Synthesis of sulfadiazinyl acyl/aryl thiourea derivatives as calf intestinal alkaline phosphatase inhibitors,pharmacokinetic properties,lead optimization,Lineweaver-Burk plot evaluation and binding analysis

To seek the new medicinal potential of sulfadiazine drug, the free amino group of sulfadiazine was exploited to obtain acyl/aryl thioureas using simple and straightforward protocol. Acyl/aryl thioureas are well recognized bioactive pharmacophore containing moieties. A new series (4a–4j) of sulfadiazine derived acyl/aryl thioureas was synthesized and characterized through spectroscopic and elemental analysis. The synthesized derivatives 4a–4j were subjected to calf intestinal alkaline phosphatase (CIAP) activity. The derivative 4a–4j showed better inhibition potential compared to standard monopotassium phosphate (MKP). The compound 4c exhibited higher potential in the series with IC₅₀ 0.251?±?0.012?µM (standard KH₂PO₄ 4.317?±?0.201?µM). Lineweaver-Burk plots revealed that most potent derivative 4c inhibition CIAP via mixed type pathway. Pharmacological investigations showed that synthesized compounds 4a–4j obey Lipinsk’s rule. ADMET parameters evaluation predicted that these molecule show significant lead like properties with minimum possible toxicity and can serve as templates in drug designing. The synthetic compounds show none mutagenic and irritant behavior. Molecular docking analysis showed that compound 4c interacts with Asp273, His317 and Arg166 amino acid residues.     

Surface properties and sub-surface aggregate assimilation of rhamnolipid surfactants in different aqueous systems

Tensioactive properties of rhamnolipids produced by a Pseudomonas aeruginosa strain were investigated in the presence or absence of Sr²⁺ or Pb²⁺. Surface and interfacial properties, and aggregate forming properties and morphologies were studied by various techniques including scanning electron microscopy. When the pH of a rhamnolipid aqueous solution (40 mg/l) was increased from 5 to 8, irregular vesicles gradually took the shape of oligo-vesicles, then regular vesicles and finally smaller spherical vesicles. Addition of metal ions controlled the aggregates’ morphology and stability, and influenced the surface and interfacial behavior of rhamnolipid solutions.     

Biological control: a novel strategy for the control of the plant parasitic nematodes

Antonie van Leeuwenhoek - Plant parasitic nematodes (Root-knot nematodes, Meloidogyne spp.) are rounded worms, microscopic, and cause many agricultural economic losses. Their attacks have a direct...