Displaying publications 1 - 20 of 23 in total

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  1. Fulltext Impact of green intellectual capital, green organizational culture, and frugal innovation on sustainable business model innovation: Dataset of manufacturing firms in Pakistan
    Bhatti SM, Zia Ul Haq M, Kanwal S, Makhbul ZKM
    Data Brief, 2024 Jun;54:110419.
    PMID: 38690320 DOI: 10.1016/j.dib.2024.110419
    This dataset integrates and helps examine the impact of green intellectual capital (GIC) which comprises of green human capital (GHC), green structural capital (GSC), and green relational capital (GRC) on green organizational culture (GOC). Secondly, it enables the investigation of GOC as a mediation phenomenon between GIC and sustainable business model innovation (SBMI). Moreover, it highlights the moderation of frugal innovation (FGL) on GOC and SBMI relationship. An online survey was designed using Google forms to collect data from 345 middle/ senior management employees working in medium and large manufacturing firms in Pakistan. Unit of analysis is the organization; thus, each response represents one firm. SPSS and Smart PLS 4 were used for data analysis. Dataset demonstrates that GHC, GSC, and GRC positively impact GOC, which subsequently enhances SBMI. Moreover, effective implementation of FGL can bolster the effect of GOC on SBMI. The dataset is valuable as it can be reproduced and reanalyzed. It offers insights for professionals to revolutionize their innovation for environmental initiatives particularly in the manufacturing sector and train their staff to use modern eco-friendly ingenuities leading to enhanced business performance as well as sustainable development goals. Furthermore, the dataset holds significance for policymakers involved in implementing green economic revitalization programs, enabling them to offer incentives or penalties to encourage compliance.
  2. Fulltext Normalized Difference Vegetation Index as a tool for wheat yield estimation: a case study from Faisalabad, Pakistan
    Sultana SR, Ali A, Ahmad A, Mubeen M, Zia-Ul-Haq M, Ahmad S, et al.
    ScientificWorldJournal, 2014;2014:725326.
    PMID: 25045744 DOI: 10.1155/2014/725326
    For estimation of grain yield in wheat, Normalized Difference Vegetation Index (NDVI) is considered as a potential screening tool. Field experiments were conducted to scrutinize the response of NDVI to yield behavior of different wheat cultivars and nitrogen fertilization at agronomic research area, University of Agriculture Faisalabad (UAF) during the two years 2008-09 and 2009-10. For recording the value of NDVI, Green seeker (Handheld-505) was used. Split plot design was used as experimental model in, keeping four nitrogen rates (N1 = 0 kg ha(-1), N2 = 55 kg ha(-1), N3 = 110 kg ha(-1), and N4 = 220 kg ha(-1)) in main plots and ten wheat cultivars (Bakkhar-2001, Chakwal-50, Chakwal-97, Faisalabad-2008, GA-2002, Inqlab-91, Lasani-2008, Miraj-2008, Sahar-2006, and Shafaq-2006) in subplots with four replications. Impact of nitrogen and difference between cultivars were forecasted through NDVI. The results suggested that nitrogen treatment N4 (220 kg ha(-1)) and cultivar Faisalabad-2008 gave maximum NDVI value (0.85) at grain filling stage among all treatments. The correlation among NDVI at booting, grain filling, and maturity stages with grain yield was positive (R(2) = 0.90; R(2) = 0.90; R(2) = 0.95), respectively. So, booting, grain filling, and maturity can be good depictive stages during mid and later growth stages of wheat crop under agroclimatic conditions of Faisalabad and under similar other wheat growing environments in the country.
  3. Fulltext Rubus fruticosus L.: constituents, biological activities and health related uses
    Zia-Ul-Haq M, Riaz M, De Feo V, Jaafar HZ, Moga M
    Molecules, 2014 Jul 28;19(8):10998-1029.
    PMID: 25072202 DOI: 10.3390/molecules190810998
    Rubus fruticosus L. is a shrub famous for its fruit called blackberry fruit or more commonly blackberry. The fruit has medicinal, cosmetic and nutritive value. It is a concentrated source of valuable nutrients, as well as bioactive constituents of therapeutic interest highlighting its importance as a functional food. Besides use as a fresh fruit, it is also used as ingredient in cooked dishes, salads and bakery products like jams, snacks, desserts, and fruit preserves. R. fruticosus contains vitamins, steroids and lipids in seed oil and minerals, flavonoids, glycosides, terpenes, acids and tannins in aerial parts that possess diverse pharmacological activities such as antioxidant, anti-carcinogenic, anti-inflammatory, antimicrobial anti-diabetic, anti-diarrheal, and antiviral. Various agrogeoclimatological factors like cultivar, environmental conditions of the area, agronomic practices employed, harvest time, post-harvest storage and processing techniques all influence the nutritional composition of blackberry fruit. This review focuses on the nutrients and chemical constituents as well as medicinal properties of different parts of R. fruticosus. Various cultivars and their physicochemical characteristics, polyphenolic content and ascorbic acid content are also discussed. The information in the present work will serve as baseline data and may lead to new biomedical applications of R. fruticosus as functional food.
  4. Fulltext Anti-inflammatory and antiplatelet activities of plasma are conserved across twelve mammalian species
    Ahmed S, Gul S, Idris F, Hussain A, Zia-Ul-Haq M, Jaafar HZ, et al.
    Molecules, 2014;19(8):11385-94.
    PMID: 25090125 DOI: 10.3390/molecules190811385
    Human plasma inhibits arachidonic acid metabolism and platelet aggregation. This helps human form a haemostatic control system that prevents the progress of certain aggregatory or inflammatory reactions. Whether this property of plasma is unique to human or extends to other species is not well known. It is speculated that this protective ability of plasma remains evolutionarily conserved in different mammals. In order to confirm this, the effect of plasma from 12 different mammalian species was investigated for its inhibitory potential against arachidonic acid metabolism and platelet aggregation. Metabolism of arachidonic acid by cyclooxygenase and lipoxygenase pathways was studies using radio-immuno assay and thin layer chromatography while platelet aggregation in the plasma of various mammals was monitored following turbedmetric method in a dual channel aggregometer. Results indicate that inhibition of AA metabolism and platelet aggregation is a common feature of plasma obtained from different mammalian species, although there exists large interspecies variation. This shows that besides human, other mammals also possess general protective mechanisms against various aggregatory and inflammatory conditions and this anti-inflammatory property of the plasma is evolutionarily conserved in mammalian species. The most likely candidates responsible for these properties of plasma include haptoglobin, albumin and lipoproteins.
  5. Fulltext Computer aided screening of secreted frizzled-related protein 4 (SFRP4): a potential control for diabetes mellitus
    Bukhari SA, Shamshari WA, Ur-Rahman M, Zia-Ul-Haq M, Jaafar HZ
    Molecules, 2014 Jul 11;19(7):10129-36.
    PMID: 25019556 DOI: 10.3390/molecules190710129
    Diabetes mellitus is a life threatening disease and scientists are doing their best to find a cost effective and permanent treatment of this malady. The recent trend is to control the disease by target base inhibiting of enzymes or proteins. Secreted frizzled-related protein 4 (SFRP4) is found to cause five times more risk of diabetes when expressed above average levels. This study was therefore designed to analyze the SFRP4 and to find its potential inhibitors. SFRP4 was analyzed by bio-informatics tools of sequence tool and structure tool. A total of three potential inhibitors of SFRP4 were found, namely cyclothiazide, clopamide and perindopril. These inhibitors showed significant interactions with SFRP4 as compared to other inhibitors as well as control (acetohexamide). The findings suggest the possible treatment of diabetes mellitus type 2 by inhibiting the SFRP4 using the inhibitors cyclothiazide, clopamide and perindopril.
  6. Fulltext Validation of ethnopharmacological uses of Murraya paniculata in disorders of diarrhea, asthma and hypertension
    Saqib F, Ahmed MG, Janbaz KH, Dewanjee S, Jaafar HZ, Zia-Ul-Haq M
    BMC Complement Altern Med, 2015;15:319.
    PMID: 26354022 DOI: 10.1186/s12906-015-0837-7
    Murraya paniculata is traditionally used for management of gut, air way and cardiovascular disorders. The study was conducted for provision of pharmacological rationalization for folkloric uses of Murraya paniculata in gut, air way and cardiovascular problems.
  7. Fulltext Robust Synthesis of Ciprofloxacin-Capped Metallic Nanoparticles and Their Urease Inhibitory Assay
    Nisar M, Khan SA, Qayum M, Khan A, Farooq U, Jaafar HZ, et al.
    Molecules, 2016 Mar 25;21(4):411.
    PMID: 27023506 DOI: 10.3390/molecules21040411
    The fluoroquinolone antibacterial drug ciprofloxacin (cip) has been used to cap metallic (silver and gold) nanoparticles by a robust one pot synthetic method under optimized conditions, using NaBH₄ as a mild reducing agent. Metallic nanoparticles (MNPs) showed constancy against variations in pH, table salt (NaCl) solution, and heat. Capping with metal ions (Ag/Au-cip) has significant implications for the solubility, pharmacokinetics and bioavailability of fluoroquinolone molecules. The metallic nanoparticles were characterized by several techniques such as ultraviolet visible spectroscopy (UV), atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) methods. The nanoparticles synthesized using silver and gold were subjected to energy dispersive X-ray tests in order to show their metallic composition. The NH moiety of the piperazine group capped the Ag/Au surfaces, as revealed by spectroscopic studies. The synthesized nanoparticles were also assessed for urease inhibition potential. Fascinatingly, both Ag-cip and Au-cip NPs exhibited significant urease enzyme inhibitory potential, with IC50 = 1.181 ± 0.02 µg/mL and 52.55 ± 2.3 µg/mL, compared to ciprofloxacin (IC50 = 82.95 ± 1.62 µg/mL). MNPs also exhibited significant antibacterial activity against selected bacterial strains.
  8. Fulltext Synthesis and Consecutive Reactions of α-Azido Ketones: A Review
    Faiz S, Zahoor AF, Rasool N, Yousaf M, Mansha A, Zia-Ul-Haq M, et al.
    Molecules, 2015 Aug 13;20(8):14699-745.
    PMID: 26287135 DOI: 10.3390/molecules200814699
    This review paper covers the major synthetic approaches attempted towards the synthesis of α-azido ketones, as well as the synthetic applications/consecutive reactions of α-azido ketones.
  9. Fulltext Nigella sativa Fixed and Essential Oil Supplementation Modulates Hyperglycemia and Allied Complications in Streptozotocin-Induced Diabetes Mellitus
    Sultan MT, Butt MS, Karim R, Zia-Ul-Haq M, Batool R, Ahmad S, et al.
    Evid Based Complement Alternat Med, 2014;2014:826380.
    PMID: 24511321 DOI: 10.1155/2014/826380
    In the recent era, diabetes mellitus has emerged as one of the significant threats to public health and this situation demands the attention of the researchers and allied stakeholders. Dietary regimens using functional and nutraceutical foods are gaining wide range of acceptance and some traditional medicinal plants are of considerable importance. The main objective of this instant study was to explore the antidiabetic potential of Nigella sativa fixed oil (NSFO) and essential oil (NSEO). Three experimental groups of rats received diets during the entire study duration, that is, D1 (control), D2 (NSFO: 4.0%), and D3 (NSEO: 0.30%). Experimental diets (NSFO & NSEO) modulated the lipid profile, while decreasing the antioxidant damage. However, production of free radicals, that is, MDA, and conjugated dienes increased by 59.00 and 33.63%, respectively, in control. On the contrary, NSFO and NSEO reduced the MDA levels by 11.54 and 26.86% and the conjugated dienes levels by 32.53 and 38.39%, respectively. N. sativa oils improved the health and showed some promising anti-diabetic results.
  10. Fulltext Multiple pathways are responsible for anti-inflammatory and cardiovascular activities of Hordeum vulgare L
    Gul S, Ahmed S, Kifli N, Uddin QT, Batool Tahir N, Hussain A, et al.
    J Transl Med, 2014;12:316.
    PMID: 25428431 DOI: 10.1186/s12967-014-0316-9
    Hordeum vulgare L. (HV or barley) is used by traditional healers to treat various inflammatory and cardiovascular diseases, without the knowledge of pharmacologic rationale behind its actions. This study was designed to explore the potential scientific mechanism(s) that could explain the use of Hordeum vulgare in traditional medicine as a treatment for various inflammatory and cardiovascular diseases.
  11. Fulltext Regioselective synthesis of 2-(bromomethyl)-5-aryl-thiophene derivatives via palladium (0) catalyzed suzuki cross-coupling reactions: as antithrombotic and haemolytically active molecules
    Rizwan K, Zubair M, Rasool N, Ali S, Zahoor AF, Rana UA, et al.
    Chem Cent J, 2014;8:74.
    PMID: 25685184 DOI: 10.1186/s13065-014-0074-z
    It is seen that the regioselective functionalizations of halogenated heterocycles play an important role in the synthesis of several types of organic compounds. In this domain, the Suzuki-Miyaura reaction has emerged as a convenient way to build carbon-carbon bonds in synthesizing organic compounds. Some of the most important applications of these reactions can be seen in the synthesis of natural products, and in designing targeted pharmaceutical compounds. Herein, we present the regioselective synthesis of the novel series of 2-(bromomethyl)-5-aryl-thiophenes 3a-i, via Suzuki cross-coupling reactions of various aryl boronic acids with 2-bromo-5-(bromomethyl)thiophene (2).
  12. Fulltext Thermodynamic and spectroscopic investigation of interactions between reactive red 223 and reactive orange 122 anionic dyes and cetyltrimethyl ammonium bromide (CTAB) cationic surfactant in aqueous solution
    Irfan M, Usman M, Mansha A, Rasool N, Ibrahim M, Rana UA, et al.
    ScientificWorldJournal, 2014;2014:540975.
    PMID: 25243216 DOI: 10.1155/2014/540975
    The present study describes the conductometric and spectroscopic study of the interaction of reactive anionic dyes, namely, reactive red 223 and reactive orange 122 with the cationic surfactant cetyltrimethyl ammonium bromide (CTAB). In a systematic investigation, the electrical conductivity data was used to calculate various thermodynamic parameters such as free energy (ΔG), enthalpy (ΔH), and the entropy (ΔS) of solubilization. The trend of change in these thermodynamic quantities indicates toward the entropy driven solubilization process. Moreover, the results from spectroscopic data reveal high degree of solubilization, with strong interactions observed in the cases of both dyes and the CTAB. The spontaneous nature of solubilization and binding was evident from the observed negative values of free energies (ΔG p and ΔG b).
  13. Fulltext Chemical composition and Biological studies of Ficus benjamina
    Imran M, Rasool N, Rizwan K, Zubair M, Riaz M, Zia-Ul-Haq M, et al.
    Chem Cent J, 2014;8(1):12.
    PMID: 24524349 DOI: 10.1186/1752-153X-8-12
    Current study has been designed to estimate the possible antioxidant, antimicrobial and hemolytic potential of Ficus benjamina different parts (leaves, stem and root).
  14. Fulltext Water Spinach, Ipomoea aquatic (Convolvulaceae), Ameliorates Lead Toxicity by Inhibiting Oxidative Stress and Apoptosis
    Dewanjee S, Dua TK, Khanra R, Das S, Barma S, Joardar S, et al.
    PLoS One, 2015;10(10):e0139831.
    PMID: 26473485 DOI: 10.1371/journal.pone.0139831
    BACKGROUND: Ipomoea aquatica (Convolvulaceae), an aquatic edible plant, is traditionally used against heavy metal toxicity in India. The current study intended to explore the protective role of edible (aqueous) extract of I. aquatica (AEIA) against experimentally induced Pb-intoxication.

    METHODS: The cytoprotective role of AEIA was measured on mouse hepatocytes by cell viability assay followed by Hoechst staining and flow cytometric assay. The effect on ROS production, lipid peroxidation, protein carbonylation, intracellular redox status were measured after incubating the hepatocytes with Pb-acetate (6.8 μM) along with AEIA (400 μg/ml). The effects on the expressions of apoptotic signal proteins were estimated by western blotting. The protective role of AEIA was measured by in vivo assay in mice. Haematological, serum biochemical, tissue redox status, Pb bioaccumulation and histological parameters were evaluated to estimate the protective role of AEIA (100 mg/kg) against Pb-acetate (5 mg/kg) intoxication.

    RESULTS: Pb-acetate treated hepatocytes showed a gradual reduction of cell viability dose-dependently with an IC50 value of 6.8 μM. Pb-acetate treated hepatocytes exhibited significantly enhanced levels (p < 0.01) of ROS production, lipid peroxidation, protein carbonylation with concomitant depletion (p < 0.01) of antioxidant enzymes and GSH. However, AEIA treatment could significantly restore the aforementioned parameters in murine hepatocytes near to normalcy. Besides, AEIA significantly reversed (p < 0.05-0.01) the alterations of transcription levels of apoptotic proteins viz. Bcl 2, Bad, Cyt C, Apaf-1, cleaved caspases [caspase 3, caspase 8 and caspase 9], Fas and Bid. In in vivo bioassay, Pb-acetate treatment caused significantly high intracellular Pb burden and oxidative pressure in the kidney, liver, heart, brain and testes in mice. In addition, the haematological and serum biochemical factors were changed significantly in Pb-acetate-treated animals. AEIA treatment restored significantly the evaluated-parameters to the near-normal position.

    CONCLUSION: The extract may offer the protective effect via counteracting with Pb mediated oxidative stress and/or promoting the elimination of Pb by chelating. The presence of substantial quantities of flavonoids, phenolics and saponins would be responsible for the overall protective effect.

  15. Fulltext Selective C-arylation of 2,5-dibromo-3-hexylthiophene via Suzuki cross coupling reaction and their pharmacological aspects
    Ikram HM, Rasool N, Ahmad G, Chotana GA, Musharraf SG, Zubair M, et al.
    Molecules, 2015 Mar 23;20(3):5202-14.
    PMID: 25806546 DOI: 10.3390/molecules20035202
    The present study reports the synthesis of various new derivatives based on 5-aryl-2-bromo-3-hexylthiophene with moderate-to-good yields via a palladium-catalyzed Suzuki cross-coupling reaction. This coupling method involved the reaction of 2,5-dibromo-3-hexylthiophene with several arylboronic acids in order to synthesize corresponding thiophene derivatives under controlled and optimal reaction conditions. The different substituents (CH3, OCH3, Cl, F etc.) present on arylboronic acids are found to have significant electronic effects on the overall properties of new products. The synthesized thiophene molecules were studied for their haemolytic, biofilm inhibition and anti-thrombolytic activities, and almost all products showed potentially good properties. The compound 2-bromo-5-(3-chloro-4-fluorophenyl)-3-hexylthiophenein particular exhibited the highest values for haemolytic and bio-film inhibition activities among all newly synthesized derivatives. In addition, the compound 2-bromo-3-hexyl-5-(4-iodophenyl)thiophene also showed high anti-thrombolytic activity, suggesting the potential medicinal applications of these newly synthesized compounds.
  16. Fulltext Scientific basis for use of Pyrus pashia Buch.-Ham. ex D. Don. fruit in gastrointestinal, respiratory and cardiovascular ailments
    Janbaz KH, Zaeem Ahsan M, Saqib F, Imran I, Zia-Ul-Haq M, Abid Rashid M, et al.
    PLoS One, 2015;10(3):e0118605.
    PMID: 25786248 DOI: 10.1371/journal.pone.0118605
    Pyrus pashia Buch.-Ham. ex D. Don. has been used conventionally by many communities in the Himalayan region for the management of gastrointestinal, respiratory, and vascular complications. Set against this background, this study was carried out to justify the scientific basis to validate folkloric uses of fruits of Pyrus pashia Buch.-Ham. ex D. Don. (Pp.Cr) in traditional systems of medicine.
  17. Development of an extended model for the permeation of environmentally hazardous CO2 gas across asymmetric hollow fiber composite membranes
    Jamil A, Ching OP, Iqbal T, Rafiq S, Zia-Ul-Haq M, Shahid MZ, et al.
    J Hazard Mater, 2021 Sep 05;417:126000.
    PMID: 33992016 DOI: 10.1016/j.jhazmat.2021.126000
    This study presents an extended thermodynamic and phenomenological combined model to mitigate the environmental hazardous acid gas over composite membranes. The model has been applied to an acid gas such as carbon dioxide (CO2) for its permeation through polyetherimide incorporated montmorillonite (Mt) nanoparticles hollow fiber asymmetric composite membranes. The well-established non-equilibrium lattice fluid (NELF) model for penetrating low molecular weight penetrant in a glassy polyetherimide (PEI) was extended to incorporate the other important polymer/filler system features such as tortuosity in acid gas diffusion pathways resulted from layered filler aspect ratio and concentration. The model mentioned above predicts the behavior of acid gas in PEI-Mt composite membranes based on thermodynamic characteristics of CO2 and PEI and tortuosity due to Mt. The calculated results are compared to experimentally determined values of CO2 permeability through PEI-Mt composite asymmetric hollow fiber membranes at varying transmembrane pressures and Mt concentrations. A reasonable agreement was found between the model predicted behavior and experimentally determined data in terms of CO2 solubility, Mt concentration and aspect ratio were calculated based on average absolute relative error (%AARE). The proposed modified model efficiently predicts the CO2 permeance across MMMs up to 3 wt% Mt loadings and 6 bar pressure with ± 10%AARE.
  18. Fulltext In-vitro and in-vivo validation of ethnopharmacological uses of methanol extract of Isodon rugosus Wall. ex Benth. (Lamiaceae)
    Janbaz KH, Arif J, Saqib F, Imran I, Ashraf M, Zia-Ul-Haq M, et al.
    BMC Complement Altern Med, 2014 Feb 22;14:71.
    PMID: 24559094 DOI: 10.1186/1472-6882-14-71
    BACKGROUND: Isodon rugosus is used in folk Pakistan traditional practices to cure ailments related to gastrointestinal, respiratory and cardiovascular problems. Present study was undertaken to validate these folkloric uses.

    METHODS: A crude methanol extract of the aerial parts of Isodon rugosus (Ir.Cr.) was used for both in vitro and in vivo experiments. The plant extract was tested on isolated rabbit jejunum preparations for possible presence of spasmolytic activity. Moreover, isolated rabbit tracheal and aorta preparations were used to ascertain the relaxant effects of the extract. Acetylcholinesterase and butyrylcholinesterase inhibitory activities of Ir.Cr were also determined as well as its antioxidant activity. The in vivo antiemetic activity of the extract was evaluated by using the chick emesis model, while the analgesic and antipyretic activities were conducted on albino mice.

    RESULTS: The application of the crude extract of I. rugosus to isolated rabbit jejunum preparations exhibited relaxant effect (0.01-0.3 mg/ml). The Ir.Cr also relaxed K+(80 m M)-induced spastic contractions in isolated rabbit jejunum preparations and shifted the Ca+2 concentration response curves towards right (0.01-0.3 mg/ml). Similarly, the extract, when applied to the isolated rabbit tracheal preparations relaxed the carbachol (1 μM)--as well as K+ (80 mM)-induced contractions in a concentration range of 0.01-1.0 mg/ml. Moreover, it also relaxed (0.01-3.0 mg/ml) the phenylephrine (1 μM)- and K+ (80 mM)-induced contractions in isolated rabbit aorta preparations. The Ir.Cr (80 mg/kg) demonstrated antipyretic activity on pyrogen-induced pyrexia in rabbits as compared to aspirin as standard drug. The Ir.Cr also exhibited anti-oxidant as well as inhibitory effect on acetyl- and butyryl-cholinesterase and lipoxygenase (0.5 mg/ml).

    CONCLUSIONS: The observed relaxant effect on isolated rabbit jejunum, trachea and aorta preparations caused by Ir.Cr is possibly to be mediated through Ca+2 channel blockade and therefore may provided scientific basis to validate the folkloric uses of the plant in the management of gastrointestinal, respiratory and cardiovascular ailments. The observed antioxidant activity as well as the lipoxygenase inhibitory activity may validate its traditional use in pain and inflammations.

  19. Fulltext Nigella sativa fixed and essential oil modulates glutathione redox enzymes in potassium bromate induced oxidative stress
    Sultan MT, Butt MS, Karim R, Ahmed W, Kaka U, Ahmad S, et al.
    BMC Complement Altern Med, 2015;15:330.
    PMID: 26385559 DOI: 10.1186/s12906-015-0853-7
    Nigella sativa is an important component of several traditional herbal preparations in various countries. It finds its applications in improving overall health and boosting immunity. The current study evaluated the role of fixed and essential oil of Nigella sativa against potassium bromate induced oxidative stress with special reference to modulation of glutathione redox enzymes and myeloperoxidase.
  20. Fulltext A convenient method for the synthesis of (prop-2-ynyloxy)benzene derivatives via reaction with propargyl bromide, their optimization, scope and biological evaluation
    Batool T, Rasool N, Gull Y, Noreen M, Nasim FU, Yaqoob A, et al.
    PLoS One, 2014;9(12):e115457.
    PMID: 25545159 DOI: 10.1371/journal.pone.0115457
    A highly convenient method has been developed for the synthesis of (prop-2-ynyloxy) benzene and its derivatives. Differently substituted phenol and aniline derivatives were allowed to react with propargyl bromide in the presence of K2CO3 base and acetone as solvent. The compounds were synthesized in good yields (53-85%). Low cost, high yields and easy availability of compounds helped in the synthesis. Electron withdrawing groups favor the formation of stable phenoxide ion thus in turn favors the formation of product while electron donating groups do not favor the reaction. Phenol derivatives gave good yields as compared to that of aniline. As aprotic polar solvents favor SN2 type reactions so acetone provided best solvation for the reactions. K2CO3 was proved to be good for the synthesis. Antibacterial, Antiurease and NO scavenging activity of synthesized compounds were also examined. 4-bromo-2-chloro-1-(prop-2-ynyloxy)benzene 2a was found most active compound against urease enzyme with a percentage inhibition of 82.00±0.09 at 100 µg/mL with IC50 value of 60.2. 2-bromo-4-methyl-1-(prop-2-ynyloxy)benzene 2d was found potent antibacterial against Bacillus subtillus showing excellent inhibitory action with percentage inhibition of 55.67±0.26 at 100 µg/ml wih IC50 value of 79.9. Based on results, it can be concluded that some of the synthesized compounds may have potential antiurease and antibacterial effects against several harmful substances.
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