A series of 17 compounds (12-16 b) with 2,4,5-trisubstitutedthiazole scaffold having 5-aryl group, 4-carboxylic acid/ester moiety, and 2-amino/amido/ureido functional groups were synthesised, characterised, and evaluated for their carbonic anhydrase (CA)-III inhibitory activities using the size exclusion Hummel-Dreyer method (HDM) of chromatography. Compound 12a with a free amino group at the 2position, carboxylic acid moiety at the 4-position, and a phenyl ring at the 5-position of the scaffold was found to be the most potent CA-III inhibitor (K i ¼ 0.5 lM). The presence of a carboxylic acid group at the 4-position of the scaffold was found to be crucial for the CA-III inhibitory activity. Furthermore, replacement of the free amino group with an amide and urea group resulted in a significant reduction of activity (compounds 13c and 14c, K i ¼ 174.1 and 186.2 lM, respectively). Thus, compound 12a (2-amino-5-phenylthiazole-4-carboxylic acid) can be considered as the lead molecule for further modification and development of more potent CA-III inhibitors.
Micellar catalysis exhibited by mixed surfactant systems and gemini surfactants was reviewed. The
review focused on mixed surfactant systems and tried to correlate the changes in the physico-chemical
properties of these systems to the variations of their catalytic activities. Mixed surfactant systems are
promising as the catalytic efficiency of some single surfactants was significantly enhanced in the
presence of other critically selected surfactants. The selection should consider the charge, size, and
structures of the head group as well as an appropriate length of hydrocarbon tail. The overall conclusion
has arrived the mixed surfactant systems could be a tool by which the reaction rate can be tuned by
changing the composition and/or the components’ structures. The higher catalytic activity of gemini
surfactants compared to conventional ones, their facile synthesis and liability for structure control
made them of superior choice for micellar catalysis.
Kinetics of oxidation of L-lysine by permanganate ion in a perchloric acid medium was investigated to explore the order of the reaction with respect to oxidant and substrate and to study the catalytic behaviour of sodium lauryl sulphate (SLS) and polyethylene glycol (PEG). The reaction was found to be first-order with respect to the oxidant and the substrate and zero-order with respect to hydrogen ion. Changes in the sodium sulphate concentration produce a non-significant variation in the rate of the reaction. SLS and PEG were found to catalyze the reaction. Surfactant catalysis was modelled by Piszkiewicz's cooperativity model, while polymer catalysis was explained with the help of the Benesi-Hildebrand equation. The temperature dependence of the rate of the reaction was elucidated, and activation parameters were obtained. Interestingly, the reaction was found to possess positive activation entropy indicating the dissociative nature of the transition state and outer-sphere electron transfer mechanism. A mechanism of the reaction that is supported by the experimental findings was suggested. KEYWORDS L-lysine, permanganate ion, micellar catalysis, polymer catalysis, outer sphere electron transfer mechanism.
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