scholarly journals Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N-Diethyl-Substituted Amido Moieties

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Olayinka O. Ajani ◽  
Oluwole B. Familoni ◽  
Feipeng Wu ◽  
Johnbull O. Echeme ◽  
Zheng Sujiang
Keyword(s):  
Antibacterial Activity ◽  
Mass Spectra ◽  
Room Temperature ◽  
Biological Activities ◽  
Chemical Structures ◽  
Wide Range ◽  
Synthetic Routes ◽  
Mic Value ◽  
C Nmr

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, and mass 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-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

scholarly journals Nigritanine as a New Potential Antimicrobial Alkaloid for the Treatment of Staphylococcus aureus-Induced Infections

Toxins ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 511 ◽  
Author(s):  
Bruno Casciaro ◽  
Andrea Calcaterra ◽  
Floriana Cappiello ◽  
Mattia Mori ◽  
Maria Loffredo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activities ◽  
Human Keratinocytes ◽  
Chemical Diversity ◽  
Bioactive Molecules ◽  
Bacterial Strains ◽  
Wide Range

Staphylococcus aureus is a major human pathogen causing a wide range of nosocomial infections including pulmonary, urinary, and skin infections. Notably, the emergence of bacterial strains resistant to conventional antibiotics has prompted researchers to find new compounds capable of killing these pathogens. Nature is undoubtedly an invaluable source of bioactive molecules characterized by an ample chemical diversity. They can act as unique platform providing new scaffolds for further chemical modifications in order to obtain compounds with optimized biological activity. A class of natural compounds with a variety of biological activities is represented by alkaloids, important secondary metabolites produced by a large number of organisms including bacteria, fungi, plants, and animals. In this work, starting from the screening of 39 alkaloids retrieved from a unique in-house library, we identified a heterodimer β-carboline alkaloid, nigritanine, with a potent anti-Staphylococcus action. Nigritanine, isolated from Strychnos nigritana, was characterized for its antimicrobial activity against a reference and three clinical isolates of S. aureus. Its potential cytotoxicity was also evaluated at short and long term against mammalian red blood cells and human keratinocytes, respectively. Nigritanine showed a remarkable antimicrobial activity (minimum inhibitory concentration of 128 µM) without being toxic in vitro to both tested cells. The analysis of the antibacterial activity related to the nigritanine scaffold furnished new insights in the structure–activity relationships (SARs) of β-carboline, confirming that dimerization improves its antibacterial activity. Taking into account these interesting results, nigritanine can be considered as a promising candidate for the development of new antimicrobial molecules for the treatment of S. aureus-induced infections.

scholarly journals Isolation and Antibacterial Activity of Indole Alkaloids from Pseudomonas aeruginosa UWI-1

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3744
Author(s):  
Antonio Ramkissoon ◽  
Mohindra Seepersaud ◽  
Anderson Maxwell ◽  
Jayaraj Jayaraman ◽  
Adesh Ramsubhag
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
High Resolution Mass Spectrometry ◽  
Indole Alkaloid ◽  
Antimicrobial Activities ◽  
Mass Spectrometry Data ◽  
Gram Positive ◽  
Chemical Structures ◽  
Wide Range

In this study, we report the first isolation of three antibiotic indole alkaloid compounds from a Pseudomonad bacterium, Pseudomonas aeruginosa UWI-1. The bacterium was batch fermented in a modified Luria Broth medium and compounds were solvent extracted and isolated by bioassay-guided fractionation. The three compounds were identified as (1) tris(1H-indol-3-yl) methylium, (2) bis(indol-3-yl) phenylmethane, and (3) indolo (2, 1b) quinazoline-6, 12 dione. A combination of 1D and 2D NMR, high-resolution mass spectrometry data and comparison from related data from the literature was used to determine the chemical structures of the compounds. Compounds 1–3 were evaluated in vitro for their antimicrobial activities against a wide range of microorganisms using the broth microdilution technique. Compounds 1 and 2 displayed antibacterial activity against only Gram-positive pathogens, although 1 had significantly lower minimum inhibitory concentration (MIC) values than 2. Compound 3 displayed potent broad-spectrum antimicrobial activity against a range of Gram positive and negative bacteria. Several genes identified from the genome of P. aeruginosa UWI-1 were postulated to contribute to the biosynthesis of these compounds and we attempted to outline a possible route for bacterial synthesis. This study demonstrated the extended metabolic capability of Pseudomonas aeruginosa in synthesizing new chemotypes of bioactive compounds.

scholarly journals Antiparasitic effects of selected isoflavones on flatworms

2021 ◽  
Vol 58 (1) ◽  
pp. 1-16
Author(s):  
D. Faixová ◽  
G. Hrčková ◽  
T. Mačák Kubašková ◽  
D. Mudroňová
Keyword(s):  
Secondary Metabolites ◽  
Biological Activities ◽  
Plant Secondary Metabolites ◽  
Therapeutic Effects ◽  
Dependent Manner ◽  
Biologically Relevant ◽  
Chemical Structures ◽  
Antiparasitic Drug ◽  
Wide Range

SummaryMedicinal plants have been successfully used in the ethno medicine for a wide range of diseases since ancient times. The research on natural products has allowed the discovery of biologically relevant compounds inspired by plant secondary metabolites, what contributed to the development of many chemotherapeutic drugs. Flavonoids represent a group of therapeutically very effective plant secondary metabolites and selected molecules were shown to exert also antiparasitic activity. This work summarizes the recent knowledge generated within past three decades about potential parasitocidal activities of several flavonoids with different chemical structures, particularly on medically important flatworms such as Schistosoma spp., Fasciola spp., Echinococcus spp., Raillietina spp., and model cestode Mesocestoides vogae. Here we focus on curcumin, genistein, quercetin and silymarin complex of flavonolignans. All of them possess a whole spectrum of biological activities on eukaryotic cells which have multi-therapeutic effects in various diseases. In vitro they can induce profound alterations in the tegumental architecture and its functions as well as their activity can significantly modulate or damage worm´s metabolism directly by interaction with enzymes or signaling molecules in dose-dependent manner. Moreover, they seem to differentially regulate the RNA activity in numbers of worm´s genes. This review suggests that examined flavonoids and their derivates are promising molecules for antiparasitic drug research. Due to lack of toxicity, isoflavons could be used directly for therapy, or as adjuvant therapy for diseases caused by medically important cestodes and trematodes.

Synthesis and SAR Evaluation of Mercapto Triazolobenzothiazole

2021 ◽  
Vol 18 (4) ◽  
pp. 362-374
Author(s):  
Mamatha S.V ◽  
S.L. Belagali ◽  
Mahesh Bhat
Keyword(s):  
Antibacterial Activity ◽  
Biological Activities ◽  
Antibacterial Activities ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Step Method ◽  
Good Antibacterial Activity ◽  
Anti Inflammatory ◽  
Mic Value

Background: Benzothiazoles possess a vast sphere of biological activities including anti- inflammatory, antibacterial activities whereas triazoles display various pharmacological properties including antimicrobial and antitubercular activities. Hence, triazole conjugated benzothiazole side-chain anticipating their interesting biological properties has been focused upon. Objective: The objective of the current work is synthesis and biological evaluation of a new series of benzothiazole appended triazole derivatives. Methods: The target compounds were prepared via a multi-step method involving the treatment of 2-amino benzothiazole with hydrazine followed by cyclization with carbon disulfide to give the corresponding triazol-2-thiol derivatives and then alkylation of these derivatives. All the synthesized compounds were characterized by FT-IR, Mass, 1H and 13C NMR spectra and were screened for their antibacterial, antioxidant, anti-inflammatory and anti-tubercular (anti-TB) activities in vitro. These molecules were also docked into the enoyl acyl carrier reductase (Inha, PDB ID-1ZID) in silico. Results: While all the synthesized compounds were active against M. tuberculosis at 50 μg/ml, the pyrrolidine and piperidine appended benzothiazolyltriazoles showed the superior activity (MIC values 12.5 to 1.6 μg/ml). Compound 5a (5-CH3 with piperidine), 5b (7-CH3 with piperidine) and 7b (7-CH3 with pyrrolidine) showed good antibacterial activity against Staphylococcus aureus with MIC value 31.25μg/ml, while compounds 7a (5-CH3 with pyrrolidine), 6b (7-CH3 with morpholine) and 8c (7-Br with pyridine) exhibited good antibacterial activity against E-coli with MIC value 62.5μg/ml. Compounds 7b (7-CH3 with pyrrolidine) and 5c (7-Br with piperidine) showed good anti-oxidant activities with IC50 values 93.25 and 82.25, respectively. Notably, these compounds were non-toxic to the normal cells even at high concentrations with IC50 value 238μg/ml. Conclusion: The compound 7b, a benzothiazolyltriazole having a pyrrolidine group (five membered ring) attached to two CH2 groups and methyl substituent at 7th position of the benzothiazole ring emerged as a novel and promising hit molecule that showed anti-TB, antimicrobial and antiinflammatory activities in vitro.

scholarly journals Synthesis, Antimicrobial, and Anti-HIV1 Activity of Quinazoline-4(3H)-one Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
K. Vijayakumar ◽  
A. Jafar Ahamed ◽  
G. Thiruneelakandan
Keyword(s):  
Elemental Analysis ◽  
Mass Spectra ◽  
Product Yields ◽  
H Nmr ◽  
Wide Range ◽  
Quinazolinone Derivatives ◽  
C Nmr

The present investigation aims to synthesize 11 compounds of quinazoline-1 derivatives and to test their antimicrobial and anti-HIV1 activities. A quick-witted method was developed for the synthesis of novel substituted quinazolinone derivatives by summarizing diverse diamines with benzoxazine reactions, and it demonstrated the benefits of typical reactions, handy operation, and outstanding product yields. These compounds were confirmed by elemental analysis, I R, 1H NMR, 13C NMR, and mass spectra. Then antimicrobial and anti-HIV1 activities of the compounds were tested in-vitro. It was found that compounds 7–11 possessed a wide range of anti microbial and anti-HIV1 activity.

Evaluation of 99mTc-Label led Vitamin K4 as an Agent for Testicular Imaging

1991 ◽  
Vol 30 (01) ◽  
pp. 35-39 ◽  
Author(s):  
H. S. Durak ◽  
M. Kitapgi ◽  
B. E. Caner ◽  
R. Senekowitsch ◽  
M. T. Ercan
Keyword(s):  
Soft Tissue ◽  
Room Temperature ◽  
Normal Subjects ◽  
Left Testis ◽  
Wide Range ◽  
Activity Ratios ◽  
The Right ◽  
Radioactivity Levels

Vitamin K4 was labelled with 99mTc with an efficiency higher than 97%. The compound was stable up to 24 h at room temperature, and its biodistribution in NMRI mice indicated its in vivo stability. Blood radioactivity levels were high over a wide range. 10% of the injected activity remained in blood after 24 h. Excretion was mostly via kidneys. Only the liver and kidneys concentrated appreciable amounts of radioactivity. Testis/soft tissue ratios were 1.4 and 1.57 at 6 and 24 h, respectively. Testis/blood ratios were lower than 1. In vitro studies with mouse blood indicated that 33.9 ±9.6% of the radioactivity was associated with RBCs; it was washed out almost completely with saline. Protein binding was 28.7 ±6.3% as determined by TCA precipitation. Blood clearance of 99mTc-l<4 in normal subjects showed a slow decrease of radioactivity, reaching a plateau after 16 h at 20% of the injected activity. In scintigraphic images in men the testes could be well visualized. The right/left testis ratio was 1.08 ±0.13. Testis/soft tissue and testis/blood activity ratios were highest at 3 h. These ratios were higher than those obtained with pertechnetate at 20 min post injection.99mTc-l<4 appears to be a promising radiopharmaceutical for the scintigraphic visualization of testes.

1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance

2019 ◽  
Vol 16 (5) ◽  
pp. 709-729 ◽  
Author(s):  
Muhammad A. Rashid ◽  
Aisha Ashraf ◽  
Sahibzada S. Rehman ◽  
Shaukat A. Shahid ◽  
Adeel Mahmood ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Significance ◽  
Biological Evaluation ◽  
Wide Range ◽  
Pharmaceutical Industries ◽  
Biological Aspects ◽  
Synthetic Routes ◽  
Biological Attributes ◽  
Synthesis Reactions ◽  
Potential Use

Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies

2020 ◽  
Vol 16 ◽  
Author(s):  
Mahboob Ali ◽  
Momin Khan ◽  
Khair Zaman ◽  
Abdul Wadood ◽  
Maryam Iqbal ◽  
...  
Keyword(s):  
In Silico ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Type Ii Diabetes Mellitus ◽  
Spectroscopic Techniques ◽  
Chalcone Derivatives ◽  
In Silico Studies ◽  
Wide Range

: Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biological activities. Objective: In the current study chalcone derivatives (1-17) were synthesized and evaluated their inhibitory potential against α-amylase enzyme. Method: For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by ClaisenSchmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via different spectroscopic techniques such as EI-MS, HREI-MS, 1H-, and 13C-NMR. Results: Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard commercial drug acarbose (IC50 = 1.34 ± 0.3 μM). Conclusion: Chalcone derivatives (1-17) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed that electron donating groups in the phenyl ring have more influence on enzyme inhibition. However, to insight the participation of different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) molecular modeling analyses were carried out.

Associated microflora of medicinal ferns: biotechnological potentials and possible applications

2016 ◽  
Vol 5 (03) ◽  
pp. 4927 ◽  
Author(s):  
Shubhi Srivastava ◽  
Paul A. K.
Keyword(s):  
Secondary Metabolites ◽  
Growth Promotion ◽  
Biological Activities ◽  
Hydrolytic Enzymes ◽  
In Vitro Production ◽  
Wide Range ◽  
Negative Effect ◽  
Bacteria And Fungi

Plant associated microorganisms that colonize the upper and internal tissues of roots, stems, leaves and flowers of healthy plants without causing any visible harmful or negative effect on their host. Diversity of microbes have been extensively studied in a wide variety of vascular plants and shown to promote plant establishment, growth and development and impart resistance against pathogenic infections. Ferns and their associated microbes have also attracted the attention of the scientific communities as sources of novel bioactive secondary metabolites. The ferns and fern alleles, which are well adapted to diverse environmental conditions, produce various secondary metabolites such as flavonoids, steroids, alkaloids, phenols, triterpenoid compounds, variety of amino acids and fatty acids along with some unique metabolites as adaptive features and are traditionally used for human health and medicine. In this review attention has been focused to prepare a comprehensive account of ethnomedicinal properties of some common ferns and fern alleles. Association of bacteria and fungi in the rhizosphere, phyllosphere and endosphere of these medicinally important ferns and their interaction with the host plant has been emphasized keeping in view their possible biotechnological potentials and applications. The processes of host-microbe interaction leading to establishment and colonization of endophytes are less-well characterized in comparison to rhizospheric and phyllospheric microflora. However, the endophytes are possessing same characteristics as rhizospheric and phyllospheric to stimulate the in vivo synthesis as well as in vitro production of secondary metabolites with a wide range of biological activities such as plant growth promotion by production of phytohormones, siderophores, fixation of nitrogen, and phosphate solubilization. Synthesis of pharmaceutically important products such as anticancer compounds, antioxidants, antimicrobials, antiviral substances and hydrolytic enzymes could be some of the promising areas of research and commercial exploitation.

scholarly journals Beehive Products as Antibacterial Agents: A Review

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Antibacterial Agents ◽  
Royal Jelly ◽  
Biological Activities ◽  
Vital Role ◽  
Bee Venom ◽  
Bacterial Strains ◽  
Wide Range ◽  
Life Threatening

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.

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