Synthesis, pharmacological and antiviral activity of 1,3-thiazepine derivatives

European Journal of Medicinal Chemistry
Marta StrugaRoberta Loddo

Abstract

The preparation of new fourteen thiourea and fourteen product of their condensation with 1,4-dibromobutane, viz. 1,3-thiazepine derivatives, of 10-isopropyl-8-methyl-4-aza-tricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione and 1-isopropyl-7-methyl-4-aza-tricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione is described. Elemental analysis, MS and (1)H NMR spectra confirmed the identity of the products. The molecular structure of linear disubstituted thiourea derivative and its cyclization product was determined by an X-ray crystal structure analysis. Two of new obtained compounds (6b' and 7a') were tested for their pharmacological activity on animal central nervous system (CNS) in behavioral animal tests. With relatively low acute toxicity (LD(50) lower than 2000 mg kg(-1) i.p.) they exhibited significant influence on spontaneous locomotor activity and body temperature. Additionally, compounds reduced number of the "head twitch" episodes after 5-hydroksytryptophan (5-HTP) administration. New compounds were evaluated in vitro against representatives of different virus classes, such as a HIV-1 (Retrovirus), a HBV (Hepadnavirus) and the single-stranded RNA(+) viruses Yellow fever virus (YFV) and Bovine viral diarrhea virus (BVDV), both belonging t...Continue Reading

Citations

Aug 15, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Carmen LimbanDiana Camelia Nuță
Jun 30, 2015·European Journal of Medicinal Chemistry·Anna BielenicaMarta Struga
Jan 23, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Franz SteppelerJacek Wojaczyński
Feb 10, 2017·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Patel NavinGildardo Rivera
May 27, 2014·Acta Crystallographica. Section E, Structure Reports Online·Joel T MagueMustafa R Albayati

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Antiviral Agents
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Hepadnaviridae
Hepatitis B Virus
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