ArticleActa parasitologica2022
Synthesis and Biological Evaluation of Tetrahydropyrimidine and Dihydropyridine Derivatives Against Leishmania Major.
Article in Acta parasitologica, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 11 citations in OpenAlex.
- Lipase-Catalyzed Pathways to the Synthesis of Pharmacologically Active Amides.Methods in molecular biology (Clifton, N.J.) · 2027Article
- Synthesis and anti-antileishmanial profile of novel thiazolidine-4-one derivatives and molecular docking and molecular dynamics simulations studies.Scientific reports · 2026Article
- In Vitro antileishmanial evaluation, molecular docking, dynamics simulations, and DFT Studies of tetrahydropyridine derivatives as potential trypanothione reductase inhibitors.Scientific reports · 2026Article
- A novel inhibitory strategy ofFuture microbiology · 2025Article
- Synthesis of Nitrostyrylthiazolidine-2,4-dione Derivatives Displaying Antileishmanial Potential.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Synthesis, biological assessment, and computational investigations of nifedipine and monastrol analogues as anti-leishmanial major and anti-microbial agents.Molecular diversity · 2023Article
- 1,4-Dihydropyridine as a Promising Scaffold for Novel Antimicrobials AgainstFrontiers in microbiology · 2022Article
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
purposeA number of tetrahydropyrimidines and their bioisosteric dihydropyridines bearing chloro substituent at various positions of phenyl ring in C4 of main scaffolds were designed, synthesized and evaluated for antileishmanial activity.
methodsThe antileishmanial activity of the synthesized compounds was evaluated against promastigote and amastigote forms. Moreover, molecular docking studies of the compounds in pteridine reductase 1 (PTR1) pocket were carried out to describe the results of biological experiments.
resultsThe compounds exhibited moderate to good antileishmanial activity against promastigote and amastigote forms. Among the screened compounds, 1d and 2c were found as the most potent compounds against promastigote form with EC
conclusionAccording to structure-activity relationship (SAR) studies, the chloro substituent in different positions of phenyl ring at C4 of 1,2,3,4-tetrahydropyrimidine (THPM) and 1,4-dihydropyridine (DHP) rings and also the length of the chain belonging to the ester groups could be important for antileishmanial activity of these compounds. Most of these compounds exhibited low cytotoxicity against macrophages. Compounds 1 h, 2a, 2b and 2c revealed higher activity than glucantime while all compounds showed lower activity toward amphotericine B. Docking studies showed that the synthesized compounds were fit well in the PTR1 pocket. Compounds 1 h and 2c indicated the highest score docking among screened compounds in PTR1 enzyme.
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