In the present communication, we conceived a new synthetic approach for the preparation of novel thiazolyl-lactam/thiazole analogs. The reaction was started through cyclization of ketone with thiourea along with substituted aryl aldehydes to culminate imine derivatives which subsequently cyclized with thioglycolic acid/chloroacetyl chloride to produce final compounds. The structural elucidation of newly synthesized compounds was performed through elemental detections, FT-IR, 1 HNMR, and Mass spectrometric techniques. Antimicrobial studies were performed for all synthesized molecules by serial dilution method by tacking the positive (K. pneumonia, S. aureus, B. subtills) and negative (P. aeruginosa and E. coli.) bacterial strains. The in vitro antimicrobial screening results show that the compounds 2e, 3c, and 3d containing o-hydroxy, p-chloro, and p-nitro substituent respectively exhibit exceptional activity against S. aureus while compounds 2d and 3f bearing p-nitro and o-chloro substituent respectively were deemed to be the most competent against B. subtilis. Compounds 2d (p-nitro) and 2f (o-chloro) were found to be most potent against E. coli. In gram-negative bacterial strains, compounds 2c (p-chloro), 2g (4-OH,-OCH3), 3b (phydroxy), and 3e (o-hydroxy) were extremely potent against P. aeruginosa while compound 2e containing o-hydroxy group shows excellent activity against E.coli.
A biocompatible nano-drug delivery vehicle can efficiently deliver the toxic drug to the targeted site in nano-quantity to treat cancer patients. Considering this, the current study aims to fabricate stable egg albumin nanoparticles by using chloroacetic acid to modify their surfaces. The carboxyl functionalized egg albumin (FEA) nanoparticles were prepared through the desolvation process using ethanol as the desolvating agent; the generated nanoparticles were stabilized by glutaraldehyde. To obtain stable nanoparticles of suitable size, various reaction parameters viz concentration of FEA, pH, agitation speed, glutaraldehyde concentration, and rate of ethanol addition were examined. In neutral and alkaline mediums, we can get nanoparticles of 120-160 nm with -32 mV zeta potential. The pH of the medium played a decisive role, which strongly influences the FEA particle diameter and surface charge, while other parameters show little influence. SEM monochrome image of functionalized EA nanoparticles also supported the particle size of around 130 nm. Gallic acid (GA) has been encapsulated under optimal desolvation conditions using the FEA/GA acid ratios of 1:1, 2:1, 4:1, and 8:1. The obtained GA entrapped FEA spherical nanoparticles (GA-FEA) had a -30.9mV zeta potential and were negatively charged. At a 2:1 polymer/drug ratio, an entrapment efficiency (EE) of 90.4 % (w/w) and drug loading capacity of about 28.7 % (w/w) were achieved. This work is beneficial to the scientists involved in the field of cancer research.
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