazole, benzimidazole and oxazolo(4,5-b)pyridine derivatives. The reverse transcriptase (RT) inhibitory activity of these compounds was determined using a commercial kit and assay system which utilizes the scintillation proximity assay principle. The results are concentration at which the compound inhibits RT activity by 50%). The compounds inhibited the in vitro binding of thymidine to the RT enzyme exhibiting IC50 values between 6.3 x 10(5) mumol/l-0.34 mumol/l and their activities were compared to some standard drugs such as 3'-azido-2',3'-dideoxythymidine triphosphate and dideoxythymidine triphosphate.

Inhibition of human glutathione transferase P1-1 by novel benzazole Derivatives

“…The synthesis of these totally 33 benzazole compounds were published before [15][16][17][18][19][20][21][22].…”

Synthesis and Biological Evaluation of 2‐Substituted‐5‐(4‐nitrophenylsulfonamido)benzoxazoles as Human GST P1‐1 Inhibitors, and Description of the Binding Site Features

“…The benzoxazoles have been the aim of much research for many years because they constitute an important class of heterocyclic compounds exhibiting substantial chemotherapeutic activities 19–35. Recently, we reported some 2,5,6‐trisubstituted benzoxazole derivatives, which exhibit antimicrobial,27–29 antiviral,30, 31 antitumor activities, inhibiting eukaryotic topoisomerase II in a cell‐free system 32–35. The aim of this research was to develop new and effective hGST P1‐1 enzyme inhibitors from sulfonamido‐containing benzoxazole derivatives.…”

Synthesis and Antioxidant Activity of a New Class of Bis and Tris Heterocycles

“…The benzoxazole ring is one of the most common heterocycles in medicinal chemistry and plays an important role in designing new drugs. Substituted benzoxazoles possess diverse chemotherapeutic activities viz., antimicrobial 15–19, antiviral 20, and antitumor 21, 22. Benzothiazole derivatives have industrial applications as antioxidants 23, vulcanization accelerators, etc.…”