Fused triazolothienopyrimidines were prepared from the corresponding 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile. These precursors were intern prepared by employing the Gewald's reaction. All the newly synthesized compounds were characterized by spectral and analytical data. Title compounds displayed promising antibacterial and antifungal activities. Compound 3h which exhibited good antimicrobial activity was incorporated into SLN and characterized for particle size, entrapment efficiency (EE%), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and in-vitro release studies. It showed narrow particle size distribution with high entrapment efficiency. In-vitro release study of compound loaded SLNs in phosphate buffer of pH 7.4, exhibited a biphasic pattern with an initial burst and prolonged release over 24 h.
A series of novel triazole fused tetracyclic thienopyrimidines (III -X) were synthesized from the corresponding precursor 5-amino-4-cyano-3-methylthiophene-2-carboxylic acid ethyl ester I. The precursor were in turn prepared via the Gewald reaction. Structures of all the newly synthesized compounds were characterized by spectral and analytical data. All the tested compounds displayed promising antibacterial and antifungal activities.
In the title compound, C9H11NOS, the phenyl ring and formamide unit make a dihedral angle of 23.93 (14)°, whereas the (methylsulfanyl)methyl group is oriented at a dihedral angle of 61.31 (8)° with respect to the phenyl ring. There are intermolecular N—H⋯O hydrogen bonds, forming C(4) chains along the [010] direction. These polymeric chains are linked by C—H⋯O hydrogen bonds to form polymeric sheets in the (110) plane.
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