Urea derivatives carrying a thiophenylthiazole moiety: Design, synthesis, and evaluation of antitubercular and InhA inhibitory activities was written by Keles Atici, Rueveyde;Dogan, Senguel Dilem;Guenduez, Miyase Gozde;Krishna, Vagolu Siva;Chebaiki, Melina;Homberset, Haavard;Lherbet, Christian;Mourey, Lionel;Toenjum, Tone. And the article was included in Drug Development Research in 2022.Formula: C8H4N2O This article mentions the following:
The recent emergence of drug-resistant strains of Mycobacterium tuberculosis (Mtb) has complicated and significantly slowed efforts to eradicate and/or reduce the worldwide incidence of life-threatening acute and chronic cases of tuberculosis. To overcome this setback, researchers have increased the intensity of their work to identify new small-mol. compounds that are expected to remain efficacious antimicrobials against Mtb. Here, we describe our effort to apply the principles of mol. hybridization to synthesize 16 compounds carrying thiophene and thiazole rings beside the core urea functionality (TTU1-TTU16). Following extensive structural characterization, the obtained compounds were initially evaluated for their antimycobacterial activity against Mtb H37Rv. Subsequently, three derivatives standing out with their anti-Mtb activity profiles and low cytotoxicity (TTU5, TTU6, and TTU12) were tested on isoniazid-resistant clin. isolates carrying katG and inhA mutations. Addnl., due to their pharmacophore similarities to the well-known InhA inhibitors, the mols. were screened for their enoyl acyl carrier protein reductase (InhA) inhibitory potentials. Mol. docking studies were performed to support the exptl. enzyme inhibition data. Finally, drug-likeness of the selected compounds was established by theor. calculations of physicochem. descriptors. In the experiment, the researchers used many compounds, for example, 3-Cyanophenylisocyanate (cas: 16413-26-6Formula: C8H4N2O).
3-Cyanophenylisocyanate (cas: 16413-26-6) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.Formula: C8H4N2O
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics