European Journal of Chemistry

Reactivity comparison by 1,3-dipolar cycloaddition of the three dipolarophiles (-)-R-Carvone (I), (-)-R-Linalool (II) and derivative of (-)-(1S,4S)-camphor (III) has been studied. By reactions of p-chlorophenylnitrile oxide, new heterocycles are obtained by stereospecific reactions for cyclic Terpenoids I and III (regardless of the length of the side chain). However the aliphatic dipolarophile II gives two diastereoisomers. Terpenoids (-)-R-Carvone I (-)-R-Linalool II and (-)-(1S,4S)-Camphor 1 are isolated respectively from Moroccan species Mentha viridis (L.), Lavandula officinalis (L.) and Artemisia herba halba (Asso). The new heterocycles obtained were identified by combination of chromatographic and spectroscopic methods.

An organic-inorganic hybrid compound of tetraethylammonium dihydrogenarsenate bis-arsenic acid salts of formula [(CH₃CH₂)₄N].[H₂AsO₄].[H₃AsO₄]₂(TEAs) were grown by the slow evaporation and characterized by means of single crystal X-ray diffraction, thermal analysis, FT-IR and Raman spectroscopy. This compound crystallize in the space groups Cc with unit cell parameters, a= 20.105(2) Å; b= 7.342(4) Å, c = 15.292(2) Å, γ = 115(4)°, Z = 4, R= 0.07. The structure has solved using direct methods and refined by least-squares analysis. In this case, the structure consists of infinite parallel two-dimensional planes built of mutually H₂AsO₄⁻, H₃AsO₄ tetrahedra connected by strong O-H···O hydrogen bonding. The thermoanalytical properties were studied using TG of TEAs method in the temperature ranges from 300 to 440 K for this hygroscopic sample. DSC measurement was carried out in the temperature range from 305 to 425 K.

A new compound, N'-[(E)-furan-2-ylmethylidene]furan-2-carbohydrazide was synthesized. Elemental analysis, IR spectrum, ¹H NMR and X-ray crystal structure studies were carried out to determine the compositions and molecular structure of the compound. It crystallizes in the orthorhombic space group Pbca with unit cell parameters a = 11.3142(4) Å, b = 7.5526(2) Å and c = 22.9030(9) Å. The crystal structure studies reveal intermolecular N-H···O hydrogen bonding interactions in the solid state.

New thieno[3,2-d][1,3]thiazine nucleosides derivatives were synthesized and structures of the new compounds were confirmed on the basis of elemental and spectral data. Some of the synthesized compounds were screened for antibacterial and antifungal activity.

The aim of the present study is to find a non time consuming, economical and reliable spectrophotometric procedures using commercially available spectrophotometric reagents for the determination of Fe(III) ions. The methods are based on the formation of colored ternary complexes using, 1,10-phenanthroline and eriochrome black T or tartrazine mixed reagents and improved using a cationic surfactant, cetyltrimethyl ammonium bromide. This surfactant interacts with the complex to build up true ternary complex. The most suitable conditions for determination of Fe(III) ions and the parameters affecting the reactions including pH, time, temperature, stoichiometric ratios and reagents concentrations are optimized. The effect of different interfering ions is studied together with the suitable masking agents. The developed methods are used for the determination of Fe(III) ions in the presence of cetyltrimethyl ammonium bromide in different types of water (polluted industrial waste, ground, river Nile and drinking water). The synthesis and spectroscopy studies of two Fe complexes were reported. Thermal analysis was carried out in order to give an idea about the thermal stability of the complexes.

Two metal complexes of Ti(IV) were synthesized with newly prepared biologically active ligands. These ligands and their functional groups were carefully designed and selected from well known anticancer drugs. The ligands were prepared by the condensation of a mixture of sulfamethoxazole and the appropriate aldehyde namely, 3,4-dimethoxybenzaldehyde and 3,4,5-trimethoxybenzaldehyde. The structure of the ligands and their complexes were confirmed by spectroscopic data i.e. IR, ¹H NMR,electronic and elemental analysis. All compounds were screened for their in vitro anticancer potential using HELA and PC3 cells. All compounds showed limited cytotoxicity and complete cleavage of calf thymus deoxyribonucleic acid (CT-DNA).

New Pd(II) and Pt(IV) binuclear complexes with two heterocyclic Schiff base ligands of type ONO derived from condensation of salicylaldehyde with 4-aminoantipyrine have been synthesized and characterized using elemental analysis, IR, electronic absorption spectra, magnetic moments. It has been found that the stoichiometric ratio is metal:ligand (2:2) with Pd(II) or Pt(IV) ions forming binuclear complexes. The electrochemistry of the Pt complexes for Pt(IV)/Pt(II) redox couple was investigated by cyclic voltammetry. According to molar conductance, the complexes may be formulated as [Pd₂(L1)₂], [Pt₂(L1)₂(H₂O)₄]Cl₂, [Pd₂(L2)₂]Cl, and [Pt₂(L2)₂(H₂O)₄]Cl₃. On the basis of the magnetic moments, square planar geometry is suggested for Pd(II) complexes and octahedral geometry is suggested for Pt(IV) complexes. The antibacterial activity of the ligands and complexes were assessed against Gram‐positive bacteria B. subtilis and S. aureus and Gram‐negative bacteria S. typhi and Salmonella spp.

The aim of this study was to examine the possibility of replacing a part of the filler in experimental dental composites by nanoparticles with antibacterial potential. Experimental dental composites containing silver nanoparticles deposited on titanium and silica dioxide of different size were analyzed in terms of antibacterial properties. The depth of cure and mechanical properties of composite surface layer were examined. Bactericidal properties were tested according to the LIVE/DEAD cell viability assay. The mechanical properties were determined with a NanoTest 600 instrument. Composites containing silver nanoparticles deposited on titanium dioxide and nanosilica carrier exhibit the strongest antibacterial properties. High content of TiO₂ causes strong absorption of light irradiation, which makes their curing process more difficult. Hardness of surface layer increases but the deeper layers of the samples remain uncured. Composites containing nanosilver on titanium dioxide and nanosilica carrier exhibit the highest antibacterial activity. High content of TiO₂ causes strong absorption of light irradiation impairing their curing process. The presence of nanosilver changes composite color causing limited light penetration and lower surface hardness.

The new tetralone acids (7a-e) were synthesized as analogues of podophyllotoxin. They were prepared by replacing 3,4,5-trimethoxyphenyl ring with cyclohexyl group in podophyllotoxin and 1,3-methylene dioxy ring with methoxy, hydrogen, methyl, thiomethyl, and fluorine atoms. The analogues of podophyllotoxin were synthesized using Gensler’s method with some changes in reagents and experimental procedure. The structures of the synthesized compounds were confirmed by IR, ¹H NMR, ¹³C NMR, mass spectra and elemental analysis data. The synthesized tetralones acids were screened for their antimitotic activity. It is noteworthy that compound 7b possessed excellent antimitotic activity, 7c and 7e showed considerable activity and remaining 7a and 7d possessed low activity.

Recently, there has been more interest with antidiabetic agents commencing natural products from plants as a better treatment than currently used synthetic drugs. The high performance liquid chromatography analysis of methanolic Acalypha wilkesiana leaves extract revealed occurrence of twenty one polyphenolic compounds. Catechin is the main constituent (29.91%), followed by apigenin (20.96%), then, ellagic acid, quercetin, kampferol, ferulic acid, luteolin, pyrogallol, rutin, caffeic acid, chlorogenic acid, protocatechouic acid, p-coumaric acid, caffiene, syrigic acid, catechol and p-OH-benzoic acid in percentages of 17.54, 10.45, 7.63, 4.67, 4.61, 4.30, 3.21, 3.15, 2.10, 1.48, 1.43, 1.13, 1.09, 1.08 and 1.05%, respectively. The antidiabetic and heamatological effects of methanolic Acalypha wilkesiana leaves extract (10, 20 and 40 mg/100 g body weight) in streptozotocin diabetic rats were investigated comparing with metformin HCl (50 mg/100 g body weight) for 30 days. Our results indicated that the most effective dose of methanolic Acalypha wilkesiana leaves extract was 40 mg/100 g body weight, which decreased blood glucose level to about 77.37% in diabetic rats, compared with a percentage of 76.50% achieved by administration with metformin HCl. Furthermore, liver functions activity, kidney functions, lipid profile, atherogenic indices and haematological parameters were scrutinized in diabetic rats treated with methanolic Acalypha wilkesiana leaves extract. These results indicate that the methanolic leaves extract of Acalypha wilkesiana, have favorable effects in bringing down the severity of diabetes and justify its use in traditional medicine for the treatment of diabetes and its complications.

A micellar liquid chromatographic method was developed for determination of tinidazole in bulk, dosage forms and human plasma using intersil cyano column and a mobile phase of 0.1 M sodium dodecyl sulphate, 20% 1-propanol, 0.3% triethylamine in 0.02 M orthophosphoric acid:water (60:40, v:v) (pH = 4). The U.V. detection was achieved at 311 nm. Various chromatographic parameters were investigated to select the optimum conditions for the separation, e.g. types of columns, pH of mobile phase, concentration of sodium dodecyl sulphate, 1-propanol, triethylamine, etc. The method was linear over the concentration range 40-200 µg/mL with regression coefficient 0.999. The result obtained by the proposed method was compared with that obtained by the reference HPLC technique. Furthermore, the proposed method was successfully applied as stability-indicating method for determination of tinidazole under different stressed conditions. The method showed good selectivity, repeatability, linearity and sensitivity according to the evaluation of the validation parameters.

Sorption of uranium from 6 M free H₂SO₄ on two anionic sorbents containing different complexing groups, the synthetic Organosilicate compound (OSC) and the Amberlite IRA 402, were investigated. The sorption mechanisms of uranium on both sorbents were also studied. Experimental data indicated that the uranium sorption on either Amberlite IRA 402 or OSC is a function in pH, depending strongly on the aqueous uranyl species. Both sorbents reached a maximum at slightly acidic (pH = ~1) when uranium is exist in the form of negatively charged sulfate complexes. These sorption values were attributed to the ion exchange process between UO₂⁺² species and interlayer anions on Amberlite IRA 402 and OSC in acidic solutions. Uranium sorbed on OSC through formation of ML₃ complex and ML₂ for Amberlite IRA 402. Also it was found that the uranium sorption capacity was 20 and 80 mg/g for Amberlite IRA 402 and OSC, respectively, and its elution were effective even with 5 mL of 1 mol/L KNO₃.

Some new dimethine and bis-dimethine, cyanine dyes derived from benzo[2,3-b; 2`,3`-b`]bis-pyrazolo[4,5-b]-l,4-(oxa-, thia-, and pyra-)-zine-6,12-dione were synthesized. Effect of chemical structure on the electronic visible absorption spectra of all the synthesized cyanine dyes was investigated in 95% ethanol solution. Effects of solvent and/or solution pH on the electronic visible absorption spectra of some selected synthesized cyanine dyes were also examined in pure solvents having different polarities and/or in aqueous universal buffer solutions, respectively. Structural confirmations were carried out through elemental analysis, mass spectroscopy, IR and ¹H NMR spectra.

2-Amino-4-phenyl-4,5-dihydro-5-oxopyrano[2,3-c]chromen-3-carbonitrile derivatives (8a-d) have been isolated in good yields by the reaction of corresponding 4-hydroxycoumarin (1) with substituted aldehydes (2a-d) and malononitrile (3) under reflux conditions. The reactivity of α-functionalized iminoethers (9a-d) with hydrazine, hydroxylamine and piperidine was studied. The synthesized compounds were characterized by various techniques including spectroscopy. Compounds 8-11 were also evaluated as potential acetylcholinesterase inhibitors.

The motivation of the synthetic process of new heterocyclic cyanine dyes is to improve the specific characterization, photosensitization behavior, and probable application in the field of biology, medical science and physics. New heterocyclic compounds having oxonium nuclei were prepared and employed for the synthesis of some new photosensitizers cyanine dyes (monomethine, trimethine and styryl cyanines). The electronic visible absorption spectra of all the synthesized cyanines were investigated in 95% ethanol to attempt and throw some light on the influence of such new heterocyclic nuclei and to compare or evaluate spectral behaviors. Antimicrobial activity of selected compounds against some bacterial strains was tested. Structural identification was carried out via elemental analysis, IR and ¹H NMR.

A reversed phase high performance liquid chromatographic method for the determination of process related impurities in pioglitazone hydrochloride was developed and validated. High-quality separation was achieved on a Luna C18 column (150 mm × 4.6 mm, 3 µm) using gradient elution at a flow rate of 1 mL/min and a column temperature of 45 °C. UV detection was performed at 254 nm. The validation was performed according to the International Conference on Harmonization (ICH) guidelines. In addition, the solution stability and method robustness were examined. The method gives satisfactory separation of impurities of pioglitazone hydrochloride and so it is suitable for quantification of the process related impurities as well as for the assay of the active compound.

A simple and regioselective synthesis of 2-chloro-3-formyl-1,8-naphthyridine, through Vilsmeier-Haack cyclization of N-(pyridin-2-yl)acetamide has been reported. The reaction of 2-chloro-3-formyl-1,8-naphthyridine is also investigated and new series of 1,8-naphthyridine derivatives such as 3-chloro-4-(2-chloro-1,8-naphthyridine-3-yl)-1-(phenylamino)azetidin-2-one, 3-chloro-4-(2-chloro-1,8-naphthyridin-3yl)-1-((4-nitrophenyl) amino)-azetidin-2-one and 3-chloro-4-(2-chloro-1,8-naphthyridine-3-yl)-1-((2,4-dinitrophenyl) amino)-azetidin-2-one have been prepared. The formyl group in the 1,8-naphthyridine is subjected to further transformation into alkoxy carbonyl (NIS-K₂CO₃/alcohol) to afford 3-alkoxy carbonyl-1,8-naphthyridine and new hetero cyclic compounds such as oxadiazolo, thiadiazolo-thion and triazolo-thion have been prepared. The reaction between 2-chloro-3-formyl-1,8-naphthyridine and sodium sulphide in DMF produced 2-mercapto-3-formyl-1,8-naphthyridine. Some of the prepared compounds were found to have good biological activity against Staphylococcus aureus and Staphylococcus epidermidis.

Several new substituted sulfonamides and sulfinyl compound derivatives were obtained by the reaction of 2-thioxo-1,2,4-triazolo[1,5-a]pyridine and pyrimidine thiol derivatives with (2-chloromethyl)benzimidazole and/or (2-chloromethyl)benzooxazole. Structures of the newly synthesized products have been deduced on the basis of spectral and analytical data. The synthesized compounds were screened for their antimicrobial activity.

New series of arylthiadiazole hydrazinecarboxamides (5a-e) have been synthesized by hydrazinolysis of carbamates (4a-e) and spectrally characterized. The new candidates have been screened for their anticonvulsant and immunomodulatory activities. Compound 5e was the most potent anticonvulsant candidate as it showed 100% protection against both maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) screens without neurotoxicity at 100 mg/kg (0.318 mmol/kg). With respect to immunomodulation, compounds 5a and 5d revealed immunostimulatory activity while compounds 5b, 5c, and 5e had immunosuppressive responses based on ELISA detection of IgM and IgG levels, counting the total mesenteric lymph nodes lymphocytes, and histo-pathological examinations.

A comparative and stability-indicating reversed phase high performance liquid chromatographic study have been developed and validated for sitagliptin phosphate. The liquid chromatographic determination was achieved isocratically on Poroshell 120 EC-C18 (100 × 4.6 mm, i.d.; particle size, 2.7 µm), Pursuit 5PFP (150 × 4.6 mm, i.d.; particle size, 5 µm) and Chromolith performance RP-18e (100 × 4.6 mm, i.d.; macropore diameter, 2 µm) columns using a mobile phase consisting of methanol:water:triethylamine:acetic acid (60:40:0.1:0.1; v:v:v:v), at a flow rate 0.5 mL/min and UV detection at 268 nm. The method was linear over the concentration range of 100-1000 µg/mL (r = 0.9998) with a limit of detection and quantitation of 10 and 30 µg/mL, respectively. All the validation parameters and stability indicating study were studied on Poroshell 120 EC-C18 column, which achieved the best separation. The proposed method has been found to have the required accuracy, selectivity, sensitivity, and precision to assay sitagliptin phosphate in bulk form and in a pharmaceutical dosage form. Degradation products resulting from the stress studies did not interfere with the detection of sitagliptin phosphate that indicates that the assay are stability-indicating assay.

The phytochemical investigation of the ethanolic extract of the aerial parts of Melilotus indicus resulted in the isolation of eight known flavonoids, namely; catechin (1), epicatechin (2), taxifolin (3), quercetin (4), quercetin 3-O-β-D-glucopyranoside (5), and quercetin 3-O-α-L-rhamnopyranoside (6), isorhamnetin 3-O-β-D-glucopyranoside (7) and isorhamnetin 3-O-β-D-rutinoside (8). These compounds have never been isolated from this species. The cytotoxic activities of the extracts of Melilotus indicus was evaluated by MTT assay against six cancer cell lines using doxorubicin as standard drug. The chloroform extract was the most potent cytotoxic agent against HepG-2cells with an IC₅₀: 9.21 µg/mL.

The non-isothermal kinetic parameters corresponding to the thermal decomposition of carisoprodol under nitrogen atmosphere was investigated at four different heating rates 5, 10, 15 and 20 °C/min. The activation energy was determined using three linear isoconversional methods, Friedman, Flynn-Wall-Ozawa and Kissinger-Akahira-Sunose. Results showed good agreement with each other. Invariant kinetic parameters (IKP) method was applied in the conversion range of 0.2 ≤ α ≤ 0.8 for the determination of the kinetic triplet. E_inv= 95.81 kJ/mol, A_inv = 2.275×10⁷ 1/min and the decomposition mechanism corresponds to nucleation and growth, following the Avrami-Erofeev model, A1.5, as the kinetic model. The Perez-Maqueda et al. criterion associated with the independence of activation parameters on the heating rate (by means of Coats-Redfern and Flynn-Wall equation) confirmed the model.

The class of compounds having diphenylmethane framework occupy a distinct place in natural bioactive compounds and also serve as useful intermediates in various commercially important synthetic molecules. Conventionally, Friedel-Craft type reactions were used to synthesize such diphenylmethane derivatives. However, herein we report a unique approach in which, two benzyl alcohol molecules were coupled in the presence of different halogenating agents (SOCl₂, PBr₃ and MeSO₂Cl) to afford the desired diphenylmethane derivative, bis(2,4-bis(benzyloxy)-5-methoxyphenyl)methane. It has been found that the coupling reaction is strongly influenced by the electronic effects and number of the substituents on the phenyl ring. The resultant compound, bis(2,4-bis(benzyloxy)-5-methoxyphenyl)methane, was obtained in excellent yield (83-85%) and completely characterize with different spectroscopic techniques.

Synthesis of ethyl 6-(8-hydroxyquinolin-5-yl)-3-methylpyridazin-4-carboxylate (4) via one-pot three component reaction of ethyl acetoacetate with (8-hydroxyquinolin-5-yl)(oxo) acetaldehyde (2) in the presence of hydrazine hydrate at room temperature in water was described. A new series of heterocyclic moieties such as oxadiazoles, triazoles, pyrazoles and Schiff bases were prepared and characterized. The structures of the newly synthesized compounds were established by elemental and spectral data. The antimicrobial activity of some of the synthesized compounds was examined against two Gram‐positive bacteria, two Gram‐negative bacteria and four fungi. The results showed that the tested compounds exhibited significant to moderate antimicrobial.

Lead poisoning occurs when lead builds up in the body, regularly over a period of months or years. Insignificant amounts of lead can cause serious health complications. The main objective of this study is to determine the effect of gases rising from electric generators and the lead-induced oxidative stress and adversarial health properties by biochemical markers in Iraqi workers employed on the operation of diesel generators mainly increased lead poisoning symptoms. Serum lead, advanced oxidation protein products (AOPP), total antioxidant activity (TAA), malondialdehyde (MDA), and other biochemical parameters were analysed in fifty workers in a large private electrical generator. The results of the study showed a significant elevation in lead, AOPP and MDA activities in Iraqi workers employed on the operation of diesel generators in association to healthy control samples. The results showed that elevated serum lead has a significant correlation with oxidative stress, and biochemical markers that may be help to detect impairment in the body function in lead exposed workers.

IL-8 is a member of the CXC class of chemokines and is chemotactic for neutrophils. The cellular activation of IL-8 takes place after IL-8 binding to its receptor in the presence of calcium and protein kinase, leading to neutrophil activation and chemo taxis in infection and inflammation. Therefore, IL-8 tasks to mediate neutrophil recruitment, accumulation, and activation. The study included 50 patients with diabetes mellitus divided into a female group, which contained 16 female patients with an age range of 39-69 years, and a male group which contained 34 male patients with an age range of 40-72 years. Control groups contained forty healthy individuals divided into a female group, which contained 16 healthy females with an age range of 35-68 years, and a male group which contained 24 males with an age range of 39-69 years. ELISA kits were used to measure insulin and IL-8. The levels of insulin and IL-8 were considerably elevated throughout (p < 0.001), total cholesterol, Low Density Lipoprotein (LDL), were significantly elevated (p < 0.001) in all patients as well. There was positive correlation between Interleukin-8 with LDL, while there was negative correlation with total cholesterol and High Density Lipoprotein (HDL). Interleukin-8 levels increase with obesity in patients and control groups, Interleukin-8 positively correlated with LDL-cholesterol and negatively correlated with HDL-C thus make us consider it as atherogenic factor, the increase in the level of IL-8 in patients who have diabetes mellitus may indicate increasing the incidence of atherosclerosis.

The study signifies the importance of olefin metathesis in developing industrially important platform chemicals from a non-edible renewable resource, palash oil using Grubb’s second generation catalyst. The reaction conditions were optimized by varying the concentration of the catalyst, 0.03-0.05 mM and the temperature, 45-100 °C of the reaction. Maximum yield of the metathesized products, as analysed using GC/GC-MS were obtained employing lower concentration of the catalyst, 0.03 Mm and temperature, 45 °C for 36 h. The metathesized products showed the formation of hydrocarbons namely 9-octadecene (10.9%) and cyclodecacyclotetradecene (27%) as major. The formation of cyclodecacyclotetradecene was observed for the first time. The study also describes the possible routes and the molecules involved in the formation of the metathesized products.

Glycerol-based SO₃H-functionalized carbon catalyst was demonstrated as an efficient and recyclable green catalyst for the chemoselective synthesis of pentaerythritol diacetals with aromatic aldehydes in the presence of ketones in excellent yields in toluene at 80 °C. In addition, the catalyst also has the capability for the deprotection of pentaerythritol diacetals in methanol at reflux temperature. The recovered catalyst without any pre-treatment was reused for 5 cycles without any deactivation and leaching into the reaction medium under optimum conditions.

Highly substituted pyrimidine/pyrrolidine derivatives were synthesized for the first time in water under neutral conditions by the reaction of aromatic amines, dimethyl/diethyl acetylene dicarboxylates, formaldehyde mediated by β-cyclodextrin (β-CD) in good to excellent yields. β-Cyclodextrin can be recovered and reused without any loss of catalytic activity. The β-Cyclodextrins employed were inexpensive and readily available when compared to other types of cyclodextrins (α, γ).

The present work reports a reverse phase high performance liquid chromatography (RP-HPLC) method and high performance thin layer chromatography (HPTLC) method for the simultaneous determination of febuxostat and diclofenac sodium in pharmaceutical dosage form. HPLC was performed using a Thermo Hypersil C₁₈ column (250 × 4.6 mm i.d., 5 μm particle size) using a mixture of methanol: KH₂PO₄ (0.02 M) (70:30, v:v) as mobile phase. Ultraviolet detection was carried out at 280 nm. The retention time of febuxostat and diclofenac sodium were found to be 6.725 and 8.892 min, respectively. The HPTLC separation was conducted on Merck HPTLC aluminum sheets of silica gel 60 F₂₅₄ as stationary phase using toluene:methanol in the ratio of 7:3 (v:v) as the mobile phase. The detection of febuxostat and diclofenac sodium was carried out at 297 nm. The R_f values of febuxostat and diclofenac sodium were found to be 0.48 and 0.60, respectively. Both the methods were validated as per ICH guidelines. The proposed methods were found to be suitable for the quantification of the selected combination of drugs in pharmaceutical dosage form.

In the present manuscript, we report synthesis of new 3 and 5 substituted 2-imino thiazolidine-4-ones by three step synthetic protocols from 3-trifluormethyl aniline or 2-amino heterocycle. The compounds were evaluated for in vitro activities against Mycobacterium tuberculosis (MTB) in presence and absence of efflux pump inhibitor, cytotoxicity against RAW 264.7 cells. Among the thirty six compounds, 2-imino-3-(5-nitrothiazol-2-yl)-5-(3,4,5-trimethoxybenzylidene)thiazolidin-4-one (5g) was found to be the most active compound in vitro with MICs of 3.31 µM against log-phase culture of MTB and also non-toxic up to 100 µM. Compound 5g showed minimum inhibitory concentration (MIC) of 0.82 µM against MTB in presence of efflux pump inhibitor verapamil.