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Design, Syntheses and Antimicrobial Evaluations of Thio-Sulfadiazine Compounds.

Record Type:	Electronic resources : Monograph/item
Title/Author:	Design, Syntheses and Antimicrobial Evaluations of Thio-Sulfadiazine Compounds./
Author:	Maashi, Sarah.
Description:	1 online resource (198 pages)
Notes:	Source: Dissertations Abstracts International, Volume: 84-06, Section: B.
Contained By:	Dissertations Abstracts International84-06B.
Subject:	Organic chemistry. -
Online resource:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=29995149click for full text (PQDT)
ISBN:	9798358492684

Design, Syntheses and Antimicrobial Evaluations of Thio-Sulfadiazine Compounds.
Maashi, Sarah.

Design, Syntheses and Antimicrobial Evaluations of Thio-Sulfadiazine Compounds. - 1 online resource (198 pages)

Source: Dissertations Abstracts International, Volume: 84-06, Section: B.

Thesis (Ph.D.)--Saint Joseph's University, 2023.

Includes bibliographical references

With the emergence of antibiotic resistance, there is a growing concern that bacteria may evolve resistance to all antimicrobials currently accessible, posing a severe health risk to all of us. As a result, new antibiotics are required to limit the spread of these infections. Sulfonamides and their derivatives have gotten a lot of attention because of their great biological activity, low toxicity, and inexpensive cost. The pressing need to address antimicrobial resistance has rekindled interest in sulfonamides and related derivatives. Sulfadiazine, a known sulfonamide, was introduced in 1941 to prevent bacterial infections. It acts by inhibiting the DHPS enzyme in the folic acid pathway. Unfortunately, the effectiveness of sulfadiazine as an antibacterial agent has been limited due to the widespread development of drug resistance. In effort to overcome this problem, our work investigates the design, synthesis and evaluation of thiophene-containing compounds that may act as benzene isosteres. As part of this study, we used molecular docking approaches to predict the binding affinity of the designed compounds. We found that the amino thio-sulfadiazine compounds have the highest binding affinity than sulfadiazine. After successfully synthesizing the promising designed compounds, they were tested as antibacterial agents. It was observed that compounds 5b, 5g, and 5j were the most active against E. coli BW25113 with MIC values of 1.63 ± 0.2, 0.78 ± 0.01, and 0.40 ± 0.08 μg/mL, respectively than the parent sulfadiazine. In comparison to sulfadiazine, compounds 5a and 5i found to be the most effective against M. smegmatis with an MIC of 0.39 ± 0.05 and 0.19 ± 0.04 μg/mL, respectively, while compound 5a found to be the most active against B. subtilis with a lower MIC value equal to 6.25 ± 0.12 μg/mL. These results confirmed that thiophene moiety is the best suitable for replacing benzene moiety in sulfadiazine.

Electronic reproduction.
Ann Arbor, Mich. :
ProQuest,
2023

Mode of access: World Wide Web

ISBN: 9798358492684Subjects--Topical Terms:

523952
Organic chemistry.
Subjects--Index Terms:

Antibiotic resistant bacteriaIndex Terms--Genre/Form:

542853
Electronic books.

Design, Syntheses and Antimicrobial Evaluations of Thio-Sulfadiazine Compounds.
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