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Recent Progress in the Preparation of Novel Heterocyclic Compounds and Their Therapeutic Applications

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Applied Chemistry".

Deadline for manuscript submissions: closed (15 December 2023) | Viewed by 2798

Special Issue Editors


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Guest Editor
School of Chemistry & Physics, University of KwaZulu-Natal, Durban, South Africa
Interests: green synthesis; heterocyclic scaffolds; medicinal chemistry; sustainable synthesis; heterogeneous catalysts
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Chemistry, GITAM Institute of Sciences, GITAM University, Visakhapatnam, India
Interests: heterocyclic moieties; biological activity; organic synthesis; cascade reactions; microwaves; sonochemistry; grinding chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Heterocyclic compounds with pyrazole, pyridine, pyrimidine, pyrans, triazole, indole and isoxazole scaffolds offer distinct pharmacological benefits. These heterocyclic compounds control auto-immune disorders with their anti-rheumatoid, anti-inflammatory, antioxidant, anti-diabetic and anti-sclerotic activities. They also contribute to treatments of cancer, helminthic and other microbial diseases. Further, some fused heterocyclic rings append their microbial inhibitory properties and are also known to relax and calm the central nervous system by acting as depressants.

One pot synthesis of heterocyclic compounds is an efficient approach to avoid the separation of the reaction intermediates. This method conserves resources, offering better yields in a shorter time in a green environment. The one-pot synthesis in water, and eco-friendly solvents with the highest specific heat capacity, allow better reaction conditions. To further assure clean reactions, solvent-free systems have been explored using non-conventional techniques such as grinding, ultra-sonication and microwave irradiation. Grindstone reactions have received significant attention owing to their high yields with less expensive tools such as mortar and a pestle. These reactions offer cheaper and economic reaction conditions, contributing to authorizable reaction mechanisms. The chemistry and biology of nitrogen and oxygen-containing heterocyclic compounds will be the key theme of this issue, comprising both original research and review articles. It will focus on novel developments in the synthesis and reactivity of new heterocyclic moieties and their promising biological activities.

Prof. Dr. Sreekantha B. Jonnalagadda
Dr. Suresh Maddila
Guest Editors

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Keywords

  • green synthesis
  • one-pot reactions
  • N-heterocycles
  • O-heterocycles
  • MCRs
  • biological applications
  • heterogeneous catalysis

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Published Papers (1 paper)

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Research

14 pages, 2805 KiB  
Article
Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity
by Ibrahim S. Al Nasr, Waleed S. Koko, Tariq A. Khan, Nevin Gürbüz, Ismail Özdemir and Naceur Hamdi
Molecules 2023, 28(3), 1359; https://doi.org/10.3390/molecules28031359 - 31 Jan 2023
Cited by 9 | Viewed by 2348
Abstract
A series of [RuCl2(p-cymene)(NHC)] complexes were obtained by reacting [RuCl2(p-cymene)]2 with in situ generated Ag-N-heterocyclic carbene (NHC) complexes. The structure of the obtained complexes was determined by the appropriate spectroscopy and elemental analysis. In addition, we evaluated the biological [...] Read more.
A series of [RuCl2(p-cymene)(NHC)] complexes were obtained by reacting [RuCl2(p-cymene)]2 with in situ generated Ag-N-heterocyclic carbene (NHC) complexes. The structure of the obtained complexes was determined by the appropriate spectroscopy and elemental analysis. In addition, we evaluated the biological activities of these compounds as antienzymatic, antioxidant, antibacterial, anticancer, and antiparasitic agents. The results revealed that complexes 3b and 3d were the most potent inhibitors against AchE with IC50 values of 2.52 and 5.06 μM mL−1. Additionally, 3d proved very good antimicrobial activity against all examined microorganisms with IZ (inhibition zone) over 25 mm and MIC (minimum inhibitory concentration) < 4 µM. Additionally, the ligand 2a and its corresponding ruthenium (II) complex 3a had good cytotoxic activity against both cancer cells HCT-116 and HepG-2, with IC50 values of (7.76 and 11.76) and (4.12 and 9.21) μM mL−1, respectively. Evaluation of the antiparasitic activity of these complexes against Leishmania major promastigotes and Toxoplasma gondii showed that ruthenium complexes were more potent than the free ligand, with an IC50 values less than 1.5 μM mL−1. However, 3d was found the best one with SI (selectivity index) values greater than 5 so it seems to be the best candidate for antileishmanial drug discovery program, and much future research are recommended for mode of action and in vivo evaluation. In general, Ru-NHC complexes are the most effective against L. major promastigotes. Full article
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