Displaying publications 1 - 20 of 52 in total

Abstract:
Sort:
  1. Fulltext Crystal structure of 2-(1,3-dioxoindan-2-yl)iso-quinoline-1,3,4-trione
    Ghalib RM, Chidan Kumar CS, Hashim R, Sulaiman O, Fun HK
    Acta Crystallogr E Crystallogr Commun, 2015 Jan 1;71(Pt 1):o6-7.
    PMID: 25705509 DOI: 10.1107/S2056989014025997
    In the title iso-quinoline-1,3,4-trione derivative, C18H9NO5, the five-membered ring of the indane fragment adopts an envelope conformation with the nitro-gen-substituted C atom being the flap. The planes of the indane benzene ring and the iso-quinoline-1,3,4-trione ring make a dihedral angle of 82.06 (6)°. In the crystal, mol-ecules are linked into chains extending along the bc plane via C-H⋯O hydrogen-bonding inter-actions, enclosing R 2 (2)(8) and R 2 (2)(10) loops. The chains are further connected by π-π stacking inter-ations, with centroid-to-centroid distances of 3.9050 (7) Å, forming layers parallel to the b axis.
    Matched MeSH terms: Quinolines
  2. LC-MS/MS quantitation of antimalarial drug piperaquine and metabolites in human plasma
    Aziz MY, Hoffmann KJ, Ashton M
    J Chromatogr B Analyt Technol Biomed Life Sci, 2017 Sep 15;1063:253-258.
    PMID: 28863865 DOI: 10.1016/j.jchromb.2017.06.035
    PURPOSE: This study aimed to develop a sensitive, quantitative assay for the antimalarial piperaquine (PQ) and its metabolites M1 and M2 in human plasma.

    RESULTS: Analytes were gradiently separated on a C18 column and detected with a Sciex API 4000 MS/MS with an ESI source operated in the positive ion mode with deuterated PQ as internal standard. The response was linear in the range 3.9-2508nM with a runtime of 7.0min per sample. The method was applied to clinical samples from healthy volunteers.

    CONCLUSION: This LC-MS/MS method for the simultaneous quantitation of PQ and two of its metabolites in plasma may prove helpful for assessment of metabolite safety issues in vivo.

    Matched MeSH terms: Quinolines/blood*; Quinolines/metabolism; Quinolines/pharmacokinetics; Quinolines/chemistry
  3. Phoebegrandine C, a novel proaporphine-tryptamine dimer, from Phoebe grandis (Nees) Merr
    Mukhtar MR, Hadi AH, Sévenet T, Martin MT, Awang K
    Nat Prod Res, 2004 Apr;18(2):163-7.
    PMID: 14984091
    A novel proaporphine-tryptamine dimer alkaloid, named phoebegrandine C 1, was isolated from the leaves of Phoebe grandis (Nees) Merr. Its structural elucidation was carried out using spectroscopic techniques, notably 2D NMR.
    Matched MeSH terms: Quinolines/isolation & purification*; Quinolines/chemistry*
  4. Furoquinoline alkaloids from Melicope bonwickii (F.Muell.) T.Hartley
    Komala I, Rahmani M, Sukari MA, Mohd Ismail HB, Cheng Lian GE, Rahmat A
    Nat Prod Res, 2006 Apr;20(4):355-60.
    PMID: 16644530
    Investigation on the leaves of Melicope bonwickii (F.Muell.) T.Hartley (Rutaceae) afforded a new 7-(2'-hydroxy-3'-chloroprenyloxy)-4-methoxyfuroquinoline (1) together with the known 7-(2',3'-epoxyprenyloxy)-4-methoxyfuroquinoline (2), evellerine (3) kokusaginine (4) and an amide aurantiamide acetate (5). Compounds 1 and 2 showed significant activity against cervical cell lines (Hela).
    Matched MeSH terms: Quinolines/isolation & purification*; Quinolines/pharmacology; Quinolines/chemistry*
  5. Fulltext Montelukast in children with allergic rhinitis amid COVID-19 pandemic
    Kow CS, Hasan SS
    Acta Paediatr, 2020 10;109(10):2151.
    PMID: 32686128 DOI: 10.1111/apa.15491
    Matched MeSH terms: Quinolines
  6. Fulltext Mathematical modelling of the growth of Klebsiella pneumoniae on 2-methylquinoline
    Shukor, M.S., Shukor, M.Y.
    Bioremediation Science and Technology Research, 2015;3(1):16-19.
    MyJurnal
    Quinolines compounds are toxic pollutants. Their biodegradation by microbes represents a tool
    for bioremediation. The growth of Klebsiella penumoniae on 2-methylquinoline shows typical
    sigmoidal bacterial growth curves. Since there exists a variety of models for describing the
    growth profile of microorganism such as logistic, Gompertz, Richards, Schnute, Baranyi-
    Roberts, Von Bertalanffy, Buchanan three-phase and more recently Huang models, the growth
    curves exhibit under such conditions would be an excellent study for finding the best model.
    The Huang model was chosen as the best model based on statistical tests such as root-meansquare
    error (RMSE), adjusted coefficient of determination (R2), bias factor (BF), accuracy
    factor (AF) and corrected AICc (Akaike Information Criterion). Novel constants obtained from
    the modelling exercise would be used for further secondary modelling.
    Matched MeSH terms: Quinolines
  7. Insects of Tasik Chini with special emphasis on Ichneumonid wasps
    Idris A, Ismail S, Haron Y, Suhana Y
    Sains Malaysiana, 2009;38.
    A preliminary study on selected insect communities of Tasik Chini was conducted from 27th May to 2nd June 2004 along three trails namely trail to Sg. Gumum, trail to Kampung Melai and trail to old tin mining area. A total of eight Malaise traps were installed along the trail to Sg. Gumum while sweeping net and 10 yellow pan traps per trail were used to sample insects along the other two trails. A total of 502 insect individuals consisting of eight orders and 46 families were successfully collected. Of these, the hymenopterans (ants and wasps) had the most number (298 individuals and 11 families) while the Blattaria was the least number (six individuals and two families). Of the hymenopterans, the ichneumonids had the most individuals collected (52) followed by evaniid (50) and vespid wasps (41). For the Coleopterans, Cleridae were the most collected (26) during this short study followed by Anthribidae (13). There were 62 of individuals Odonata consisting of 9 species identified.
    Matched MeSH terms: Quinolines
  8. Fulltext Modified bicinchoninic acid assay for accurate determination of variable length reducing sugars in carbohydrates
    Hussain, H., Ngaini, Z., Chong, N.F-M.
    International Food Research Journal, 2018;25(6):2614-2619.
    MyJurnal
    The accurate determination of reducing ends of malto-oligosaccharides is essential for calculating the enzyme activities of starch debranching enzymes. The suitability of the 3,5-Dinitrosalicylic acid (DNS) method, the Dygert method, and the Bicinchoninic acid (BCA) method for accurate determination of reducing ends from malto-oligosaccharides of different chain lengths is compared. The results showed that BCA assay was much more accurate than the other assays. The results for the BCA assay showed that different malto-oligosaccharides gave observed (measured) values that were significantly similar to the expected (predetermined) values. In contrast, the DNS and Dygert assays underestimated the amount of reducing sugar present for glucose. Furthermore, both DNS and Dygert methods showed increasing degree of overestimation of the amount of reducing sugar present with the increasing length of the malto-oligosaccharide sugar chains. The BCA assay can suitably quantify reducing sugars even in mixtures of oligosaccharides with different chain lengths. Thus, enzyme activities can be measured without bias towards higher values for enzymes that preferentially cleave the longer chain lengths.
    Matched MeSH terms: Quinolines
  9. Novel acyl hydrazide derivatives of polyhydroquinoline as potent anti-diabetic and anti-glycating agents: Synthesis, in vitro α-amylase, α-glucosidase inhibition and anti-glycating activity with molecular docking insights
    Ur Rahman S, Alam A, Parveen Z, Zainab, Assad M, Adnan Ali Shah S, et al.
    Bioorg Chem, 2024 Sep;150:107501.
    PMID: 38865858 DOI: 10.1016/j.bioorg.2024.107501
    In this study, eleven novel acyl hydrazides derivative of polyhydroquinoline were synthesized, characterized and screened for their in vitro anti-diabetic and anti-glycating activities. Seven compounds 2a, 2d, 2i, 2 h, 2j, 2f, and 2 g exhibited notable α-amylase inhibitory activity having IC50 values from 3.51 ± 2.13 to 11.92 ± 2.30 µM. Similarly, six compounds 2d, 2f, 2 h, 2i, 2j, and 2 g displayed potent α-glucosidase inhibitory activity compared to the standard acarbose. Moreover, eight derivatives 2d, 2 g, 2f, 2j, 2a, 2i, 2 g, and 2e showed excellent anti-glycating activity with IC50 values from 6.91 ± 2.66 to 15.80 ± 1.87 µM when compared them with the standard rutin (IC50 = 22.5 ± 0.90 µM). Molecular docking was carried out to predict the binding modes of all the compounds with α-amylase and α-glucosidase. The docking analysis revealed that most of the compounds established strong interactions with α-amylase and α-glucosidase. All compounds fitted well into the binding pockets of α-amylase and α-glucosidase. Among all compounds 2a and 2f were most potent based on docking score -8.2515 and -7.3949 against α-amylase and α-glucosidase respectively. These results hold promise for the development of novel candidates targeted at controlling postprandial glucose levels in individuals with diabetes.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/pharmacology; Quinolines/chemistry
  10. Click chemistry approach: regioselective one-pot synthesis of some new 8-trifluoromethylquinoline based 1,2,3-triazoles as potent antimicrobial agents
    Garudachari B, Isloor AM, Satyanarayana MN, Fun HK, Hegde G
    Eur J Med Chem, 2014 Mar 3;74:324-32.
    PMID: 24486415 DOI: 10.1016/j.ejmech.2014.01.008
    Three series of 8-trifluoromethylquinoline based 1,2,3-triazoles derivatives (5a-c, 6a-d and 7a-c) were synthesized by multi-step reactions by click chemistry approach. Synthesized compounds were characterized by spectral studies and X-ray analysis. The final compounds were screened for their in-vitro antimicrobial activity by well plate method (zone of inhibition). Compounds 5c, 6b, 8b, 11 and 12 were found to be active against tested microbial strains. The results are summarized in Tables 5 and 6.
    Matched MeSH terms: Quinolines/chemistry*
  11. Synthesis of quinoline derivatives as diabetic II inhibitors and molecular docking studies
    Taha M, Sultan S, Imran S, Rahim F, Zaman K, Wadood A, et al.
    Bioorg Med Chem, 2019 09 15;27(18):4081-4088.
    PMID: 31378594 DOI: 10.1016/j.bmc.2019.07.035
    In searchof the potenttherapeutic agent as an α-glucosidase inhibitor, we have synthesized twenty-five analogs (1-25) of quinoline-based Schiff bases as an inhibitoragainst α-glucosidase enzyme under positive control acarbose (IC50 = 38.45 ± 0.80 µM). From the activity profile it was foundthat analogs 1, 2, 3, 4, 11, 12 and 20with IC50values 12.40 ± 0.40, 9.40 ± 0.30, 14.10 ± 0.40, 6.20 ± 0.30, 14.40 ± 0.40, 7.40 ± 0.20 and 13.20 ± 0.40 µMrespectively showed most potent inhibition among the series even than standard drug acarbose (IC50 = 38.45 ± 0.80 µM). Here in the present study analog 4 (IC50 = 6.20 ± 0.30 µM) was found with many folds better α-glucosidase inhibitory activity than the reference drug. Eight analogs like 5, 7, 8, 16, 17, 22, 24 and 25 among the whole series displayed less than 50% inhibition. The substituents effects on phenyl ring thereby superficially established through SAR study. Binding interactions of analogs and the active site of ligands proteins were confirmed through molecular docking study. Spectroscopic techniques like 1H NMR, 13C NMR and ESIMS were used for characterization.
    Matched MeSH terms: Quinolines/chemical synthesis*
  12. Single dose kinetic study of the triple combination mefloquine/sulphadoxine/pyrimethamine (Fansimef) in healthy male volunteers
    Mansor SM, Navaratnam V, Mohamad M, Hussein S, Kumar A, Jamaludin A, et al.
    Br J Clin Pharmacol, 1989 Mar;27(3):381-6.
    PMID: 2785812
    A single dose pharmacokinetic study of a combined antimalarial formulation of mefloquine, sulphadoxine and pyrimethamine (Fansimef) has been performed in 10 healthy adult male Malaysian volunteers. The dose consisted of two tablets containing 250 mg mefloquine base, 500 mg sulphadoxine base and 25 mg pyrimethamine base each. Plasma concentrations of mefloquine and pyrimethamine were measured by GC-ECD, those of sulphadoxine by h.p.l.c. Time to peak concentrations (mean +/- s.d. for mefloquine (5.70 +/- 0.95 h), sulphadoxine (3.75 +/- 2.03 h) and pyrimethamine (3.30 +/- 1.98 h) were similar to those observed by others after administration of the single compounds. This was also true for elimination half-lives (t1/2). The t1/2s for mefloquine, sulphadoxine and pyrimethamine were 387 +/- 98 h, 255 +/- 61 h and 114 +/- 42 h, respectively.
    Matched MeSH terms: Quinolines/pharmacokinetics*
  13. The single dose treatment of falciparum malaria with nivaquine; a review of 164 cases treated at the District Hospital, Kuala Kangsar
    LAING AB
    Med J Malaya, 1955 Mar;9(3):216-21.
    PMID: 14393212
    Matched MeSH terms: Quinolines/therapeutic use*
  14. Synthesis of novel quinoline-based thiadiazole, evaluation of their antileishmanial potential and molecular docking studies
    Almandil NB, Taha M, Rahim F, Wadood A, Imran S, Alqahtani MA, et al.
    Bioorg Chem, 2019 04;85:109-116.
    PMID: 30605884 DOI: 10.1016/j.bioorg.2018.12.025
    New series of quinoline-based thiadiazole analogs (1-20) were synthesized, characterized by EI-MS, 1H NMR and 13C NMR. All synthesized compounds were subjected to their antileishmanial potential. Sixteen analogs 1-10, 12, 13, 16, 17, 18 and 19 with IC50 values in the range of 0.04 ± 0.01 to 5.60 ± 0.21 µM showed tremendously potent inhibition as compared to the standard pentamidine with IC50 value 7.02 ± 0.09 µM. Analogs 11, 14, 15 and 20 with IC50 8.20 ± 0.35, 9.20 ± 0.40, 7.20 ± 0.20 and 9.60 ± 0.40 µM respectively showed good inhibition when compared with the standard. Structure-activity relationships have been also established for all compounds. Molecular docking studies were performed to determine the binding interaction of the compounds with the active site target.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/metabolism; Quinolines/pharmacology*
  15. Synthesis, in vitro β-glucuronidase inhibitory potential and molecular docking studies of quinolines
    Bano B, Arshia, Khan KM, Kanwal, Fatima B, Taha M, et al.
    Eur J Med Chem, 2017 Oct 20;139:849-864.
    PMID: 28865280 DOI: 10.1016/j.ejmech.2017.08.052
    In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1-40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22-24 having IC50 values in the range of 1.60-8.40 μM showed superior activity than the standard saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Moreover, molecular docking studies of selected compounds were also performed to see interactions between active compounds and binding sites. Structures of all the synthetic compounds were confirmed through (1)H NMR, EI-MS and HREI-MS spectroscopic techniques.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/pharmacology*; Quinolines/chemistry
  16. Synthesis and study of the α-amylase inhibitory potential of thiadiazole quinoline derivatives
    Taha M, Tariq Javid M, Imran S, Selvaraj M, Chigurupati S, Ullah H, et al.
    Bioorg Chem, 2017 10;74:179-186.
    PMID: 28826047 DOI: 10.1016/j.bioorg.2017.08.003
    α-Amylase is a target for type-2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized thiadiazole quinoline analogs (1-30), characterized by different spectroscopic techniques such as 1HNMR and EI-MS and screened for α-amylase inhibitory potential. Thirteen analogs 1, 2, 3, 4, 5, 6, 22, 23, 25, 26, 27, 28 and 30 showed outstanding α-amylase inhibitory potential with IC50 values ranges between 0.002±0.60 and 42.31±0.17μM which is many folds better than standard acarbose having IC50 value 53.02±0.12μM. Eleven analogs 7, 9, 10, 11, 12, 14, 15, 17, 18, 19 and 24 showed good to moderate inhibitory potential while seven analogs 8, 13, 16, 20, 21 and 29 were found inactive. Our study identifies novel series of potent α-amylase inhibitors for further investigation. Structure activity relationship has been established.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/pharmacology*; Quinolines/chemistry
  17. Fulltext Prediction of Improved Antimalarial Chemoprevention with Weekly Dosing of Dihydroartemisinin-Piperaquine
    Permala J, Tarning J, Nosten F, White NJ, Karlsson MO, Bergstrand M
    Antimicrob Agents Chemother, 2017 May;61(5).
    PMID: 28242661 DOI: 10.1128/AAC.02491-16
    Intermittent preventive treatment (IPT) is used to reduce malaria morbidity and mortality, especially in vulnerable groups such as children and pregnant women. IPT with the fixed dose combination of piperaquine (PQ) and dihydroartemisinin (DHA) is being evaluated as a potential mass treatment to control and eliminate artemisinin-resistant falciparum malaria. This study explored alternative DHA-PQ adult dosing regimens compared to the monthly adult dosing regimen currently being studied in clinical trials. A time-to-event model describing the concentration-effect relationship of preventive DHA-PQ administration was used to explore the potential clinical efficacy of once-weekly adult dosing regimens. Loading dose strategies were evaluated and the advantage of weekly dosing regimen was tested against different degrees of adherence. Assuming perfect adherence, three tablets weekly dosing regimen scenarios maintained malaria incidence of 0.2 to 0.3% per year compared to 2.1 to 2.6% for all monthly dosing regimen scenarios and 52% for the placebo. The three tablets weekly dosing regimen was also more forgiving (i.e., less sensitive to poor adherence), resulting in a predicted ∼4% malaria incidence per year compared to ∼8% for dosing regimen of two tablets weekly and ∼10% for monthly regimens (assuming 60% adherence and 35% interindividual variability). These results suggest that weekly dosing of DHA-PQ for malaria chemoprevention would improve treatment outcomes compared to monthly administration by lowering the incidence of malaria infections, reducing safety concerns about high PQ peak plasma concentrations and being more forgiving. In addition, weekly dosing is expected to reduce the selection pressure for PQ resistance.
    Matched MeSH terms: Quinolines/administration & dosage; Quinolines/pharmacokinetics*; Quinolines/therapeutic use*
  18. Seco-tabersonine alkaloids from Tabernaemontana corymbosa
    Lim KH, Thomas NF, Abdullah Z, Kam TS
    Phytochemistry, 2009 Feb;70(3):424-9.
    PMID: 19217125 DOI: 10.1016/j.phytochem.2009.01.001
    Two seco-tabersonine alkaloids, jerantiphyllines A and B, in addition to a tabersonine hydroxyindolenine, jerantinine H, and a recently reported vincamine alkaloid 7, were isolated from the leaf extract of the Malayan Tabernaemontana corymbosa and the structures were established using NMR and MS analysis. Biomimetic conversion of jerantinines A and E to their respective vincamine and 16-epivincamine derivatives were also carried out.
    Matched MeSH terms: Quinolines/isolation & purification; Quinolines/chemistry*
  19. Efficacy and safety of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum malaria in endemic countries: meta-analysis of randomised controlled studies
    Naing C, Mak JW, Aung K, Wong JY
    Trans R Soc Trop Med Hyg, 2013 Feb;107(2):65-73.
    PMID: 23222952 DOI: 10.1093/trstmh/trs019
    The present review aimed to synthesise available evidence on the efficacy of dihydroartemisinin-piperaquine (DP) in treating uncomplicated Plasmodium falciparum malaria in people living in malaria-endemic countries by performing a meta-analysis of relevant studies. We searched relevant studies in electronic data bases up to December 2011. Published results from randomised controlled trials (RCTs) comparing efficacy of DP with other artemisinin-based combination therapies (ACTs), or non-ACTs, or placebo were selected. The primary endpoint was 28-day and 42-day treatment failure. We identified 26 RCTs. Many of the studies included in the present review were of high quality. Overall, DP, artesunate-mefloquine (MAS3) and artemether-lumefentrine (AL) were equally effective for reducing the risk of recurrent parasitaemia. The PCR confirmed efficacy of DP (99.5%) and MAS3 (97.7%) at day 28 exceeded 90%; both are efficacious. Comparable efficacy was also found for DP (95.6%) and AL (94.3%). The present review has documented that DP is comparable to other currently used ACTs such as MAS3 and AL in treating uncomplicated falciparum malaria. The better safety profile of DP and once-daily dosage improves adherence and its fixed co-formulation ensures that both drugs are taken together. Our conclusion is that DP has the potential to become a first-line antimalarial drug.
    Matched MeSH terms: Quinolines/adverse effects; Quinolines/therapeutic use*
  20. Current progress in antimalarial pharmacotherapy and multi-target drug discovery
    Tibon NS, Ng CH, Cheong SL
    Eur J Med Chem, 2020 Feb 15;188:111983.
    PMID: 31911292 DOI: 10.1016/j.ejmech.2019.111983
    Discovery and development of antimalarial drugs have long been dominated by single-target therapy. Continuous effort has been made to explore and identify different targets in malaria parasite crucial for the malaria treatment. The single-target drug therapy was initially successful, but it was later supplanted by combination therapy with multiple drugs to overcome drug resistance. Emergence of resistant strains even against the combination therapy has warranted a review of current antimalarial pharmacotherapy. This has led to the development of the new concept of covalent biotherapy, in which two or more pharmacophores are chemically bound to produce hybrid antimalarial drugs with multi-target functionalities. Herein, the review initially details the current pharmacotherapy for malaria as well as the conventional and novel targets of importance identified in the malaria parasite. Then, the rationale of multi-targeted therapy for malaria, approaches taken to develop the multi-target antimalarial hybrids, and the examples of hybrid molecules are comprehensively enumerated and discussed.
    Matched MeSH terms: Quinolines/pharmacology*; Quinolines/chemistry
Related Terms
Filters
Contact Us

Please provide feedback to Administrator ([email protected])

External Links