TY - JOUR
T1 - Synthesis, characterization and derivatization of some novel types of mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones with antitumor, antiviral, antibacterial and antifungal activities - part I
AU - El-Sharief, Ahmed M.Sh
AU - Moussa, Ziad
N1 - Funding Information:
This work was supported by the Deanship of Scientific Research of Taibah University (project number: 245/429). Ziad Moussa (principle investigator) and Ahmed M. Sh. El-Sharief greatly acknowledge this generous financial support. We extend our gratitude to Prof. M.M. Al-Nozha (Taibah University president), Dr. A. Alharbe (Dean of Science).
PY - 2009/11
Y1 - 2009/11
N2 - Halogenated and alkylated N-arylcyanothioformanilides were reacted with the nucleophilic reagents triethylamine, hydrazine and diphenyldiazomethane to produce N-arylcyanothioformanilide ammonium salts, a thiosemicarbazide and a 2-(arylamino)-3,3-diphenylacrylonitrile, respectively. They also underwent several types of electrophilic reactions with aryl-, arylbisisocyanates and arylisothiocyanates to yield mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones. Treatment of imidazolidineiminothiones with hydrogen sulfide, substituted ortho-phenylenediamines and thiocarbohydrazide afforded the corresponding thiohydantoin, quinoxaline and imidazotriazine derivatives. Several of the synthesized products were subjected to in vitro biological evaluation against antitumor, antiviral, antimicrobial and antifungal strains. Most tested compounds showed significant activities.
AB - Halogenated and alkylated N-arylcyanothioformanilides were reacted with the nucleophilic reagents triethylamine, hydrazine and diphenyldiazomethane to produce N-arylcyanothioformanilide ammonium salts, a thiosemicarbazide and a 2-(arylamino)-3,3-diphenylacrylonitrile, respectively. They also underwent several types of electrophilic reactions with aryl-, arylbisisocyanates and arylisothiocyanates to yield mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones. Treatment of imidazolidineiminothiones with hydrogen sulfide, substituted ortho-phenylenediamines and thiocarbohydrazide afforded the corresponding thiohydantoin, quinoxaline and imidazotriazine derivatives. Several of the synthesized products were subjected to in vitro biological evaluation against antitumor, antiviral, antimicrobial and antifungal strains. Most tested compounds showed significant activities.
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U2 - 10.1016/j.ejmech.2009.07.019
DO - 10.1016/j.ejmech.2009.07.019
M3 - Article
C2 - 19664865
AN - SCOPUS:70349972338
SN - 0223-5234
VL - 44
SP - 4315
EP - 4334
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 11
ER -