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Efficient synthesis and characterization of new ligand and their transition metal complexes derived from 4-methyl-1,2,3-thiadiazoles-5-carboxylic acid hydrazide Pages 531-540 Download PDF

Authors: Amol D. Kale, Ram B. Kohire, Gautam P. Sadawarte, Rajendra P. Phase, Vasant B. Jagrut

DOI: 10.5267/j.ccl.2024.2.006

Keywords: Acid hydrazide, Heterocyclic ligand, Metal complexes, Microwave irradiation, Biological activity

Abstract:

Synthesis of the new metal complexes, by allowing the condensation of Ligand, HL, (E)-N'-(2-hydroxy-5-methoxybenzylidene)-4-methyl-1,2,3-thiadiazole-5-carbohydrazide (3) with some transition metals. Here an attempt is also made to compare reported conventional methods with microwave irradiation for synthesized compounds. Spectroscopic technique, IR, ¹H-NMR, C¹³NMR, elemental analysis and TGA-DTA were used to characterize synthesized ligands and their complexes. The metal complexes were also evaluated for in vitro antimicrobial screening.

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Synthesis and biological activity of rhodanine-furan conjugates: A review Pages 287-302 Download PDF

Authors: Yuliia Matiichuk, Iryna Drapak, Natalia Darmograi, Nataliia Bartoshyk, Yana Drapak, Vasyl Matiychuk

DOI: 10.5267/j.ccl.2023.12.003

Keywords: Rhodanine, Furan, Heterocyclic conjugates, Synthesis, Biological activity

Abstract:

Rhodanines are recognized as privileged heterocycles in medicinal chemistry. The main achievements include the development of drug-like molecules with numerous biological activities as well as approved drugs. The Furan nucleus is considered one of the promising heterocyclic cores in medicinal chemistry that showed numerous ranges of activity. The combination of several heterocycles in a one molecule commonly provides much more interest in the enhanced activity profile of its analogs than their parent separate constituents. Such conjugates are promising objects for modern medicinal chemistry. In this review paper recent advances in the synthesis and biological activities rhodanine-furan conjugates which its application in the different field of drug discovery.

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Nitro-functionalized analogues of 1,3-Butadiene: An overview of characteristic, synthesis, chemical transformations and biological activity Pages 15-30 Download PDF

Authors: Mikołaj Sadowski, Karolina Kula

DOI: 10.5267/j.ccl.2023.9.003

Keywords: Nitrobutadiene, Synthesis, Spectral Characteristics, Chemical Transformation, Biological activity

Abstract:

The nitrovinyl moiety is surely one of the most reactive fragments in organic chemistry, continuously employed to explore original pathways and reach new targets. One of the most important classes of chemicals containing this fragment are nitro-functionalised analogues of 1,3-butadiene. In this paper a comprehensive review study of these compounds is performed. The manuscript includes an analysis of physicochemical properties, spectral characteristic, synthesis, biological activity, and possible transformations of nitro substituted analogues of 1,3-butadiene. The analysis was divided into several parts, depending on the number of nitro groups included in the structure of a 1,3-butadiene analogue. In addition, the work includes information about hazards and safety principles when working with nitro compounds. Based on the analysis of the literature, it can be concluded that nitro-functionalised analogues of 1,3-butadiene exhibit diversified profile of properties, and an outstanding potential as valuable reagents in organic synthesis useful to obtain heterocycles that can be applied in medicine.

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Synthesis, characterization, and biological activities of five new trivalent lanthanide complexes of hydrazine and 3,3’-thiodipropanoic acid Pages 721-732 Download PDF

Authors: K. Kumar, S. Murugesan, T. M Muneeswaran, C. M. Ramakritinan

DOI: 10.5267/j.ccl.2023.5.003

Keywords: Hydrazine, Carboxylic Acid, Lanthanoids, Metal Complexes, Biological Activity

Abstract:

Some new hydrazine complexes of trivalent lanthanide 3,3’-thiodipropanoates of empirical formulae [M(N₂H₅)(tdp)₂] and [Pr(N₂H₅)(tdp)₂·H₂O], where M = La, Ce, Sm and Nd, H₂tdp = 3,3’-thiodipropanoic acid, have been prepared and characterized by elemental analysis, mass, FTIR, Raman and electronic spectral, powder X-ray diffraction, scanning electron microscopy (SEM) and simultaneous TG–DTA techniques. The presence of bidentate carboxylate anion and coordinated N2H5 in these complexes are confirmed by IR spectra. TGA/DTA results confirmed that all the rare earth metal complexes give the corresponding metal carbonate (heating up to 1000 °C) through a metal oxalate intermediate. SEM images of Pr2O3 residue obtained from its complex show nano-sized clusters, thus the complex may be used as a precursor for nano-Pr₂O₃ preparation. The synthesized complexes show good antimicrobial activity against six bacteria (Bacillus cereus, Staphylococcus aureus, Proteus vulgaris, Pseudomonas aeruginosa, Escherichia coli, and Serratia species) and four fungi (Candida albicans, Aspergillus niger, Aspergillus fumigatus, and Penicillium variance) as assessed by in vitro biological activity.

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Synthetic approaches, modification ability and biological activity of 1,3,4-thiadiazole based [5+5] annelated heterosystems: Mini-review Pages 769-780 Download PDF

Authors: Maryan Lelyukh, Maria Zhukrovska, Zoryana Komarenska, Vadym Flud, Stefano Harkov

DOI: 10.5267/j.ccl.2023.4.004

Keywords: Fused heterocycles, Thiadiazoles, Synthesis, Structural modification, Biological activity

Abstract:

Condensed bicyclic systems with thiadiazole core being annelated to other five-membered heterocycles such as 1,3-thiazole, imidazole or 1,2,4-triazole occupy prominent place in medicinal chemistry because of their broad spectrum of pharmacological activities. The combination of several heterocycles into a bicyclic system commonly provides much more interest in the enhanced activity profile of its analogs than their parent separate constituents. In this review, we summarized the literature data about the main approaches for obtaining and possible directions of structural modification of the most common 1,3,4-thiadiazole containing [5+5] annelated heterosystems as promising objects for modern medicinal chemistry.

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Synthesis, spectroscopic characterization and biological activities of some metal complexes with new heterocyclic azodye ligand 2-(2-hydroxynaphthalen-1-yl azo)-pyridin-3-ol Pages 55-64 Download PDF

Authors: V. G. Vidya, V. Sadasivan

DOI: 10.5267/j.ccl.2022.9.006

Keywords: 2-amino-3-hydroxypyridine, β-naphthol, Azodye, DNA cleavage, Biological activity

Abstract:

Metal complexes of [2-(2-hydroxynaphthalen-1-ylazo)-pyridin-3-ol] are derived from 2-amino-3-hydroxypyridine and β-naphthol was synthesized and characterized by thermal, spectral and analytical tools. The ligand was reacted with Mn(II), Fe(II), Co(II), Ni(II), Cu(II) and Zn(II) in 1:2 stoichiometry. The IR spectra confirms the azo ligand coordination to metal ions via azo nitrogen and phenolic oxygen of pyridine after deprotonation. Both IR and 1HNMR spectra recorded involvement of deprotonated hydroxyl groups with proton displacement. The magnified fluorescence was shown by Mn(II) and Ni(II) complexes. None of the prepared ligands or complexes show any NLO activity with KDP as standard. The DNA cleavage and anticancerous activities done. The influence of zinc chelates on cure characteristics of rubber compounds was estimated based on rheometer measurements. The ligand and metal complexes are tested in vitro against some bacteria and fungi species. The antioxidant activities, DNA cleavage and anticancerous activities done. Ligand and its complexes catalysed cleavage of DNA.

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Synthetic and therapeutic potential of 4-thiazolidinone and its analogs Pages 119-138 Download PDF

Authors: Neetu Agrawal

DOI: 10.5267/j.ccl.2020.11.002

Keywords: 4-Thiazolidinone, Heterocyclic, Synthesis, Biological Activity, 5-Membered Ring

Abstract:

Past researches on 4-thiazolidinone nucleus have revealed the prominent potential of derivatives containing this nucleus to be developed as a potent therapeutic agent. Because of these biological activities, their structure-activity relationship has created an interest for medicinal chemists leading to the discovery of a number of lead molecules. This review highlights the routes for its synthesis and summarizes the past and recent studies on its biological activities to guide the medicinal chemists working on this nucleus in the development of clinically viable drugs.

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Fast and green synthesis of biologically important quinoxalines with high yields in water Pages 183-188 Download PDF

Authors: Hossein Ghafuri

Keywords: 1-2-Diketones, Biological activity, Diamines, Quinoxaline, Water

Abstract:

Optimal method were developed for the green synthesis of quinoxaline derivatives based on the highly efficient and simple condensation reaction of various aromatic 1,2-diketones and 1,2-diamines in nearly quantitative yields in water. In this method we did not use any catalyst. The very mild reaction conditions, the high yields of the products, and the absence of any catalyst make this methodology an efficient and green route for synthesis of quinoxalines.

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Microwave synthesis, spectral, thermal, and antimicrobial activities of some transition metal complexes involving 5-bromosalicylaldehyde moiety Pages 163-174 Download PDF

Authors: Rajendra K. Jain, A. P. Mishra

DOI: 10.5267/j.ccl.2012.7.003

Keywords: 5-Bromosalicylaldehyde, Aniline, Biological activity, Microwave synthesis, Thermal analysis

Abstract:

The coordination complexes of Co(II), Ni(II) and Cu(II) derived from 5-bromosalicylidene-3,4-dimethylaniline (BSMA) and 5-bromosalicylidene-3,4-dichloroaniline (BSCA) have been synthesized by conventional as well as microwave methods. These compounds have been characterized by elemental analysis, FT-IR, molar conductance, electronic spectra, 1H-NMR, FAB-mass, ESR, magnetic susceptibility, electrical conductivity and thermal analysis. The complexes are coloured and stable in air. Analytical data revealed that all the complexes exhibited 1:2 (metal: ligand) ratio with coordination number 4 or 6. IR data shows that the ligand coordinates with the metal ions in a bidentate manner through the phenolic oxygen and azomethine nitrogen. FAB-mass and thermal data show degradation pattern of the complexes. Solid state electrical conductivity studies reflect semiconducting nature of the complexes. The Schiff base and metal complexes show a good activity against the Gram-positive bacteria; Staphylococcus aureus and Gram-negative bacteria; Escherichia coli and fungi Aspergillus niger and Candida albicans.

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Synthesis of novel dihydropyrimidin-2(1h)-ones derivatives using lipase and their antimicrobial activity Pages 59-68 Download PDF

Authors: Bhushan N. Borse, Vasant S. Borude, Sanjeev R. Shukla

DOI: 10.5267/j.ccl.2012.3.001

Keywords: Biocatalyst, Biological activity, Rhizopus Oryzae

Abstract:

A series of novel dihydropyrimidin-2(1H)-ones derivatives is synthesized by using Rhizopus Oryzae lipase biocatalyst in deep eutectic solvent. The reaction is characterized by high efficiency and selectivity, short reaction time, mild and environmentally friendly reaction conditions. The yields are found to be significantly higher and reuse of both the lipase and deep eutectic solvent is possible up to four consecutive cycles. The products are found to exhibit appreciable in vitro antibacterial activity against Echerichia coli, Pseudomonas neumoniae and in vitro antifungal activity against Aspergillus niger and Candida albicans.

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