Triphenyltin Hydroxide Research Articles

Molecular docking of some Triphenyltin (IV) aminobenzoate compounds as potential antiviral agents

The triphenyltin (IV) hydroxide reaction by 2-, 3-, as well as 4-aminobenzoic acid was used to analyze the molecular docking of some triphenyltin (IV) aminobenzoate compounds in this research. These include; triphenyltin (IV) 2-aminobenzoate (2), triphenyltin (IV) 3-aminobenzoate (3) as well as triphenyltin (IV) 4-aminobenzoate (4) were well characterized by means of some spectroscopy techniques and microelemental analysis. The molecular docking was conducted on protein isolated from SARS-Cov-2 virus. The protein chosen was MPro and was docked toward the three compounds synthesized and compared with the commercial drug used for the treatment of virus, boceprevir. Based on the analysis of the energy binding calculation, the result revealed that the energy binding of the compounds 2-4 was -9.74; -9.97 and 10.42kcal/mol, respectively, while for boceprevir was -9.60kcal/mol. These results indicated that the three compounds were stronger as antivirus than the standard drug used, thus they are potentially used and developed as drugs in the treatment of virus SARS-Cov-2.

Synthesis and in vitro activity investigation of some dibutyl-, diphenyl- and triphenyltin(IV) carboxylates against leukemia cancer cell, L-1210

Abstract Successful synthesis of several dibutyl-, diphenyl- and triphenyltin(IV) carboxylate compounds and evaluation of their activity as anticancer against leukemia cancer cell, L-1210 was reported. The compounds were synthesized by reacting dibutyltin(IV) oxide (DBTO) (1), diphenyltin(IV) oxide (DPTO) (4) and triphenyltin(IV) hydroxide (TPTOH) (7) with respective carboxylic acids, and subsequently characterized using NMR, FTIR, and UV–Vis spectroscopies, microelemental analyzer, and melting point apparatus. The compounds were then tested as anticancer, revealing that derivatives of triphenyltin(IV) (compounds 8 dan 9) exhibit the IC50 value of 3.7 and 2.9 μg/mL, respectively, which are much higher activity than those of dibutyltin(IV) and diphenyltin(IV) derivatives.

Comparative Bioactivity Study of some Organotin (IV) 2-Chlorobenzoate compounds as Disinfectant agent

This research was carried out to study the bioactivitytest as disinfectant of two derivatives of organotin(IV) carboxylate compounds; diphenyltin(IV) di-2-chlorobenzoate (DPT2-CBz) (2) and triphenyltin(IV) 2-chlorobenzoate (TPT2-CBz) (4), against two pathogenic bacteria. Compounds 2 and 3 were successfully prepared by reactingdiphenyltin(IV) oxide (DPTO) (1) and triphenyltin(IV) hydroxide (TPTOH) (3) with 2-chlorobenzoic acid(2-HCBz)with yieldsof 87.71% and 88.73%, respectively. The characterization of the synthesized compounds was performed with several spectroscopy techniques such as UV, IR, 1HNMR, 13CNMR, and microelemental analyzer. The optical density (OD) test for both compounds measured using UV-Vis at 600 nm showeda goodbioactivity against two bacteria, Gram-negative Salmonella sp. and Gram-positive Staphylococcus aureus. The data revealed that compound 4 has bigger bioactivity than compound 2 and the positive control ofcommercial disinfectant (2.5% pine oil). The bioactivity of compound 4was optimum at concentration of 5x10-4 M and contact timeof 15 minutes.These data corresponding to the decrease of absorbance from 0.6640 to 0.0955 for Salmonella sp., and 0.6565 to 0.1295 for S. aureus, whereas although compound 2reached the optimum activityat the same concentration and contact time with compound 4, but the decrease of absorbance was less namely 0.6640 to 0.1305 for Salmonella sp., and 0.6565 to 0.196 for S. aureus. The decrease of absorbance in the measurement of OD implies that both compounds are potential to be used as disinfectant agent.

Synthesis, Characterization, and Comparison of Disinfectant Bioactivity Test of Two Triphenyltin(IV) Compounds

This paper aims to report the synthesis of two new organotin(IV) carboxylate derivatives, triphenyltin(IV) 4-aminobenzoate (2) and triphenyltin(IV) 4-nitrobenzoate (3) and to examine their antibacterial activity as a disinfectant. These compounds were prepared by reacting triphenyltin(IV) hydroxide (1) with 4-aminobenzoic acid and 4-nitrobenzoic acid, respectively. Compound (2) was obtained as a yellow solid with a yield of 84.09% and compound (3) in the form of a white solid with a yield of 80.70%. These compounds were well characterized using UV-Vis spectrometry, FT-IR spectrometry and NMR spectroscopy. The bioactivity test as a disinfectant was tested against Salmonella typhosa and Staphylococcus aureus. The activity test was carried out by measuring the optical density (OD) of the tested compounds with concentration variations of 5x10-3, 1x10-3, and 5x10-4 M in methanol and 5% dimethyl sulfoxide (DMSO), commercial Wipol (2.5% pine oil) was used as a positive control with observations monitored at contact times of 0, 5, 10, and 15 minutes. The results showed that of both compounds were active against the two bacteria compared to the positive control with compound 3 found to be more active than compound 2.

Thermogravimetric and Biological Studies of Organotin(IV) Complexes with 4-(Hydroxymethyl)piperidine-1-Carbodithioic Acid

Present studies were conducted to perform thermogravimetric characterization and biological activity investigations of organotin dithiocarbamates of general formulae R3SnL (R = n-Bu, 1; Ph, 2; Cy, 3), R2Sn(Cl)L (R = Me, 4; Ph, 5) and R2SnL2 (R = Me, 6) where L = 4-(hydroxymethyl)piperidine-1-carbodithioate. A novel procedure was also developed for the synthesis of product 2 by direct reflux of 4-(hydroxymethyl)piperidine-1-carbodithioic acid (HL) with triphenyltin(IV) hydroxide. HL was decomposed at low temperatures as compared to the metal complexes. The coordinated products were degraded leaving behind the tin or SnOCl inorganic residues. The products1-6 have shown excellent antimicrobial activities against the tested bacterial (Escherichia coli, Salmonella typhi, Staphylococcus aureus, and Bacillus subtilis) and fungal (Fusarium solani, Aspergillus niger, Alternaria solani, and Fusarium verticillioides) strains. The biological activities were found to depend upon the substitution pattern at the central tin atom.

Abstract 1297: Synthesis and structural analysis on an ionic diphenyltin complex as a potential anticancer agent

Abstract Triorganotins are popular among chemists due to their potential biological properties against bacteria, fungi, and cancer cell lines. However, they have limited applications due to their poor water solubility. We hypothesize that solubility can be improved when the complex exhibits partial ionic characteristics. Therefore, it is our research goal to synthesize triphenyltin complexes that possess ionic characteristics. Syntheses of the ionic triphenyltin complex involved the reaction of a diprotic carboxylic acid, with triphenyltin chloride in the presence of di-isopropylamine. However, a tin-carbon cleavage reaction was observed, as IR/NMR spectroscopy and X-ray Crystallography studies showed that an ionic diphenyltin complex was successfully obtained in the reaction. The ionic complex consists of a diphenyltin anionic moiety, two oxalate ligands are observed coordinating to the tin atom in the bidentate mode, and two diisopropylammonium as the counterions. The anionic diphenyltin moieties has a distorted octohedral geometry with two carbons and two oxygens atom occupying the equatorial positions and two oxygen atoms occupying the axial positions. The ionic complex is essentially a 1-D polymer chain through an extensive hydrogen-bonding network between the oxalate groups (OCO) and the N atom from the ammonium cations. Compared to the similar reaction with triphenyltin hydroxide, which resulted in ionic triphenyltin complexes, cleavage of one phenyl group was observed for the first time in the reaction with triphenyltin chloride. Future studies will be focused on the mechanistic studies on the Sn-C cleavage. Citation Format: Jade Witter, Xueqing Song, Tajera Henry, William Li. Synthesis and structural analysis on an ionic diphenyltin complex as a potential anticancer agent [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr 1297.

Assessing the Association of Mitochondrial Function and Inflammasome Activation in Murine Macrophages Exposed to Select Mitotoxic Tri-Organotin Compounds.

Background:Mitochondrial function is implicated as a target of environmental toxicants and found in disease or injury models, contributing to acute and chronic inflammation. One mechanism by which mitochondrial damage can propagate inflammation is via activation of the nucleotide-binding oligomerization domain (NOD)-like receptor (NLR) family, pyrin domain-containing receptor (NLRP)3 inflammasome, a protein complex that processes mature interleukin . plays an important role in the innate immune response and dysregulation is associated with autoinflammatory disorders.Objective:The objective was to evaluate whether mitochondrial toxicants recruit inflammasome activation and processing.Method:Murine macrophages (RAW 264.7) exposed to tri-organotins (triethyltin bromide (TETBr), trimethyltin hydroxide (TMTOH), triphenyltin hydroxide (TPTOH), bis(tributyltin)oxide) [Bis(TBT)Ox] were examined for pro-inflammatory cytokine induction. TMTOH and TETBr were examined in RAW 264.7 and bone marrow-derived macrophages for mitochondrial bioenergetics, reactive oxygen species (ROS) production, and inflammasome activation via visualization of aggregate formation, caspase-1 flow cytometry, enzyme-linked immunosorbent assay and Western blots, and microRNA (miRNA) and mRNA arrays.Results:TETBr and TMTOH induced inflammasome aggregate formation and release in lipopolysaccharide (LPS)-primed macrophages. Mitochondrial bioenergetics and mitochondrial ROS were suppressed. Il1a and Il1b induction with LPS or challenge was diminished. Differential miRNA and mRNA profiles were observed. Lower miR-151-3p targeted cyclic adenosine monophosphate (cAMP)-mediated and AMP-activated protein kinase signaling pathways; higher miR-6909-5p, miR-7044-5p, and miR-7686-5p targeted Wnt beta-catenin signaling, retinoic acid receptor activation, apoptosis, signal transducer and activator of transcription 3, IL-22, IL-12, and IL-10 signaling. Functional enrichment analysis identified apoptosis and cell survival canonical pathways.Conclusion:Select mitotoxic tri-organotins disrupted murine macrophage transcriptional response to LPS, yet triggered inflammasome activation. The differential response pattern suggested unique functional changes in the inflammatory response that may translate to suppressed host defense or prolong inflammation. We posit a framework to examine immune cell effects of environmental mitotoxic compounds for adverse health outcomes. https://doi.org/10.1289/EHP8314

Synthesis, characterization and the antifungal activity test of some organotin(IV) benzoates

In continuing search on the biological activity of the organotin compounds we are working with, We here reported the synthesis and the antifungal activity test of three organotin(IV) complexes of dibutyltin(IV) dibenzoate (3), diphenyltin(IV) dibenzoate (6) and triphenyltin(IV) benzoate (9). These three compounds were prepared by the reaction of dibutyltin(IV) dichloride (1), diphenyltin(IV) dichloride (4), and triphenyltin(IV) chloride (7) via dibutyltin(IV) oxide (2), diphenyltin(IV) oxide (5), and triphenyltin(IV) hydroxide (8) with benzoic acid. The product obtained in each step was characterized by UV, IR and NMR spectroscopies and also microelemental analysis. The antifungal activity test was carried out against Fusarium oxysporum strain. The results showed that the inhibition zone shown by these organotin(IV) benzoate were found by far much more active compared to the free benzoic acid, the starting materials 1, 4, 7, and the intermediate products, 2, 5 and 8. The inhibition zone of each of the compounds tested was compared with the control where the fungus alone was grown in the media. The results showed that triphenyltin(IV) benzoate (9) was the most active compound against the fungus and the minimum inhibitory concentration obtained was about 0.7 mM.

In Vitro Antimicrobial Activity Study of Some Organotin(IV) Chlorobenzoates against Staphylococcus aureus and Escherichia coli ‎

In vitro antibacterial activity of some organotin(IV) chlorobenzoates including diphenyltin(IV) o-, m-, p-dichlorobenzoate (2, 3, 4) and triphenyltin(IV) o-, m-, p-chlorobenzoate (6, 7, 8) against Staphylococcus aureus and Escherichia coli was studied. The compounds were synthesized by the reaction of diphenyltin(IV) dihydroxide (1) and triphenyltin(IV) hydroxide (5) with o-, m-, p-chlorobenzoic acid in a maximum refluxed time of 4 h using methanol as the solvent of the reaction. The antibacteri

Synthesis and antimalarial activity of some triphenyltin(IV) aminobenzoate compounds against Plasmodium falciparum

Abstract This paper presents antimalarial activity of several triphenyltin(IV) aminobenzoate compounds synthesized from the reaction of triphenyltin(IV) hydroxide with 2-, 3-, and 4-aminobenzoic acid. The activity of the compounds as anti-malaria agents was evaluated using Plasmodium falciparum, and demonstrated that the compounds have about the same IC50 with that of chloroquine (2×10−3 μg/mL) applied as the positive control. The result also showed that the Plasmodium is non-resistent to the compounds synthesized, which is the opposite to chloroquine.

Structure and surface analysis of ibuprofen-organotin conjugate: Potential anti-cancer drug candidacy of the compound is proven by in-vitro DNA binding and cytotoxicity studies

An ibuprofen-organotin conjugate (TPTDI) was synthesized by reacting ibuprofen with triphenyltin hydroxide (fentin hydroxide) in dry ethanol under acidic conditions. Characterization data of the compound, obtained by spectroscopic techniques (FTIR, 1H NMR and 13C NMR), elemental analysis and its X-ray single crystal were found to corroborate the stoichiometry and structure of the title organotin (IV) ester. A detailed Hirshfeld surface analysis for the elucidation of possible intermolecular interactions indicated that the most important contributions to the crystal packing were from H…H (66.7%), H…C/C…H (27.9%) and H…O/O…H (5.3%) interactions. Hydrogen-bonding and van der Waals interactions were the dominant interactions in the crystal packing. TPTDI – DNA binding studies were done by DFT, molecular docking, UV–visible and fluorescence spectroscopies, cyclic voltammetry (CV) and by viscosity measurements at neutral pH (7.0) and at 37 °C. Theoretical and experimental investigations were found compatible and revealed significant reactivity of TPTDI with DNA via mixed mode of interaction. Binding parameters (ΔG, Kb and n) confirmed the reaction spontaneity and intercalation as prominent mode along with groove binding. In-vitro Huh-7 cancer cell line activity suggested TPTDI to be a potential anti-cancer drug candidate. Molecular, chemical and biological findings showed good correlations.

Structure and Surface Analysis of Ibuprofen-Organotin Conjugate: Potential Anti-Cancer Drug Candidacy of the Compound is Proven by In-Vitro DNA Binding and Cytotoxicity Studies

An ibuprofen-organotin conjugate (TPTDI) was synthesized by reacting ibuprofen with triphenyltin hydroxide (fentin hydroxide) in dry ethanol under acidic conditions. Characterization data of the compound, obtained by spectroscopic techniques (FTIR, 1 H-NMR and 13 C-NMR), elemental analysis and its X-ray single crystal were found to corroborate the stoichiometry and structure of the title organotin (IV) ester. A detailed Hirshfeld surface analysis for the elucidation of possible intermolecular interactions indicated that the most important contributions to the crystal packing were from H…H (66.7%), H…C/C…H (27.9%) and H…O/O…H (5.3%) interactions. Hydrogen-bonding and van der Waals interactions were the dominant interactions in the crystal packing. TPTDI – DNA binding studies were done by DFT, molecular docking, UV-visible and fluorescence spectroscopies, cyclic voltammetry (CV) and by viscosity measurements at neutral pH (7.0) and at 37 o C. Theoretical and experimental investigations were found compatible and revealed significant reactivity of TPTDI with DNA via mixed mode of interaction. Binding parameters (∆G, K b and n) confirmed the reaction spontaneity and intercalation as prominent mode along with groove binding. In-vitro Huh-7 cancer cell line activity suggested TPTDI to be a potential anti-cancer drug candidate. Molecular, chemical and biological findings showed good correlations.

Synthesis and structural determination of ionic triphenyltin complexes of mercaptoacetic and 3-mercaptopropionic acids

Two ionic triphenyltin complexes were obtained when two thiocarboxylic acids, mercaptoacetic acid and 3-mercaptopropionic acid, were mixed with triphenyltin hydroxide in the presence of dicylcohexylamine. Their structures have been characterized by IR and multi-nuclear (1H, 13C{1H} and 119Sn{1H}) NMR spectroscopies. Coordination difference was observed between triphenyltin complexes of mercaptoacetate and 3-mercaptopropionate. The coordination assignments of the tin atoms in the two triphenyltin complexes are confirmed by X-ray crystallographic studies. In the solid state, the bidentate binding mode of mercaptoacetate ligand gives a five-coordinate ionic triphenyltin complex with a cis-trigonal-bipyramid (TBP) geometry around tin, while the tin in dicyclohexylammonium 3-mercaptopropionatotriphenylstannate was found to be four-coordinate with tetrahedral geometry around tin, as the 3-mercaptopropionate is monodentate via sulfur. Important hydrogen bonding between dicyclohexylammonium and carboxylate have been observed for both complexes.

Synthesis, structural characterization, Hirshfeld surface analysis and in vitro-antimicrobial activities of triphenyltin (IV) compounds of azo-carboxylates derived from 2- or 4-amino benzoic acids and naphthalen-1 or 2-ol

Synthesis of three new triphenyltin(IV) compounds 1–3 were reported by the reaction of azo-carboxylic acid ligands viz.2/4-(2-hydroxynaphthylazo)-benzoic acids [compounds 1 and 2] or 2-(4-hydroxynaphthylazo)-benzoic acid [compound 3] with triphenyltin(IV) hydroxide. The compounds were completely characterized with the help of elemental analysis, IR and multinuclear [1H, 13C and 119Sn]-NMR spectroscopy. The mode of coordination and geometry around tin atoms in compounds 1 and 3 were determined by X-ray crystallography. Compounds 1 and 3 exhibited monomeric structure with intermediate deformation between the trigonal bipyramidal and square-pyramidal geometry or distorted tetrahedral geometry around tin atom respectively. Hirshfeld surface analysis for both structures was also performed. The main difference between 1 and 3 is observed for stacking interactions. 119Sn NMR spectral study of all the compounds suggested that the compounds adopted 4-coordinated tetrahedral structures in solution. The antimicrobial activities of the compounds showed effective antibacterial activity against S. aureus and antifungal activity against F. oxysporum. The antimicrobial activity of these compounds was found to be higher than the tested standard compounds against some selected microbes.

Antimalarial Activity of Some Organotin(IV) Chlorobenzoate Compounds against Plasmodium falciparum

This paper reported the comparative study on antimalarial activity of some organotin(IV) derivatives with some chlorobenzoic acid derivatives used as the ligands. The compounds were synthesized by reacting the intermediate products of dibutyltin(IV) oxide, diphenyltin(IV) dihydroxide and triphenyltin(IV) hydroxide, with chlorobenzoic acid. The antimalarial activity was performed against Plasmodium falciparum. The results showed that the IC50 of the compounds tested were about the same with the chloroquine (2 x 10-3 µg/mL) used as the positive control, but unlike chloroquine which has been known to have resistance as antimalarial, these organotin(IV) compounds prepared are not resistant to the Plasmodium. The result also showed that the derivative of triphenyltin(IV) has higher IC50respective to others.

Cephradine-Capped Gold Nanoparticle Modified Glassy Carbon Electrode for Trace Level Sensing of Triphenyltin Hydroxide

Synthesis of highly stable gold nanoparticles (AuNps) was accomplished using cephradine (Cep) drug as the capping molecule and sodium borohydride as the reducing agent. Characterization studies such as ultraviolet-visible (UV–vis) spectroscopy confirmed the formation of AuNps while fourier transform infra-red (FT-IR) spectroscopy showed the interaction of AuNps with Cep. The size and shape of Cep-AuNps were investigated using atomic force microscopy (AFM) while their crystallinity was determined through X-ray diffractometry (XRD). The synthesized Cep-AuNps, after getting deposited on a glassy carbon electrode (GCE), proved as a highly responsive sensor for low-level detection of triphenyltin hydroxide (TPTH) using cyclic voltammetry (CV) as the determining mode in stirred solution. The developed sensor linearly responded to TPTH in the range of 1–80 nM with a lower detection limit (LDL) of 0.12 nM and R2 value of 0.9948 under optimized conditions. Importantly, the sensor was highly stable and reproducible, showing a relative standard deviation (RSD) value of 1.1% based on 15 replicative runs and proved to be extremely selective for TPTH with negligible interference in the presence of expected interfering species. The developed sensor was effectively utilized for monitoring TPTH in natural water samples.

The Potency Study of Organotin(IV) 3-Nitrobenzoate Compounds as Antimalarial Agents

This paper reports the potency study of organotin(IV) 3-nitrobenzoate as antimalarial agent. The organotin(IV) 3-nitrobenzoate compounds were synthesized by reacting the intermediate products dibutyltin(IV) oxide, diphenyltin(IV) dihydroxide and triphenyltin(IV) hydroxide, with 3-nitrobenzoic acid. The antimalarial activity study was performed against Plasmodium falcifarum and the result of IC50 of the three compounds tested, i.e. dibutyltin(IV) di-3-nitrobenzoate, diphenyltinIV) di-3-nitrobenzoate and triphenyltin(IV) 3-nitrobenzoate were 8.1 x 10−3, 5.2 x 10−2 and 7.2 x 10−3 µg/mL, respectively, while the the chloroquine gave IC50 2 x 10−3 µg/mL). The IC50 of the compounds tested were little bit higher than the positive control, however these organotin(IV) compounds synthesized are not resistent to Plasmodium, thus the possible development as antimalarial agent is widely opened.

Fungicide Sensitivity Monitoring of Alternaria spp. Causing Leaf Spot of Sugarbeet (Beta vulgaris) in the Upper Great Lakes.

Alternaria leaf spot (ALS), caused by Alternaria spp., can occur wherever sugarbeet is grown. Infection by Alternaria spp. and disease management has historically been considered a minor issue in sugarbeet production in the United States. An increase of both incidence and severity in 2016 of ALS high enough to cause yield loss has been observed in Michigan. With a renewed need to consider potential management of this disease, the sensitivity was determined for populations of Alternaria spp. to three classes of fungicides currently labeled for management of leaf spot on sugarbeet, including demethylase inhibitor (DMI), quinone outside inhibitor (QoI), and organo-tin fungicides. Leaves with symptoms of ALS were sampled from sugarbeet fields in east-central Michigan and southwestern Ontario, Canada. Monoconidial isolates were obtained to determine sensitivity to each fungicide class above. A spiral gradient dilution method was used to estimate the fungicide effective concentration (in milligrams per liter) that caused a 50% inhibition of fungal growth in vitro for all isolates. Significant temporal shifts were detected in the frequencies of sensitivity phenotypes to DMI and QoI but not organo-tin fungicides from 2016 through 2017. Individual isolates of Alternaria spp. were recovered with cross-resistance to DMI and multiple resistance to DMI, QoI, and triphenyltin hydroxide fungicides. To our knowledge, this is the first report of a fungus other than Cercospora beticola with resistance to organo-tin fungicides. Fungicide sensitivity monitoring indicates that an effective integrated disease management approach combining fungicide efficacy trials and monitoring pathogen biology is essential for developing effective resistance management recommendations.

Simultaneous determination of three organotin pesticides in fruits and vegetables by high‐performance liquid chromatography/tandem mass spectrometry

The presence of organotins in the environment affects food safety, making it important to monitor the levels of organotin pesticides (OTPs) in fruit and vegetable samples. In the present study, a simple and low cost method for simultaneous determination of three OTPs (azocyclotin, fenbutatin oxide and triphenyltin hydroxide) in vegetable and fruit samples was developed and validated, based on solid-phase extraction and liquid chromatography/tandem mass spectrometry. Extraction with acetonitrile containing 0.2% formic acid positively affected the recoveries of the three OTPs. Moreover, the simultaneous purification of the three OTPs was the most efficient using mixed-mode cation-exchange cartridges and 5.0% ammonium hydroxide in methanol as eluent, and, in this case, mild matrix effects (-9.3% to 21.6%) were obtained for the three OTPs monitored. The developed method reached limits of quantification of 1 μg kg-1 , and linearity was satisfactory, with correlation coefficients >0.995. A fortification study showed that when spiked at 1.0-50.0 μg kg-1 the mean trueness values were from 72.3 to 110.0% in all matrices (three vegetables and three fruits). The intra-day precision was <14.1%, and the inter-day precision (n = 11) was <18.2%. The proposed method was successfully applied to the simultaneous analysis of three OTPs in vegetables and fruits.

In vitro antimalarial activity of some organotin(IV)2-nitrobenzoate compounds against Plasmodium falciparum

Antimalarial activity study of organotin(IV) derivatives with nitrobenzoic acid derivatives used as ligands has been performed. The targeted compounds were prepared from their organotin(IV) chlorides via dibutyltin(IV) oxide, diphenyltin(IV) dihydroxide, and triphenyltin(IV) hydroxide intermediate products, followed by reacting the intermediate products with 2-nitrobenzoic acid. The antimalarial activity was performed against P. falciparum. The results showed that the IC50values of dibutyiltin(IV) di-2-nitrobenzoate, diphenyltin(IV) di-2-nitrobenzoate, and triphenyltin(IV) 2-nitrobenzoate were in 8.4 × 10‑3, 5.3 × 10–2, and 9.1 × 10–3 µg/ml, respectively. The IC50 values were slightly higher than the value for chloroquine (2 × 10–3 µg/ml) used as the positive control; however, one advantage is that all prepared organotin(IV) compounds were not resistant to Plasmodium, making the use of organotin(IV) as an antimalarial is possible. The results indicated that the derivative of triphenyltin(IV) was more potent when used as an antimalarial, as expected, and has potential to be developed as an antimalarial drug in the future.