Exploring the potential of bacterial-augmented floating treatment wetlands for the remediation of detergent-contaminated water.

Due to industrialization and urbanization, the use of detergents inadvertently led to contamination of aquatic environments, thus posing potential threat to aquatic organisms and human health. One of the main components of detergents is linear alkylbenzene sulfonate (LAS), which can cause toxic effects on living organisms, particularly aquatic life in the environment. In this study, floating treatment wetlands (FTWs) mesocosms were developed and augmented with LAS-degrading bacteria. The plant species, Brachiaria mutica (Para grass), was vegetated to establish FTWs and bacterial consortium (1:1:1:1) of Pseudomonas aeruginosa strain PJRS20, Bacillus sp. BRRH60, Acinetobacter sp. strain CYRH21, and Burkholderia phytofirmans Ps.JN was augmented (free or immobilized) in these mesocosms. Results revealed that the FTWs removed LAS from the contaminated water and their augmentation with bacteria slightly increased LAS removal during course of the experiment. Maximum reduction in LAS concentration (94%), chemical oxygen demand (91%), biochemical oxygen demand (93%), and total organic carbon (91%) was observed in the contaminated water having FTWs augmented with bacterial consortium immobilized on polystyrene sheet. This study highlights that the FTWs supported with immobilized bacteria on polystyrene sheets can provide an eco-friendly and sustainable solution for the remediation of LAS-bearing water, especially for developing countries like Pakistan.

This pilot-scale study provided insights to resolve the detergent-contaminated wastewater issue, using floating treatment wetlands (FTWs) augmented with bacteria. The FTWs augmented with bacteria immobilized on a polystyrene sheet and vegetated with Brachiaria mutica led to high degradation of LAS, a toxic compound of detergent, from the contaminated water.

Contemporary Developments in Ferrocene Chemistry: Physical, Chemical, Biological and Industrial Aspects.

Ferrocenyl-based compounds have many applications in diverse scientific disciplines, including in polymer chemistry as redox dynamic polymers and dendrimers, in materials science as bioreceptors, and in pharmacology, biochemistry, electrochemistry, and nonlinear optics. Considering the horizon of ferrocene chemistry, we attempted to condense the neoteric advancements in the synthesis and applications of ferrocene derivatives reported in the literature from 2016 to date. This paper presents data on the progression of the synthesis of diverse classes of organic compounds having ferrocene scaffolds and recent developments in applications of ferrocene-based organometallic compounds, with a special focus on their biological, medicinal, bio-sensing, chemosensing, asymmetric catalysis, material, and industrial applications.

The Development of Highly Fluorescent Hemicyanine and Dicyanoisophorone Dyes for Applications in Dye-Sensitized Solar Cells.

Ruthenium-based metal complex dyes have been employed extensively in dye-sensitized solar cells (DSSCs) as photosensitizers, but the cost and toxicity of metal complexes have promoted the development of metal-free organic dyes. The present investigation deals with the synthesis of hemicyanine and Dicyanoisophorone (DCI) based dyes adopting the D-π-A strategy, and their application on sensitization of nano-crystalline ZnO electrodes by appending the carboxyl (COOH) anchoring group as a pendant on the primary skeleton of dyes. Dyes have been characterized by UV, FTIR, and NMR spectroscopic studies. Absorption maxima (λmax) were found in the region 416-551 nm while emission wavelength (λem) was observed in the range 575-685 nm. Cyclic voltammetry and DFT calculations were used to estimate redox potential and band gap energies of dyes.

Polyethylene glycol capped copper ferrite porous nanostructured materials for efficient photocatalytic degradation of bromophenol blue.

Three different types (blank, annealed, and functionalized) of copper ferrite nanoparticles (CuFe2O4) were synthesized by the co-precipitation method. The CuFe2O4 NPs were characterized by Fourier transform infrared (FTIR), Scanning electron microscopy (SEM), X-ray diffraction (XRD), and Energy-dispersive X-ray spectroscopy (EDX) techniques. FTIR analysis confirmed that 3-APTES is successfully grafted on the surface of CuFe2O4 NPs. XRD results show the amorphous nature of blank CuFe2O4 NPs, and crystalline structure was observed for annealed and functionalized CuFe2O4 NPs. XRD results revealed that crystallite size ranges from 23.6 to 34.6 nm. SEM micrographs of blank CuFe2O4 NPs show the irregular shape and size of the nanostructure. The spherical and strongly linked structure was seen in the micrograph of functionalized CuFe2O4 NPs. EDX analysis revealed the nanostructure composed of Fe, Cu, O, and a small percentage of Si. The photocatalytic degradation efficiency of synthesized CuFe2O4 NPs was examined under UV irradiation in an aqueous medium against bromophenol blue (BPB) dye. The effect of different parameters such as irradiation time and pH on the photodegradation of BPB dye was studied by all three types of CuFe2O4 photocatalyst. Results show that the maximum photocatalytic degradation efficiency was observed for functionalized CuFe2O4 nanoparticles that degraded 98% of BPB dye in the acidic medium at pH = 1. The optimum contact time for dye degradation was 120 min by synthesized photocatalyst. Photodegradation performance of blank and annealed CuFe2O4 NPs is less than 90%. The synthesized CuFe2O4 NPs were recycled and reused, which shows good photocatalytic degradation efficiency up to 4 consecutive cycles. The kinetic model displayed that degradation reaction followed pseudo 1st order kinetics. The blank, annealed, and functionalized CuFe2O4 NPs have turnover numbers of 10.7x10 (Mudhoo et al., 2019), 12.9x10 (Mudhoo et al., 2019), and 22.2x10 (Mudhoo et al., 2019) (kg-1 sec-1) accordingly. In conclusion, all results revealed the high efficiency of prepared photocatalyst for tested hazardous dye from wastewater and encouraged more work on photodegradation of organic pollutants from wastewater.

Azomethine-clubbed thiazoles as human tissue non-specific alkaline phosphatase (h-TNAP) and intestinal alkaline phosphatase (h-IAP) Inhibitors: kinetics and molecular docking studies.

Thiazole derivatives are known inhibitors of alkaline phosphatase, but various side effects have reduced their curative efficacy. Conversely, compounds bearing azomethine linkage display a broad spectrum of biological applications. Therefore, combining the two scaffolds in a single structural unit should result in joint beneficial effects of both. A new series of azomethine-clubbed thiazoles (3a-i) was synthesized and appraised for their inhibitory potential against human tissue non-specific alkaline phosphatase (h-TNAP) and human intestinal alkaline phosphatase (h-IAP). Compounds 3c and 3f were found to be most potent compounds toward h-TNAP with IC50 values of 0.15 ± 0.01 and 0.50 ± 0.01 µM, respectively, whereas 3a and 3f exhibited maximum potency for h-IAP with IC50 value of 2.59 ± 0.04 and 2.56 ± 0.02 µM, respectively. Molecular docking studies were also performed to find the type of binding interaction between potential inhibitor and active sites of enzymes. The enzymes inhibition kinetics studies were carried out to define the mechanism of enzyme inhibition. The current study leads to discovery of some potent inhibitors of alkaline phosphatase that is promising toward identification of compounds with druggable properties.

Synthesis of novel hybrid pharmacophore of N-((4-sulfamoylphenyl)carbamothioyl)alkanamides as potent carbonic anhydrase-II and 15-lipoxygenase inhibitors.

A series of N-((4-sulfamoylphenyl)carbamothioyl)alkanamides (5a-j) were synthesized by the reaction of sulphanilamide in dry acetone with freshly prepared alkyl and acyl isothiocyanates (5a-j). The structures of products were confirmed by IR, 1 H, and 13 C NMR. The synthesized compounds were screened as inhibitors of the bovine erythrocyte carbonic anhydrase isoform II (bCA II) and 15-lipoxygenase enzyme (15-LOX). Most of the derivatives showed significant activity against bCA-II while only few compounds were found active against 15-LOX. Molecular docking studies of most active compounds were carried out against bCA II as well as 15-LOX to rationalize the binding mode and interactions of compound in the active sites. Additionally, the pharmacokinetic properties of the compounds were predicted through computational tools, which reflect that these compounds possess acceptable pharmacokinetic profile and good drug-likeness.

Synthesis, characterization and biological evaluation of indomethacin derived thioureas as purinergic (P2Y1, P2Y2, P2Y4, and P2Y6) receptor antagonists.

G-protein-coupled receptors for extracellular nucleotides are known as P2Y receptors and are made up of eight members that are encoded by distinct genes and can be classified into two classes based on their affinity for specific G-proteins. P2Y receptor modulators have been studied extensively, but only a few small-molecule P2Y receptor antagonists have been discovered so far and approved by drug agencies. Derivatives of indole carboxamide have been identified as P2Y12 and P2X7 antagonist, as a result, we developed and tested a series of indole derivatives4a-lhaving thiourea moiety as P2Y receptor antagonist by using a fluorescence-based assay to measure the inhibition of intracellular calcium release in 1321N1 astrocytoma cells that had been stably transfected with the P2Y1, P2Y2, P2Y4 and P2Y6 receptors. Most of the compounds exhibited moderate to excellent inhibition activity against P2Y1 receptor subtype. The series most potent compound, 4h exhibited an IC50 value of 0.36 ± 0.01 µM selectivity against other subtypes of P2Y receptor. To investigate the ligand-receptor interactions, the molecular docking studies were carried out. Compound 4h is the most potent P2Y1 receptor antagonist due to interaction with an important amino acid residue Pro105, in addition to Ile108, Phe119, and Leu102.

Synthesis, X-ray, Hirshfeld surface analysis, exploration of DNA binding, urease enzyme inhibition and anticancer activities of novel adamantane-naphthyl thiourea conjugate.

1-(adamantane-1-carbonyl-3-(1-naphthyl)) thiourea (C22H24N2OS (4), was synthesized by the reaction of freshly prepared adamantane-1-carbonyl chloride from corresponding acid (3) with ammonium thiocyanate in 1:1 M ratio in dry acetone to afford the adamantane-1-carbonyl isothiocyanate (2) in situ followed by treatment with 1-naphthyl amine (3). The structure was established by elemental analyses, FTIR, 1H, 13C NMR and mass spectroscopy. The molecular and crystal structure were determined by single crystal X-ray analysis. It belongs to triclinic system P - 1 space group with a = 6.7832(5) Å, b = 11.1810(8) Å, c = 13.6660(10) Å, α = 105.941(6)°, ß = 103.730(6)°, γ = 104.562(6)°, Z = 2, V = 910.82(11) Å3. The naphthyl group is almost planar. In the crystal structure, intermolecular CH···O hydrogen bonds link the molecules into centrosymmetric dimers, enclosing R22(14) ring motifs, while the intramolecular NH···O hydrogen bonds enclose S(6) ring motifs, in which they may be effective in the stabilization of the structure. The Hirshfeld surface analysis of the crystal structure indicates that the most important contributions for the crystal packing are from H … H (59.3%), H … C/C … H (19.8%) and H … S/S … H (10.1%) interactions. Hydrogen bonding and van der Waals interactions are the dominant interactions in the crystal packing. DFT, molecular docking and urease inhibition studies revealed stability and electron withdrawing nature of 4 as compared to DNA base pairs and residues of urease. The DNA binding results from docking, UV- visible spectroscopy, and viscosity studies indicated significant binding of 4 with the DNA via intercalation and groove binding. Further investigation of the compound was done on hepatocellular carcinoma; Huh-7 cell line as well as normal human embryonic kidney; Hek-293 cell line. The compound showed significant cytotoxic activity against Huh-7 cells in comparison to normal Hek-293 cells indicating selective cytotoxicity towards cancer cells.

Effect of organic solvents on solvatochromic, fluorescence, and electrochemical properties of synthesized thiazolylcoumarin derivatives.

In this present investigation, thiazolylcoumarin derivatives (5a-5k) were synthesized from thiosemicarbazide, ethyl acetoacetate, and naphthaldehyde through a multistep route. The formation of thiazolylcoumarin derivatives with bioactive scaffolds was confirmed through nuclear magnetic resonance spectroscopy. A solvatochromic study of synthesized thiazolylcoumarin derivatives was carried out using ultraviolet-visible methods for dimethylformamide (DMF), ethyl acetate, and ethanol solvents. The redox behaviour of as-synthesized thiazolylcoumarin derivatives (5a-5k) was examined in dimethyl sulphoxide by conducting an electrochemical study. Fluorescence properties of thiazolylcoumarin derivatives were studied in DMF, ethanol, and ethyl acetate to visualize the solvent effect on the emitting ability of thiazolylcoumarin derivatives.

A comparative study of synthetic approaches towards total synthesis of histrionicotoxin: a selective inhibitor of nicotinic acetylcholine receptors.

The aim of this review is to provide a critical and comparative account of the total synthetic approaches toward histrionicotoxins, alkaloids isolated from skin extracts of Colombian poison arrow frog Dendrobates histrionicus. We have summarized the maneuvers in each paper by graphically detailing the synthesis and associated reaction niceties of only the key intermediates by different researchers. Fascinating structural feature of histrionicotoxins is "8-hydroxy-l-azaspiro[5.5]undecane core" with two side chains at C-2 and C-7 which differ in their length and nature of unsaturation. All synthetic approaches to histrionicotoxins aim at the construction of key intermediate "azaspiro[5.5]undecane ring" and installation of side chains at C-2 and C-7.

An efficient synthetic approach toward a sporadic heterocyclic scaffold: 1,3-Oxathiol-2-ylidenes; alkaline phosphatase inhibition and molecular docking studies.

We developed a simple and robust method for synthesis of 1,3-oxathiol-2-ylidene benzamides (4a-m) a sporadic class of heterocycles, by reacting freshly prepared aroyl isothiocyanates, with ethyl 2-chloroacetoacetate in presence of N-methylimidazole in dry acetonitrile. The synthesized compounds were explored for their inhibition against alkaline phosphatases and HeLa cancer cell lines. The results suggest that almost all the compounds possess good % inhibition against both enzymes, with compound 4m showing dual inhibition while 4g and 4i as potent and selective inhibitors of TNAP and c-IAP respectively. Structure activity relationship for the active members of series has been carried out based on molecular docking studies. The result of SAR shows the involvement of active inhibitors in H-bonding at various sites with different amino acid residues in addition to secondary metal ion interactions with Zn ions inside the active pocket of the enzyme. The π-π interactions between the 1,3-oxathiole ring and imidazole ring of His321 and His 317 further defines the dual mode of inhibition by compound 4m. These compounds also possess inhibition potential against cervical cell lines in the range of 2.42-69.03% with the maximum inhibition shown by the unsubstituted member 4a compared to the reference drug cisplatin.

Donor-Pi-Acceptor Fluorene Conjugates, Based on Chalcone and Pyrimidine Derivatives: an Insight into Structure-Property Relationship, Photophysical and Electrochemical Properties.

A small set of four new fluorenyl chromophores (5-5a-c) was accomplished by stepwise nucleophilic substitution, Friedel-Crafts acylation, Ullman coupling, aldol condensation and cyclization reactions. The fluorene moiety was substituted at 2,7,9 and 9' positions with diverse groups. The synthesized derivatives were characterized by FTIR, 1H-NMR and 13C-NMR spectroscopic techniques. The optical properties were evaluated by by UV-VIS absorption and Fluorescence studies. HOMO and LUMO energy levels were evaluated by electrochemical studies and were found at -5.37-5.83 eV and - 2.47-2.94 eV respectively with band gap energy values 2.88 to 2.91 eV. The band gap energy values suggested that these synthesized molecules can be manipulated in the designing of blue and green OLEDS. Graphical Abstract.

3-Aminobenzenesulfonamides incorporating acylthiourea moieties selectively inhibit the tumor-associated carbonic anhydrase isoform IX over the off-target isoforms I, II and IV.

We describe the synthesis of a series of novel 1-aroyl/acyl-3-(3-aminosulfonylphenyl) thioureas (4a-k) acting as human carbonic anhydrase (hCA, EC 4.2.1.1) inhibitors. Reaction of alkyl/aryl isothiocyanates with 3-aminobenzenesulfonamide afforded a series of the title compounds incorporating a variety of short as well as highly lipophilic long tails. The newly synthesized sulfonamides were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IV, and IX). Several compounds showed interesting inhibitory activity. The tumor-associated hCA IX was the most sensitive isoform to inhibition with these compounds, with KIs in the range of 21.5-44.0 nM and selectivity ratios over the major cytosolic isoform hCA II in the range of 3.35-37.3. The sulfonamides incorporating the phenylacetylthioureido and pentadecanoylthioureido moieties were the most hCA IX-selective inhibitors detected in this work, making them of interest for further investigations.

Design, synthesis and biological evaluation of trinary benzocoumarin-thiazoles-azomethines derivatives as effective and selective inhibitors of alkaline phosphatase.

Design, synthesis and characterization of new trinary Benzocoumarin-Thiazoles-Azomethine derivatives having three bioactive scaffolds in a single structural unit were carried out. The newly synthesized molecules were investigated for the inhibitory activity on human tissue nonspecific alkaline phosphatase (h-TNAP) and human intestinal alkaline phosphatase (h-IAP) isozymes. All the tested compounds exhibited the potent inhibition profile on both isozymes of alkaline phosphatase i.e., h-TNAP and h-IAP. Molecular docking studies were performed to explore the putative binding mode of interactions of selective inhibitors. Moreover, the synthesized derivatives were evaluated against cervical cancer cell line, HeLa and a few compounds exhibited significant inhibition in the range of 21.0-69.7%. The derivatives can be potential and selective alkaline phosphatase inhibitors for future studies.

Synthesis, molecular docking and kinetic studies of novel quinolinyl based acyl thioureas as mushroom tyrosinase inhibitors and free radical scavengers.

The enzyme tyrosinase plays a vital role in melanin biosynthesis and enzymatic browning of vegetables and fruits. A series of novel quinolinyl thiourea analogues (11a-j) were synthesized by reaction of 3-aminoquinoline and corresponding isothiocyanates, in moderate to excellent yields with different substitutions and their inhibitory effect on mushroom tyrosinase and free radical scavenging activity were evaluated. The compound N-(quinolin-3-ylcarbamothioyl)hexanamide (11c) exhibited the maximum tyrosinase inhibitory effect (IC50 = 0.0070 ±â€¯0.0098 µM) compared to other derivatives and the reference Kojic acid (IC50 = 16.8320 ±â€¯0.0621 µM). The docking studies were carried out and the compound (11c) showed most negative estimated free energy of -7.2 kcal/mol in mushroom tyrosinase active site. The kinetic analysis revealed that the compound (11c) inhibits the enzyme tyrosinase non-competitively to form the complex of enzyme and inhibitor. The results revealed that 11c could be identified as putative lead compound for the design of efficient tyrosinase inhibitors.

Identification and mapping of QTLs associated with drought tolerance traits in rice by a cross between Super Basmati and IR55419-04.

Water stress, in a climate change scenario is one of the major threats for sustainable rice productivity. Combining drought resistance with yield and desirable economic traits is the most promising solution for the researchers. Although several studies resulted in the identification of QTLs for drought resistance in rice, but none of them serve as a milestone. Therefore, there is always a quest to find the new QTLs. The present investigation was carried out to map QTLs involved in drought resistance and yield related parameter in a cross of IR55419-04 and Super Basmati. An F2 population of 418 individuals was used as the mapping population. The raised nursery was transplanted in lyzimeters. Two extreme sets of tolerant (23 Nos.) and sensitive (23 Nos.) individuals were selected based on total water uptake under water stress conditions. Two hundred thirty microsatellite markers staggered on the whole genome were used for identifying polymorphic markers between the two parents. The selected 73 polymorphic microsatellites were used to genotype individuals and were scattered on a distance of 1735 cM on all 12 linkage groups. QTL analysis was performed by using the WinQTL Cartographer 2.5 V. A total of 21 QTLs were detected using composite interval mapping. The QTLs relating to drought tolerance at the vegetative stage were found on chromosome 1. Novel genomic regions were detected in the marker interval RM520-RM143 and RM168-RM520. The region has a significant QTL qTWU3.1 for total water uptake. Root morphological trait QTLs were found on chromosome 3. QTLs responsible for additive effects were due to the alleles of the IR55419-04. These novel QTLs can be used for marker assisted breeding to develop new drought-tolerant rice varieties and fine mapping can be used to explore the functional relationship between the QTLs and phenotypic traits.

Phytochemical profiling and antiviral activity of Ajuga bracteosa, Ajuga parviflora, Berberis lycium and Citrus lemon against Hepatitis C Virus.

Hepatitis C is a serious health issue and cause liver disorders in millions of people. Available therapeutic agents require long term administration with numerous side effects. Therefore, there is a dire need to find alternative treatment options for this disease. Since ancient times, medicinal plants are widely used to cure various diseases with no or less harmful effects. Therefore, this study was designed to find out phytochemicals and investigate antiviral activity of methanol extract of Ajuga bracteosa, Ajuga parviflora, Berberis lycium and Citrus lemon against Hepatitis C Virus (HCV infection). Phytochemical analysis of the plant extract was performed using various chemical tests. Toxicity of the plant extract was determined against using trypan blue exclusion method. Antiviral activity of the selected plant extract was find out against HCV infected HepG2 cells. For this purpose, HepG2 cells were seeded with HCV positive and negative serum and nontoxic doses of plant extract for 24 and 48 h. After this RNA was extracted and viral load was determined using Real-time PCR. Phytochemical analysis showed the presence of flavonoids and phenols in all plant extracts while amino acids, alkaloids and tannins were present in B. lycium and saponins were detected in C. lemon. Toxicity assay showed that all plant extracts were nontoxic at maximum concentration of 200 µg/ml except B. lycium, which showed mild toxicity at 40 µg/ml and were extremely toxic at 60 µg/ml and above doses. Real-time PCR quantitation result revealed that after 24 h treatments A. parviflora showed highest antiviral activity, followed by A. bracteosa, while B. lycium extract had low (35%) and C. lemon has no antiviral effects. The 48 h treatments showed an increase antiviral activity by A. bracteosa followed by A. parviflora and B. lycium while C. lemon showed negative effect. Our results depicted that mentioned plants might be used as an alternative therapeutic regime or in combination with existing treatments against HCV.

Synthesis of Symmetric Bridged Bis-Pyrazolone Based Metal Complex Acid Dyes and their Applications on Leather.

Our present investigation aims at the synthesis and application of new, symmetric bridged bis-pyrazolone based acid dyes. The bis-pyrazolone compounds were accomplished from bis- hydrazine of 4,4'-Diaminostilbene-2,2'-disulfonic acid and ethyl acetoacetate. The bis-pyrazolones have been coupled with diazonium salts of o-hydroxyl aromatic amines which resulted in ligand dyes. The intermediate ligand dyes were treated with 3d transition metals to achieve the targeted metal complex acid dyes. The structures of investigated compounds were confirmed with the help of spectroscopic techniques. Dyes were applied on leather and their application parameters including their light fastness, wash fastness and rubbing fastness were determined. Graphical Abstract Symmetric brymmetric Bridged bis-Pyrazolone based Metal Complex Acid.

4-Aminopyridine based amide derivatives as dual inhibitors of tissue non-specific alkaline phosphatase and ecto-5'-nucleotidase with potential anticancer activity.

Ecto-nucleotidase members i.e., ecto-5'-nucleotidase and alkaline phosphatase, hydrolyze extracellular nucleotides and play an important role in purinergic signaling. Their overexpression are implicated in a variety of pathological states, including immunological diseases, bone mineralization, vascular calcification and cancer, and thus they represent an emerging drug targets. In order to design potent and selective inhibitors, new derivatives of 4-aminopyridine have been synthesized (10a-10m) and their structures were established on the basis of spectral data. The effect of nature and position of substituent was interestingly observed and justified on the basis of their detailed structure activity relationships (SARs) against both families of ecto-nucleotidase. Compound 10a displayed significant inhibition (IC50 ±â€¯SEM = 0.25 ±â€¯0.05 µM) that was found ≈168 fold more potent as compared to previously reported inhibitor suramin (IC50 ±â€¯SEM = 42.1 ±â€¯7.8 µM). This compound exhibited 6 times more selectivity towards h-TNAP over h-e5'NT. The anticancer potential and mechanism were also established using cell viability assay, flow cytometric analysis and nuclear staining. Molecular docking studies were also carried out to gain insight into the binding interaction of potent compounds within the respective enzyme pockets and herring-sperm DNA.

Substituted (E)-2-(2-benzylidenehydrazinyl)-4-methylthiazole-5-carboxylates as dual inhibitors of 15-lipoxygenase & carbonic anhydrase II: synthesis, biochemical evaluation and docking studies.

15-Lipoxygenase (15-LOX) plays a major role in many inflammatory lung diseases including chronic obstructive pulmonary disease (COPD), asthma and chronic bronchitis. Over-expression of 15-LOX is related with some specific carcinomas including pancreatic, gastric and brain tumor. Similarly among different isozymes of carbonic anhydrase (CA), CA II is expressed in pancreatic, gastric carcinomas as well as in brain tumors. Therefore, novel potent inhibitors of both 15-LOX and CA II are required to explore the role of these enzymes further and to enable the drug discovery efforts. For this purpose, a series of benzyledinyl-hydrazinyl substituted thiazole derivatives were designed, synthesized and characterized by FTIR, 1H, &13C NMR spectroscopy. The derivatives were then evaluated for their potential to inhibit 15-LOX and bovine carbonic anhydrase II (bCA II). Most of these compounds showed excellent inhibitory potential for 15-LOX with an IC50 of 0.12 ± 0.002 to 0.69 ± 0.5 µM and showed moderate inhibition potency for bCA II with compound 5h (IC50 = 1.26 ± 0.24 µM) being the most active. The most potent compound 5a that emerged as a dual inhibitor of both enzymes, exhibiting 24 times greater selectivity for 15-LOX over bCA II. Compound 5a exhibited dual potent inhibitory activity against both 15-LOX and bCA II enzymes having IC50 values of 0.12 ± 0.002 and 2.93 ± 0.22 µM, respectively. Molecular docking studies of potent as well as dual inhibitors were also carried out to provide an insight into the binding site interactions.