A series of novel 2-substituted-thio-1,3,4-thiadiazoles bearing a 5-nitroaryl moiety including nitrofuran, nitrothiophene or nitroimidazole at the 5-position and a bulky residue attached to the 2-position of the thiadiazole ring were synthesised as potential antileishmanial agents. The target compounds were evaluated against the promastigote form of Leishmania major using the tetrazolium bromide salt (MTT) colorimetric assay. All test compounds exhibited high activity against L. major promastigotes with 50% inhibitory concentrations (IC(50)) ranging from 1.11 to 3.16 μM. The structure-activity relationship study indicated that the S-pendant group attached to the 2-position of the thiadiazole ring has a high flexibility for structural alteration therefore retaining good antileishmanial activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.3109/14756361003733654 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
extracts mediated synthesis of copper oxide nanoparticles and their biological applications.
Heliyon
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.
With the passage of time there is enormous development in the field of science and technology, however, human health remained the utmost concern. There are different strategies that helps us to treat various diseases but they have adverse reactions on our bodies. Nanobiotechnology is the advanced field consisting of new techniques and fabrication procedures for nanostructures for making drugs more effective against diseases in less time.
View Article and Find Full Text PDFNatural phytochemicals reverting M2 to M1 macrophages: A novel alternative Leishmaniasis therapy.
Microb Pathog
January 2025
Immunology lab, Biotechnology & Bioengineering, Indian Institute of Advanced Research, Gandhinagar, Gujarat, 382426, India. Electronic address:
Introduction: Leishmaniasis is a tropical parasitic disease caused by the protozoan Leishmania which remains a significant global health concern with diverse clinical manifestations. Transmitted through the bite of an infected sandfly, its progression depends on the interplay between the host immune response and the parasite. The disease outcome is linked to macrophage polarisation into M1 and M2 phenotypes.
View Article and Find Full Text PDFEvaluation of SB-83, a 2-amino-thiophene derivative, against Leishmania species that cause visceral leishmaniasis.
Int Immunopharmacol
January 2025
Infectious Diseases Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brazil. Electronic address:
Visceral leishmaniasis is a systemic disease that affects various internal organs and represents the most severe and fatal form of leishmaniasis. Conventional treatment presents significant challenges, such as prolonged management in hospital settings, high toxicity, and an increasing growing number of cases of resistance. In previous studies, our research group demonstrated the effective and selective activity of the 2-amino-thiophene derivative SB-83 in preclinical models of cutaneous leishmaniasis.
View Article and Find Full Text PDF2-Aminothiophene Derivatives-New Drug Candidates Against Leishmaniasis: Drug Design, Synthesis, Pharmacomodulation, and Antileishmanial Activity.
Pharmaceuticals (Basel)
January 2025
Laboratory of Synthesis and Drug Delivery, Department of Biological Sciences, State University of Paraíba, João Pessoa 58071-160, Brazil.
: Leishmaniasis is one of the 20 Neglected Tropical Diseases according to the WHO, affecting approximately 12 million people in four continents, generating serious public health problems. The lack of therapeutic options, associated with toxicity and the emergence of resistance to the few available drugs, makes it urgent to develop new drug options. In this context, the aims of this work are to expand the knowledge about the pharmacophore group responsible for the antileishmanial potential of 2-aminothiophene derivatives.
View Article and Find Full Text PDFIdentification of a New Pentafluorosulfanyl-Substituted Chalcone with Activity Against Hepatoma and Human Parasites.
Pharmaceuticals (Basel)
January 2025
Institute of Physiology, Charité-Universitätsmedizin Berlin, Corporate Member of the Freie Universität Berlin, Humboldt-Universität zu Berlin and Berlin Institute of Health, Charitéplatz 1, 10117 Berlin, Germany.
Background/objectives: New drugs are required for the treatment of liver cancers and protozoal parasite infections. Analogs of the known anticancer active and antileishmanial 2',4',6'-trimethoxychalcone SU086 were prepared and investigated.
Methods: The chalcones were prepared according to the Claisen-Schmidt condensation protocol and analyzed.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!