Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N -Diethyl-Substituted AmidoMoieties

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, andmass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl) pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethyl sulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL

Synthesis and Antibacterial Activity of N,N-Diethylamide Bearing Benzenesulfonamide Derivatives

Sulfonamides are known to represent a class of medicinally important compounds which are extensively used as antibacterial agents. Hence, a series of new N,N-diethyl amide bearing sulfonamides (2a-k) were synthesized via amidation of easily prepared benzenesulfonamide precursors (1a-k). The chemical structures of all synthesized compounds were substantiated using spectroscopic means such as IR, Mass spectra and 1H-NMR as well as analytical data. The antimicrobial activity of these compounds along with streptomycin, was investigated on Escherichia coli and Staphylococcus aureus. The results showed that this skeletal framework exhibited marked potency as antibacterial agents. The most active antibacterial agent against both targeted organisms was N,Ndiethyl-1-(phenylsulfonyl) piperidine-2-carboxamide (2b)

Antibacterial, Antifungal and Anti-tubercular Activities of Chloroform Fraction of the Leaf Extract of Irvingia Gabonensis (African Bush Mango)

The prevalence of anti-drug resistance by disease causing microorganisms has necessitated the search for alternative sources of drugs for the treatment of the ailments caused by these microorganisms. This study examines the biological properties of extracts from the leaves of Irvingia gabonensis (bush mango). Objective: The objective of this study is to determine the anti-microbial activity of chloroform fraction of the leaf extract and compare it with that of clinical reference. Method: Antimicrobial activity of the chloroform fraction of the leaf extract of Irvingia gabonensis was evaluated against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Shigella dysenteriae, Salmonella typhi, Klebsiella pneumonia, Salmonella paratyphi, Candida albicans and Trichophyton rubrum by using the agar well diffusion method and Mycobacterium tuberculosis using agar proportion method on Lowenstein–Jensen medium. Preliminary phytochemical screening of the chloroform leaf fraction was done using qualitative standard methods. Result: This showed the presence of saponins, flavonoids, tannins, coumarin, phenol and alkaloids. Organisms were susceptible to chloroform fraction at different concentrations. The lowest MIC value obtained was 0.625mg/mL for S. aureus and S. typhi. While, five out of seven mycobacterial strains that were used, were susceptible. Conclusion: The antimicrobial activity is a result of the phytochemicals present in leaf. Therefore, we conclude that Irvingia gabonensis leaves can be used in the development of new pharmaceuticals research activities such as drug productio

Send Orders of Reprints at [email protected] The Open Organic Chemistry Journal

Abstract: An highly expeditious synthetic approach for the synthesis of benzenemethanesulfonamides (1a-k) and their new corresponding N,N-diethyl substituted amido moieties (2a-k) has been achieved in aqueous medium at room temperature. The reaction condition was thoroughly optimized thereby allowing significant rate enhancement and resulting into excellent yields. The chemical structures of the successful candidates were confirmed using elemental analytical and spectroscopic data such as IR, 1 H NMR, 13 C NMR and some selected mass spectral data. Graphical Abstract Environmental friendly synthesis of new N,N-diethyl-substituted-2-(phenylmethylsulfo namido)alkanamide derivatives was achieved in aqueous medium via synthetic modification of the benzenemethanesulfonamide precursors

IN-VITRO ANTIBACTERIAL, PHYTOCHEMICAL, ANTIMYCOBACTERIAL ACTIVITIES AND GC-MS ANALYSES OF Bidens pilosa LEAF EXTRACT.

The phytochemical constituents, antimicrobial activity, anti-mycobacterial activity and gas chromatography-mass spectrometry (GCMS) analysis of the West African ecotype of Bidens pilosa was investigated for possible medicinal properties. The antimicrobial activity of the hexane, dichloromethane, ethyl acetate and methanol extracts from the leaf of Bidens pilosa was evaluated using agar dilution method. The qualitative and quantitative phytochemical screening was carried out according to standard procedures. Partitioned fractions of the methanolic extract was subjected to anti-mycobacterial bioassay. Different fractions of the leaf were subjected to GCMS to ascertain the compounds present. The antimicrobial analysis revealed the methanolic fraction as having the highest number of activity against test organisms such as: Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Candida albicans and Rhizopus sp. between 10 - 40 mm. The minimum inhibitory concentration showed the methanolic fraction to be active against Candida albicans and Rhizopus sp. at the concentration of 6.25 g/ml and 3.25 g/ml respectively. The phytochemical screening revealed the presence of alkaloids, cardiac glycosides and terpenoids in all the solvents. Tannin was present in all the solvent fractions except hexane fraction. Saponin was not found in any of the solvents. The hexane-methanol interface of the partitioned solvents was sensitive to the anti-mycobacterial activity while other solvents showed resistance. The GC-MS and the chromatogram gave insight into the volatile components of the leaf extract. The findings reveals Bidens pilosa as a medicinal plant with potentials for the treatment of tuberculosis. • Copyright of Journal of Microbiology, Biotechnology & Food Sciences is the property of Slovak University of Agriculture in Nitra, Faculty of Biotechnology & Food Sciences and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract

Phytochemical Screening and Antimicrobial Studies of Stem and Root Extracts of Crateva adansonii

Aim: This study was designed to explore the phytochemical and antimicrobial screening of the stem and root extracts of Crateva adansonii. Place and Duration of Study: Sample: Iyesi village, Ota, Ogun State, and analysis carried out at Department of Chemistry and Department of Biological Sciences, Covenant University, Ota, Ogun State and for duration of three months (November 2016 to February 2017). Methodology: Standard universal procedures were employed for both phytochemical and antimicrobial analysis. Results: The result obtained from the stem and root extracts of Crateva adansonii indicated the presence of flavonoids, terpenoids, alkaloids, and cardiac glycosides. Root extract was found to be richer in source of phytochemicals when compared to the stem extract. However, the highest antibacterial activity was observed against selected bacteria by both stem and root extracts. The potency of the root extract was observed to be higher than the stem extract against Bacillus cereus, Staphylococcus aureus, Aspergillus niger and Serratia spp. Conclusion: The preliminary studies on the stem and the root of Crateva adansonii extracts revealed their antimicrobial potential which could be further investigated for global utilization in pharmaceutical treatment, natural therapies, food preservation and cosmetic applications

Phytochemical Screening and Antimicrobial Studies of Crateva adansonii Leaf Extract

Diverse challenges of microbial infections and upsurge of multi-drug resistant microbes informed the investigation into the phytochemical and antibacterial properties of Crateva adansonii. Cold extraction was carried out using methanol solvent. The crude extract of Crateva adansonii was fractionated into the n-hexane, methanol and chloroform layers successively. The phytochemical screening indicated the presence of alkaloids, saponins, terpenoids, flavonoids and cardiac glycosides. The antimicrobial assay showed that, for Bacillus spp, the organism was sensitive to the chloroform fraction of leaf extract at 1.562 mg/ml. For Microccocus varians, result showed organism was sensitive to the crude extract at 3.125 mg/ml. According to the result of antifungal screening, the n-hexane fraction and crude extract showed activity against Aspergillus niger at 12.500 mg/ml and 3.125 mg/ml respectively. From these results, the crude extract of the leaf of Crateva adansonii shows activity against both bacteria and Fungi; hence, it may might be a good source of new drug for treating infections caused by these pathogen

Antimicrobial and GC-MS Analyses of Stem and Root Extracts of Bidens Pilosa Linn

This study describes the qualitative phytochemical screening, antimicrobial and GC-MS analyses of the crude methanol extract of the stem and roots parts of Bidens pilosa partitioned between methanol, dichloromethane, ethyl acetate and hexane solvents. Phytochemical analysis indicated the presence of cardiac glycosides, terpenoids, flavonoids and alkaloids. Saponins were not found in any of the fractions of stem and root of B. pilosa. Antibacterial studies indicated that the lowest concentration (6.25 mg/mL) was achieved for Candida subtilis for the ethyl acetate fraction of the stem extract and hexane fraction of the root extract. Antimycobacterial test activity of these solvent fractions revealed that the hexane fraction of the root extract was susceptible to the bacterium isolate. Gas chromatography-Mass spectrometric study revealed the presence of the following compounds-cis-9-Hexadecenal, 2-hydroxyl ethyl (Z)-9-Octadecenoate, Octadecanal, Oleic acid, 4-(dimethylamino)-Benzaldehyde, 4,6,7-Trimethoxy-2,3-dihydrofuro(2,3-b)quinolon

Anti-mycobacterial and GC-MS Studies of Irvingia gabonensis Baill Ex. Lanen Stem Extracts

Irvingia gabonensis baill ex. lanen (Bush mango) is an ethno-medicinal plant that has been used for traditional therapeutic purposes. With the increasing rate of drug resistance to various diseases in the society today, there is the need for alternative sources of drugs for the treatment of such disease. The Bush mango plant presents a potential candidate for such drugs discovery. Extracts from the plant stem were derived by cold maceration separately in methanol (MeOH) and Dichloromethane (DCM) for a period of 7 days. Phyto-constituents were also identified in extracts of stems by using hyphenated mass spectrometer and chromatographic technique, the Gas Chromatography - Mass Spectrometer (GC/MS) while the functional group of such phyto-constituents were identified with the aid of Nicolet 5700 Fourier Transform– Infra-Red spectrometer. Anti-tubercular screening was performed on extracts against clinically isolated drug-susceptible strains (DS-MTB-1 - DS-MTB-5), drug resistant strains (DR-MTB-1, DR-MTB-2) and a standard tubercular strain, H37Rv. This was controlled with drug standards, rifampicin and levofloxacin. Extracts revealed the presence of phyto-constituents such as saponins, tannin, alkaloids and phenol. It was observed that both extracts recorded high % alkaloid content at 10.37±0.02. Also, identified by FTIR as the principal part of the extracts are hydrocarbon groups such as carboxylic acid (1042), while the presence of the volatile components such as 9- Oxabicyclo [6.1.0] nonane (C8H14O) and 1-Chlorobutatriene (C4H3C) were reported by GC-MS. Extracts exhibited significant anti-tubercular activity against all organisms. Therefore, this study promotes the use of Irvingia gabonensis baill ex. lanen for phytotherapeutics purposes

Pinus glabra: As a Potential Source of Anti- Mycobacterium tuberculosis Agent: Phytochemical and antimicrobial Studies of its Stem Extracts

With the increasing incidence of tuberculosis and rated second to HIV-AIDS by the World Health Organisation as a leading cause of death from infectious disease and increased resistance to drugs currently in use, there is therefore the need for alternative sources of drugs for the treatment of this disease. Pinus glabra presents as a potential candidate for such drugs discovery. Concoctions derived from the plant have been used to treat cases of rheumatism, cough, piles and catarrh. Sample extraction was performed by soaking the stem samples in ethanol for 172 h, which gave reddish-yellow oil after removal of the ethanol solvent. The oil was partitioned between 1:1 water/chloroform mixture. The aqueous layer was further partitioned separately with ethyl acetate and hexane. The phytochemical screening of the crude ethanol extract revealed the presence of alkaloids, saponins, tannins and flavonoids. Antimicrobial tests were performed on the crude ethanol extract, ethyl acetate and hexane fractions against clinical isolates Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Klebsiella sp. by measurement of zones of inhibition. All test samples exhibited significant antimicrobial activity against the organisms albeit to different extent