Hetarylcyanamides: Synthesis of Novel Thiazole, Triazole and Pyrimidine Derivatives and Prediction of their Biological Activity via PASS Inet

Khodairy, Ahmed; Moustafa, Amr H.; W. Ahmed, Walaa

doi:10.18576/jpac/030310

Hetarylcyanamides: Synthesis of Novel Thiazole, Triazole and Pyrimidine Derivatives and Prediction of their Biological Activity via PASS Inet

Document Type : Original Article

Authors

Department of Chemistry, Faculty of Science, Sohag University, Sohag 82524, Egypt

10.18576/jpac/030310

Abstract

Some new N-thiazolylaminopyrimidine derivatives 3a,b have been synthesized via the reaction of 1-(4,6-
dimethylpyrimidin-2-yl)thiourea 2, obtained via sulfidation of cyanamide 1a with phenacyl bromides. Acid hydrolysis of
N-(pyrimidin-2-yl)cyanamides 1b,c gave the corresponding pyrimidinylurea derivatives 4a,b. Reaction of cyanamide 1b
with thieno[2,3-b]thiophene derivative 5, at molar ratios (1:1 or 2:1), gave the unexpected thienopyrimidine derivative 6,
not the expected bis-thienopyrimidine derivative 7. Triazolylaminopyrimidine derivative 8 has been obtained via the
heterocyclization reaction of cyanamide 1b with benzhydrazide. Prediction the activity spectra of synthesized compounds
using PASS Inet at Pa > 70%, showing high probability of Mucomembranous protector, Transcription factor STAT
inhibitor and Gluconate 2-dehydrogenase (acceptor) inhibitor.

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