Interlending & Document Supply, 2001 to 2010: A bibliometric study

The study intends to evaluate journal of Interlending & Document Supply (ILDS) from 2001 to 2010 using different bibliometric indicators and to find out various dimensions of publication trends of this journal. In accordance with the objectives of the study, the bibliographic citations appended at the end of each article were copied and stored in a separate MS-Word file. The details with regard to each published article such as type of papers, number of articles in each issue of the journal, number of references and their forms in each article, number of pages, number of authors, and the name of journals, etc. were recorded and analyzed. The study applied Lotka's law to assess authorship productivity pattern, and Bradford's law to ascertain the scattering of journals. In analyzing 315 scholarly articles published in ILDS for a period of 10 years ranging from 2001 to 2010, the study reveals that the highest numbers of articles are found to be single authored contributions, followed by two-authored contributions. The authorship productivity pattern partially complies with Lotka's Law. In regard to country productivity, UK leads the table, followed by USA, and France. Moreover, ILDS authors are found to have fairly cited recent literature in their papers which is evident from the half life period of documents. Furthermore, the study concludes that ILDS can enrich its standard if it can fine tune its editorial policy

Interlending & Document Supply: A bibliometric study from 2001 to 2010

The study intends to evaluate journal of Interlending & Document Supply (ILDS) from 2001 to 2010 using different bibliometric indicators and to find out various dimensions of publication trends of this journal. In accordance with the objectives of the study, the bibliographic citations appended at the end of each article were copied and stored in a separate MS-Word file. The details with regard to each published article such as type of papers, number of articles in each issue of the journal, number of references and their forms in each article, number of pages, number of authors, and the name of journals, etc. were recorded and analyzed. The study applied Lotka's law to assess authorship productivity pattern, and Bradford's law to ascertain the scattering of journals. In analyzing 315 scholarly articles published in ILDS for a period of 10 years ranging from 2001 to 2010, the study reveals that the highest numbers of articles are found to be single authored contributions, followed by two-authored contributions. The authorship productivity pattern partially complies with Lotka's Law. In regard to country productivity, UK leads the table, followed by USA, and France. Moreover, ILDS authors are found to have fairly cited recent literature in their papers which is evident from the half life period of documents. Furthermore, the study concludes that ILDS can enrich its standard if it can fine tune its editorial policy

Computational attempts for synthesis of potent antibacterial sulfamethoxazole-monocyclic terpenes conjugates

To develop 6 conjugate agents of the moribund antibiotic sulfamethoxazole (SMZ) joined to 6 individual monoterpenes, followed by protocols of medicinal chemistry as potent antibacterials, against multidrug resistant (MDR) human gruesome pathogenic bacteria. Antibacterial activities of the proposed conjugates were ascertained by the ‘prediction of activity spectra of substances’ (PASS) program. Drug-likeness parameters and toxicity profiles of conjugates were standardized with the Lipinski rule of five, using cheminformatic tools, Molsoft, molinspiration, OSIRIS and ProTox. Antibacterial activities of individual chemicals and conjugates were examined by targeting the bacterial folic acid biosynthesis enzyme, dihydropteroate synthases (DHPSs) of bacteria, Bacillus anthracis, Escherichia coli, Staphylococcus aureus, Streptococcus pneumoniae and Mycobacterium tuberculosis, with 3D structures of DHPSs from protein data bank. According to the PASS program, biological spectral values of conjugate-2, conjugate-5 and conjugate-6 were ascertained effective with ‘probably active’ or ‘Pa’ value > 0.5, for anti-infective and an- tuberculosic activities. Using molecular docking against 5 cited bacterial DHPSs, effective docking scores of 6 monoterpenes in the specified decreasing order (kcal/mol): −9.72 (eugenol against B. anthracis), −9.61 (eugenol against S. pneumoniae), −9. 42 (safrol, against B. anthracis), −9.39 (thymol, against M. tuberculosis), −9.34 (myristicin, against S. pneumoniae) and −9.29 (thymol, against B. anthracis); whereas the lowest docking score of SMZ was -8.46 kcal/mol against S. aureus DHPS. Similarly, effective docking scores of conjugates were as specified (kcal/mol.): −10.80 (conjugate-4 consisting SMZ + safrol, against M. tuberculosis), −10.78 (conjugate-5 consisting SMZ + thymol, against M. tuberculosis), −10.60 (conjugate- 5 against B. anthracis), −10.26 (conjugate-2 consisting SMZ + eugenol, against M. tuberculosis), −10.25 (conjugate-5, against S. aureus) and −10.19 (conjugate-2 against S. pneumoniae. Conjugates-2 and -5 were the most effective antibacterials based on Lipinski rule of five with lethal doses 3471 and 3500 mg/kg, respectively and toxicity class levels. Conjugate-2 and conjugate-5 were more effective than individual monoterpenes and SMZ, against pathogenic bacteria. Synthesis, characterization and in vitro antibacterial study with acute toxicity testing for Wister rat model of the conjugate-5 could land at success in the recorded computational trial and it could be promoted for synthesis in the control of MDR bacteria

Nano-technology platforms to increase the antibacterial drug suitability of essential oils: A drug prospective assessment

A huge number of plant-derived essential oils (EOs) are reported to have lots of ethnomedicinal and biological properties with excellent antibacterial activities. Approximately three hundred EOs (ajowan, anise, basil, camphor, chamomile, clove, citronella, coriander, cumin, eucalyptus, lavender, lemon, orange, peppermint, thyme oils, etc.) are documented under economic class based on commercial and pharmaceutical values. However, most active crude EOs and their constituents like carvacrol, eugenol, geraniol, linalool, thymol, 1,8-cineole, etc. are not found in mainstream drug development modules due to their low solubility, poor bioavailability, and rapid volatility profiles, which reduce their potency, half-life, and pharmacokinetics to achieve the ideal drug-ability profiles. To improve the mainstream use of EOs via nanotechnology, we first gathered more information on plant sources, extraction methods, antibacterial potency with mode of action, and the economic importance of EOs. Further, various nanotechnology platforms, such as nanocarriers, nanoemulsions, liposomes, and cyclodextrins with chemical structure conjugation concept with relevant examples were described. Technically, through optimization in particle size and morphology via a nanotechnology platform, EOs enhance the potency without losing any sensitive properties, easily penetrate and cross the bacterial cell membrane, protect from rapid volatility by coating biocompatible materials, improve the aqueous solubility, improve bioavailability, ensure sustainable release, etc. We hope that the detailed analyses of EOs and nanotechnology platforms will encourage academic and pharmaceutical researchers to use antibacterials by overcoming inadequate drug-ability profiles as potent agents in drugs, food, nutrition, beverages, packaging, and coating materials

Synthesis of novel thymol derivatives against MRSA and ESBL producing pathogenic bacteria

<p>Twelve substituted aryl-azo-thymol derivatives (<b>4a</b> to <b>4 l</b>) were synthesized and characterized by several spectral techniques such as, FTIR, UV-vis, proton NMR, Mass spectrometry and elemental analysis. Antimicrobial activities were evaluated by agar-well diffusion method against isolated MRSA, ESBL-producing pathogenic bacteria and antifungal resistant fungi, <i>in vitro</i>. In addition, drug likeness properties of derivatives were assessed through bioinformatic tools such as, PASS prediction, molecular docking and Lipinski rules of five, along with determination of toxic nature and LD₅₀ values. Among 12 derivatives, <b>4a</b>, <b>4b</b>, <b>4c</b>, <b>4 g, 4i, 4j</b> and <b>4 k</b> had significant antibacterial and antifungal activities with minimum inhibitory concentration values, 40 to 80 μg/ml. Moreover, the docking scores of derivatives were −8.27 to −11.44 kcal/mol, against 4 bacterial targets and −9.45 to −12.49 kcal/mol against 2 fungal targets. Thus, from <i>in vitro</i> and <i>in silico</i> studies, thymol derivatives had control of MRSA, ESBL-producing bacteria and antifungal resistant fungi.</p

Computer-aided synthesis of dapsone-phytochemical conjugates against dapsone-resistant Mycobacterium leprae

Abstract: Leprosy continues to be the belligerent public health hazard for the causation of high disability and eventual morbidity cases with stable prevalence rates, even with treatment by the on-going multidrug therapy (MDT). Today, dapsone (DDS) resistance has led to fear of leprosy in more unfortunate people of certain developing countries. Herein, DDS was chemically conjugated with five phytochemicals independently as dapsone-phytochemical conjugates (DPCs) based on azo-coupling reaction. Possible biological activities were verified with computational chemistry and quantum mechanics by molecular dynamics simulation program before chemical synthesis and spectral characterizations viz., proton-HNMR, FTIR, UV and LC-MS. The in vivo antileprosy activity was monitored using the ‘mouse-foot-pad propagation method’, with WHO recommended concentration 0.01% mg/kg each DPC for 12 weeks, and the host-toxicity testing of the active DPC4 was seen in cultured-human-lymphocytes in vitro. One-log bacilli cells in DDS-resistant infected mice footpads decreased by the DPC4, and no bacilli were found in the DDS-sensitive mice hind pads. Additionally, the in vitro host toxicity study also confirmed that the DCP4 up to 5,000 mg/L level was safety for oral administration, since a minor number of dead cells were found in red color under a fluorescent microscope. Several advanced bioinformatics tools could help locate the potential chemical entity, thereby reducing the time and resources required for in vitro and in vitro tests. DPC4 could be used in place of DDS in MDT, evidenced from in vivo antileprosy activity and in vitro host toxicity study