Ectoine gel transdermal formulation as a novel therapeutic approach in melanoma using 3D printed microneedles.

A 7%w/w ectoine formula, from natural source, is formulated to reduce melanomagenesis, enhance penetration by 3D printed microneedles (MNs), with specified length, diameter and tip to ensure painless effect. Ectoine gel formulations were prepared using Carbopol 940 and Pluronic (F127). The effect of the polymers on pH, viscosity, spreadability, and the , release profiles was obtained.

From Phenylthiazoles to Phenylpyrazoles: Broadening the Antibacterial Spectrum toward Carbapenem-Resistant Bacteria.

The narrow antibacterial spectrum of phenylthiazole antibiotics was expanded by replacing central thiazole with a pyrazole ring while maintaining its other pharmacophoric features. The most promising derivative, compound , was more potent than vancomycin against multidrug-resistant Gram-positive clinical isolates, including vancomycin- and linezolid-resistant methicillin-resistant MRSA), with a minimum inhibitory concentration (MIC) value as low as 0.5 μg/mL.

Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.

A series of second-generation analogues for 2-(1-(2-(4-butylphenyl)-4-methylthiazol-5-yl)ethylidene)aminoguanidine (1) have been synthesized and tested against methicillin-resistant Staphylococcus aureus (MRSA). The compounds were designed with the objective of improving pharmacokinetic properties. This main aim has been accomplished by replacing the rapidly hydrolyzable Schiff-base moiety of first-generation members with a cyclic, unhydrolyzable pyrimidine ring.