Seleem, Mohammed A. published the artcileSecond-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties, Safety of 4-Butylthiobenzamide, the main research area is methicillin resistant Staphylococcus aureus antibacterial phenylthiazole preparation; thiazole phenyl preparation methicillin resistant Staphylococcus aureus antibacterial.
A series of second-generation analogs for 2-(1-(2-(4-butylphenyl)-4-methylthiazol-5-yl)ethylidene)aminoguanidine 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. The hydrazide-containing analog I was identified as the most potent analog constructed thus far. The corresponding amine was 8 times less active. Finally, incorporating the nitrogenous side chain within an aromatic system completely abolished the antibacterial character. Replacement of the Bu group with cyclic bioisosteres revealed cyclohexenyl analog II, which showed significant improvement in in vitro anti-MRSA potency. Increasing or decreasing the ring size deteriorated the antibacterial activity. Compound I demonstrated a superior in vitro and in vivo pharmacokinetic profile, providing compelling evidence that this particular analog is a good drug candidate worthy of further anal.
Journal of Medicinal Chemistry published new progress about Antibacterial agents. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, Safety of 4-Butylthiobenzamide.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics