In 2019.0 BIOORG CHEM published article about DISCOVERY; DESIGN; POTENT; STAPHYLOCOCCI; OPTIMIZATION; IV in [Ghannam, Iman A. Y.; Abd El-Meguid, Eman A.; Ali, Islam H.; Sheir, Donia H.] Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Chem Nat & Microbial Prod Dept, Cairo 12622, Egypt; [El Kerdawy, Ahmed M.] Cairo Univ, Dept Pharmaceut Chem, Fac Pharm, Kasr El Aini St,POB 11562, Cairo, Egypt; [El Kerdawy, Ahmed M.] Cairo Univ, Mol Modeling Unit, Fac Pharm, Kasr El Aini St,POB 11562, Cairo, Egypt; [El Kerdawy, Ahmed M.] New Giza Univ, Dept Pharmaceut Chem, Fac Pharm, Km 22 Cairo Alexandria Desert Rd, Cairo, Egypt in 2019.0, Cited 41.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4. Safety of 4′-Hydroxyacetophenone
A series of new 2-arylbenzothiazole derivatives (4, 5, 6a-j, 7a-i and 8a,b) was synthesized and tested for their antimicrobial activity against different Gram-positive, Gram-negative bacteria and yeast using ciprofloxacin and fluconazole as positive controls for the antibacterial and antifungal activities, respectively. The target compounds showed stronger inhibitory activity against Gram-negative than Gram-positive bacteria. The minimum inhibitory concentration (MIC) values were determined for those compounds showed zone of inhibition >= 13 mm. Based on the MIC values for the tested compounds against E. coli, compounds (4, 5, 6c, 6d, 6g, 6i, 6j, 7b, 7c, 7g and 8a) were selected and tested for their E. coli gyrase inhibitory activity. The tested compounds showed moderate inhibitory activity against E. coli gyrase. Compounds 5, 6c, 6i, 6j and 7b displayed high inhibitory activity against E. coli gyrase with IC50 values below 10 mu M, however, they were less active than ciprofloxacin (E. coli gyrase IC50 = 1.14 mu M). The p-hydroxy-m-methoxy benzothiazole analogue 6c was the most active tested compound (E. coli gyrase IC50 = 4.85 mu M). Quantitative structure-activity relationship (QSAR) study was also implemented for the newly synthesized compounds. The QSAR study indicated that the structural feature that governs the anti-microbial activity for the newly synthesized benzothiazole derivatives is their structural hydrophilic-lipophilic balance what agrees with the chemical intuition where this balance governs their cellular absorption and so their antimicrobial activity. Molecular docking showed that the newly synthesized compounds possess the required structural feature for E. coli gyrase B inhibition through interaction with the key amino acids Asp73 and Gly77.
About 4′-Hydroxyacetophenone, If you have any questions, you can contact Ghannam, IAY; Abd El-Meguid, EA; Ali, IH; Sheir, DH; El Kerdawy, AM or concate me.. Safety of 4′-Hydroxyacetophenone
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles