In 2022,Fayed, Eman A.; Mohsen, Marwa; El-Gilil, Shimaa M. Abd; Aboul-Magd, Dina S.; Ragab, Ahmed published an article in Journal of Molecular Structure. The title of the article was 《Novel cyclohepta[b]thiophene derivative incorporating pyrimidine, pyridine, and chromene moiety as potential antimicrobial agents targeting DNA gyrase》.Category: esters-buliding-blocks The author mentioned the following in the article:
To cultivate novel and effectual antimicrobial agents, the triumphant synthesis of a novel class of cyclohepta-thieno-pyrimidines, I, II [R = Me, 4-MeC6H4, 4-ClC6H4, etc.; R1 = Me, NC, H2OC], cyclohepta[b]thiophene appended 2-imino-2H-chromene-3-carboxamide and 3-imino-3H-benzo[f]chromene-2-carboxamide derivatives , III [R2 = H; R3 = H, Br; R2R3 = C4H4] were presented to enrich their biol. behavior. The desired mols. underwent in-vitro appraisal for their antimicrobial activity, demonstrating encouraging results. Besides, the time-kill kinetics, antibiofilm activity and the DNA gyrase inhibition of the active thiophene compounds were evaluated. The DNA gyrase inhibition by the active thiophenes was also determined with IC50 values to range between (5.3-18.7μM) compared with Levofloxacin and Ciprofloxacin. Also, the sum of the Fractional Inhibitory Concentration Index (ΣFICI) was used to assess synergy between thiophenes and Levofloxacin. Addnl., the antimicrobial activity of the most active thiophene derivative was analyzed after γ-irradiation Moreover, the in-silico prediction methodol. was contemplated for foretelling the physicochem., pharmacokinetic and ADME traits of the most active synthesized compounds and the standard reference drugs: Levofloxacin and Ciprofloxacin. The docking examination was carried out for the most promising derivatives, I, III [R2 = R3 = H] IV [R4 = H2N, (2-cyanoacetyl)amino, (2-chloroacetyl)amino], Novobiocin, and Levofloxacin inside the active site of DNA gyrase, and their resp. docking scores were contrasted with the scores of the above-mentioned standard drugs. In the experiment, the researchers used many compounds, for example, Ethyl 2-methyl-3-oxobutanoate(cas: 609-14-3Category: esters-buliding-blocks)
Ethyl 2-methyl-3-oxobutanoate(cas: 609-14-3) belongs to ketone compounds. Ketones are highly reactive, although less so than aldehydes, to which they are closely related. Much of their chemical activity results from the nature of the carbonyl group. Ketones readily undergo a wide variety of chemical reactions.Category: esters-buliding-blocks
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics