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.
ZooBotanica (SMC-Private) Limited
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...
Phytochemical analysis and in vitro antileishmanial activity of Basella alba extract cultivated in Iraq
Phytochemical analysis and in vitro antileishmanial activity of Basella alba extract cultivated in Iraq
Basella alba, widely known as Malabar spinach, is a fast-growing perennial native to tropical regions Worldwide. B. alba has been widely utilized in traditional medicine because of...
Cedrus deodara
Cedrus deodara
Background & objectives:
The existing antileishmanial drugs for complete cure of visceral leishmaniasis (kala-azar) are limited. The available drugs are either toxi...
Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach
Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach
With an estimated annual incidence of one million cases, leishmaniasis is one of the top five vector-borne diseases. Currently available medical treatments involve side effects, in...
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...
ANTILEISHMANIAL ACTIVITY EVALUATION OF BLACK CUMIN EXTRACTS AGAINST LEISHMANIA TROPICA
ANTILEISHMANIAL ACTIVITY EVALUATION OF BLACK CUMIN EXTRACTS AGAINST LEISHMANIA TROPICA
Objectives: In addition to the high cost of antileishmanial drugs, the resistance that develops against these drugs and their side effects has led to the investigation of leishmani...
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...

