Search engine for discovering works of Art, research articles, and books related to Art and Culture
ShareThis
Javascript must be enabled to continue!

Antileishmanial and Antibacterial Activities of Aminobenzothiazole Sulfonamides

View through CrossRef
Leishmaniasis and multidrug-resistant (MDR) bacterial infections remain major global health challenges due to drug toxicity and increasing antimicrobial resistance. In this study, a library of previously synthesized N-sulfonylated and N-alkylated aminobenzothiazole derivatives (19–39) was evaluated for antileishmanial and antibacterial activities. Antileishmanial screening against Leishmania tropica (Khyber Medical University-KMU 25 strain) using a promastigote viability assay revealed IC₅₀ values ranging from 57.10–415 µg mL-1, with compounds 27 (N-allyl-N-(benzo[d]thiazol-2-yl)-4-bromobenzenesulfonamide),  (IC₅₀ = 57.10 ± 5.02 µg mL-1) and 23 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-fluorobenzenesulfonamide),  (IC₅₀ = 68.07 ± 6.03 µg mL-1) showing the highest potency. Antibacterial activity, assessed by agar well diffusion and microbroth dilution, indicated that compounds 19 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-methylbenzenesulfonamide), 21 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-chlorobenzenesulfonamide), 22 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-nitrobenzenesulfonamide), 27 (N-allyl-N-(benzo[d]thiazol-2-yl)-4-bromobenzenesulfonamide), and 31  (N-allyl-N-(benzo[d]thiazol-2-yl)benzenesulfonamide), exhibited notable inhibition against Escherichia coli and Staphylococcus aureus, with MIC values ranging from 0.15 to 0.43 µg mL-1. These results identify aminobenzothiazole sulfonamides as promising dual-active scaffolds with potential relevance for future development of antileishmanial and antibacterial agents.
Title: Antileishmanial and Antibacterial Activities of Aminobenzothiazole Sulfonamides
Description:
Leishmaniasis and multidrug-resistant (MDR) bacterial infections remain major global health challenges due to drug toxicity and increasing antimicrobial resistance.
In this study, a library of previously synthesized N-sulfonylated and N-alkylated aminobenzothiazole derivatives (19–39) was evaluated for antileishmanial and antibacterial activities.
Antileishmanial screening against Leishmania tropica (Khyber Medical University-KMU 25 strain) using a promastigote viability assay revealed IC₅₀ values ranging from 57.
10–415 µg mL-1, with compounds 27 (N-allyl-N-(benzo[d]thiazol-2-yl)-4-bromobenzenesulfonamide),  (IC₅₀ = 57.
10 ± 5.
02 µg mL-1) and 23 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-fluorobenzenesulfonamide),  (IC₅₀ = 68.
07 ± 6.
03 µg mL-1) showing the highest potency.
Antibacterial activity, assessed by agar well diffusion and microbroth dilution, indicated that compounds 19 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-methylbenzenesulfonamide), 21 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-chlorobenzenesulfonamide), 22 (N-(benzo[d]thiazol-2-yl)-N-benzyl-4-nitrobenzenesulfonamide), 27 (N-allyl-N-(benzo[d]thiazol-2-yl)-4-bromobenzenesulfonamide), and 31  (N-allyl-N-(benzo[d]thiazol-2-yl)benzenesulfonamide), exhibited notable inhibition against Escherichia coli and Staphylococcus aureus, with MIC values ranging from 0.
15 to 0.
43 µg mL-1.
These results identify aminobenzothiazole sulfonamides as promising dual-active scaffolds with potential relevance for future development of antileishmanial and antibacterial agents.

Related Results

Target site bioanalysis and pharmacokinetics of antileishmanial drugs
Target site bioanalysis and pharmacokinetics of antileishmanial drugs
This thesis focuses on bioanalytical method development and validation of antileishmanial drugs amphotericin B, miltefosine, and paromomycin in human plasma and human skin tissue f...
Molecular Docking and Antileishmanial Potential of Isolated Compounds from Asparagus gracilis
Molecular Docking and Antileishmanial Potential of Isolated Compounds from Asparagus gracilis
Background: Leishmaniasis remains a neglected tropical disease with high global disease burden and limited safe therapeutic options. Medicinal plants offer an important source of b...
Sulfonamides: far from obsolete
Sulfonamides: far from obsolete
Sulfa drugs or sulfonamides were introduced in 1935 by the German physician Gerhard Domagk (1895-1964). Domagk worked closely with two chemists, Fritz Mietzsch and Josef Klarer. Th...
Unveiling a New Selenocyanate as a Multitarget Candidate with Anticancer, Antileishmanial and Antibacterial Potential
Unveiling a New Selenocyanate as a Multitarget Candidate with Anticancer, Antileishmanial and Antibacterial Potential
Currently, cancer, leishmaniasis and bacterial infections represent a serious public health burden worldwide. Six cinnamyl and benzodioxyl derivatives incorporating selenium (Se) a...
Overview on Design and Synthesis of Sulfonamide Derivative through Condensation of Amino Group Containing Drug
Overview on Design and Synthesis of Sulfonamide Derivative through Condensation of Amino Group Containing Drug
In medicinal and non-pharmacological chemistry, sulfonamides (SN) are an advisory functional group that forms the basis of many drugs. As such, they are very important. Recently, v...
Antiplasmodial and Antileishmanial Activities of a New Limonoid and Other Constituents from the Stem Bark of Khaya senegalensis
Antiplasmodial and Antileishmanial Activities of a New Limonoid and Other Constituents from the Stem Bark of Khaya senegalensis
Plasmodium falciparum and Leishmania sp. resistance to antiparasitic drugs has become a major concern in malaria and leishmaniasis control. These diseases are public health problem...
In Vitro Antileishmanial Activity and GC-MS Analysis of Whole Plant Hexane Fraction of Achillea wilhelmsii (WHFAW)
In Vitro Antileishmanial Activity and GC-MS Analysis of Whole Plant Hexane Fraction of Achillea wilhelmsii (WHFAW)
In this study, GC-MS analysis has shown that whole plant hexane fraction of Achillea wilhelmsii (WHFAW) consists of 66 compounds which exhibited antileishmanial activity. Antileish...
Investigating the Antibacterial Characteristics of Japanese Bamboo
Investigating the Antibacterial Characteristics of Japanese Bamboo
Natural materials, such as bamboo, is able to withstand the rough conditions posed by its environment, such as resistance to degradation by microorganisms, due to notable antibacte...

Back to Top