Design, Development and Evaluation of N-Mannich Base Prodrugs of Norfloxacin For In Vitro Release Behavior and Antimicrobial Properties

2017 ◽  
Vol 7 (2) ◽  
Author(s):  
Sharma Chander ◽  
Piplani Mona
Keyword(s):  
Antibacterial Activity ◽  
Parent Compound ◽  
Research Work ◽  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Physical Analysis ◽  
Design Development ◽  
Standard Drug ◽  
E Coli

In this research work, prodrugs of norfloxacin with various benzothiazoles were synthesized and studied for hydrolytic studies at various physiological pH. The results indicated that all of the prodrugs exhibited more and faster hydrolysis mainly in phosphate buffer (pH 7.4) rather than in HCl buffer (pH 1.2). These prodrugs were characterized by FTIR, 1H NMR, mass spectroscopy and physical analysis. The synthesized prodrugs showed better partition coefficient as compared to parent compound, norfloxacin. All of the prodrugs were tested for antimicrobial activity against selected microbial strains. Among the synthesized prodrugs, M1 was found to exhibit significant antibacterial efficacy having MIC 6.25 µg/ml against S. aureus MTCC 96 and prodrug M6 depicted good antibacterial activity (MIC 6.25 µg/ml) against E. coli MTCC 443 when compared with norfloxacin (MIC 10 µg/ml). Prodrugs M2 and M4 showed comparable activity against E. coli MTCC 443 and P. aeruginosa MTCC 1688 respectively to standard drug norfloxacin. The antibacterial activity of prodrug M4 (MIC 25 µg/ml) was found to be better than ciprofloxacin (MIC 50 µg/ml) against S. pyogenus MTCC 442. Moreover, prodrugs M4 and M6 possessed better antifungal activities (MIC 250, 75 µg/ml respectively) against C. albicans MTCC 227 while M2 showed significant potency against A. niger MTCC 282 and A. clavatus MTCC 1323 (MIC 50 µg/ml) compared to standard drug nystatin (MIC 100 µg/ml).

scholarly journals Synthesis and Pharmacological Evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

2020 ◽  
Vol 10 (5) ◽  
pp. 274-292
Author(s):  
Rohit Kumar ◽  
Sushil Kumar ◽  
Mohammad Asif Khan
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Biological Activities ◽  
Diffusion Method ◽  
Gram Positive ◽  
Standard Drug ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Pharmacological Evaluation

Recently a series of Schiff bases of diphenylamine derivatives have been synthesized and evaluated in vitro for their antibacterial activity against pathogenic both Gram-positive bacteria B. subtitles and Gram-negative bacteria E. coli using ciprofloxacin as standard drug at conc. of 50 μg/ml and 100 μg/ml. Literature review revels that chalcones possesses various biological activities like antimicrobial, antiviral, anti-inflammatory, anticancer and sedative etc. Therefore the present study was designed on synthesis and pharmacological evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides. Target compound was synthesized by reaction of chloroacetylchloride with diphenylamine to afford 2-chloro-N, N-diphenylacetamide which further by reaction with substituted Chalcones and characterized following recrystallization and evaluated for anti-microbial potential through cup-diffusion method. In results, the target compounds were tested for activity against B. Subtilis, E.Coli and C. albicans. The chalcones having the lipophilic 4-chloro group (RKCT2) showed the greatest antimicrobial activity (zone of inhibition 20 & 22 mm against. B. subtilis, E. Coli, C. Albicans respectively. It suggests further researchers to go through anti-microbial evaluations against a more varieties of bacteria and fungi. Keywords: Schiff bases of diphenylamine derivatives, antibacterial activity, Gram-positive bacteria, 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

scholarly journals In vitro antibacterial and antioxidant activity of Rosmarinus officinalis

2021 ◽  
Vol 285 ◽  
pp. 05012
Author(s):  
A. K. Milyuhinа ◽  
L. A. Zabodalova ◽  
U. Kyzdarbek ◽  
I. R. Romazyaeva ◽  
N. Yu. Klyuchko
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Antimicrobial Properties ◽  
Ethanol Extract ◽  
Rosmarinus Officinalis ◽  
E Coli ◽  
Rosmarinus Officinalis L ◽  
Antibacterial And Antioxidant Activity

Rosmarinus officinalis L. is known for its antioxidant and antibacterial properties against a variety of microorganisms. In this work, research has been carried out on pharmacy rosemary. Its antioxidant and antimicrobial properties have been determined. This study showed that the ethanol extract of R. officinalis L. has a pronounced antimicrobial activity against strains of both gram-positive and gram-negative bacteria. The extract also showed good antioxidant activity. Rosemary showed significantly more potent antibacterial activity against E. coli. The diameter of the zone of oppression was 17 mm. Thus, Rosemary Pharmaceutical has demonstrated potential as a dietary supplement due to its stronger antibacterial activity.

scholarly journals Facile Synthesis, Characterization, and In Vitro Antimicrobial Screening of a New Series of 2,4,6-Trisubstituted-s-triazine Based Compounds

2015 ◽  
Vol 2015 ◽  
pp. 1-10
Author(s):  
Ravi Bhushan Singh ◽  
Nirupam Das ◽  
Md. Kamaruz Zaman
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Elemental Analysis ◽  
Broad Spectrum ◽  
Antibacterial Efficacy ◽  
Facile Synthesis ◽  
Standard Drug ◽  
E Coli

A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, 1HNMR, 13CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 μgmL−1 against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 μgmL−1) and S. aureus (MIC 6.25 μgmL−1). The studies demonstrated that the para-fluorophenylpiperazine substituted s-triazine (4n) was potent and exhibited broad spectrum antibacterial activity against S. epidermidis, K. pneumoniae, and P. aeruginosa with MIC of 6.25 μgmL−1 and for E. coli, it showed an MIC of 3.125 μgmL−1 equipotent with reference to the standard drug. Among all the compounds under investigation, compound 4g also demonstrated significant antifungal activity (3.125 μgmL−1) against C. albicans.

Synthesis and Antibacterial Activity of Azetidinonyl Norfloxacin Congeners

2015 ◽  
Vol 8 (3) ◽  
pp. 2967-2971
Author(s):  
Shalabh Sharma ◽  
Kuldeep Kumar Saxena
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Elemental Analysis ◽  
Standard Drug ◽  
Reference Drug ◽  
E Coli ◽  
Subtilis Atcc ◽  
Structure Activity ◽  
Drug Compound

Some novel Schiff bases and azetidinone congeners of norfloxacin have been synthesized and screened for antibacterial activity. The structures of compounds 1-ethyl-6-fluoro-7-piperazinyl-4-oxo-3-(substitutedarylidinylcarboxy- hydrazido)quinolines (2-6) and 1-ethyl-6-fluoro-7-pipera-zinyl-4-oxo-3-(3′-choloro-2′-oxo-4′-substitutedaryl-3′-aze-tidinyl)-aminocarboxy quinolines (7-11) were established by spectral and elemental analysis. The compounds 2-11 were evaluated in vitro against various strains of bacteria: E. coli ATCC 25922,    B. subtilis ATCC 1633 and S. aureus ATCC 25923 to determine their antibacterial activity and feasible structure-activity relationships. The results of the study were compared with reference drug. Compound 8: 1-ethyl-6-fluoro-7-piperazinyl-4-oxo-3-(3′-choloro-2′-oxo-4′-(4′′-methoxyphenyl)-3′-azetidinyl)-aminocarboxyquinoline has displayed more potent antibacterial activity as compared to standard drug, chloramphenicol.   

scholarly journals Antibacterial Activity of Fistulin: A Protease Inhibitor Purified from the Leaves of Cassia fistula

2012 ◽  
Vol 2012 ◽  
pp. 1-4 ◽  
Author(s):  
I. Arulpandi ◽  
R. Sangeetha
Keyword(s):  
Antibacterial Activity ◽  
Gel Filtration ◽  
Antimicrobial Properties ◽  
Antibacterial Efficacy ◽  
Bacterial Strains ◽  
Streptomycin Sulphate ◽  
Cassia Fistula ◽  
Standard Drug ◽  
E Coli ◽  
Plant Protease

Plant protease inhibitors (PPIs) are one of the important components of a plant’s defense machinery. PPIs are active against the insects and microbes which invade the plant. Cassia species possess anti-insecticidal and antimicrobial properties and this study was aimed at investigating the antibacterial efficacy of a PPI present in the leaves of Cassia fistula. A PPI, fistulin, was isolated from the leaves of C. fistula and purified by gel filtration chromatography. The antibacterial activity of the purified fistulin was studied against five bacterial strains, namely, Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli. The PPI was found to be very active against S. aureus, E. coli, B. subtilis, and K. pneumonia, and its efficacy was comparable to the standard drug, streptomycin sulphate.

Solubility Enhancement of Poorly Water-Soluble Antifungal Drug Acyclovir by Nanocrystal Formulation Approach

2018 ◽  
Vol 11 (2) ◽  
pp. 4036-4042
Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H
Keyword(s):  
Chemical Interaction ◽  
Research Work ◽  
Antiviral Drug ◽  
In Vitro Release ◽  
Oral Route ◽  
Water Soluble ◽  
Precipitation Method ◽  
Dsc Studies ◽  
Ft Ir

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 

Quality-by-Design Enabled Chitosan Nanoparticles for Antitubercular Therapy: Formulation, Statistical Optimization, and In vitro Characterization

2020 ◽  
Vol 15 ◽  
Author(s):  
Manasi M. Chogale ◽  
Sujay S. Gaikwad ◽  
Savita P. Kulkarni ◽  
Vandana B. Patravale
Keyword(s):  
Side Effects ◽  
Treatment Regimen ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Antitubercular Therapy ◽  
Prolonged Treatment ◽  
High Dose ◽  
Average Size

Background: Tuberculosis (TB) continues to be among the leading causes for high mortality among developing countries. Though a seemingly effective treatment regimen against TB is in place, there has been no significant improvement in the therapeutic rates. This is primarily owing to the high drug doses, their associated sideeffects, and prolonged treatment regimen. Discontinuation of therapy due to the severe side effects of the drugs results in the progression of the infection to the more severe drug-resistant TB. Objectives: Reformulation of the current existing anti TB drugs into more efficient dosage forms could be an ideal way out. Nanoformulations have been known to mitigate the side effects of toxic, high-dose drugs. Hence, the current research work involves the formulation of Isoniazid (INH; a first-line anti TB molecule) loaded chitosan nanoparticles for pulmonary administration. Methods: INH loaded chitosan nanoparticles were prepared by ionic gelation method using an anionic crosslinker. Drugexcipient compatibility was evaluated using DSC and FT-IR. The formulation was optimized on the principles of Qualityby-Design using a full factorial design. Results: The obtained nanoparticles were spherical in shape having an average size of 620±10.97 nm and zeta potential +16.87±0.79 mV. Solid state characterization revealed partial encapsulation and amorphization of INH into the nanoparticulate system. In vitro release study confirmed an extended release of INH from the system. In vitro cell line based safety and efficacy studies revealed satisfactory results. Conclusion: The developed nanosystem is thus an efficient approach for antitubercular therapy.

In Vitro Antibacterial activity of ethanolic extract of Myrsine africana against laboratory Strains of Pathogenic Organisms

2016 ◽  
Vol 5 (04) ◽  
pp. 4512
Author(s):  
Jackie K. Obey ◽  
Anthoney Swamy T* ◽  
Lasiti Timothy ◽  
Makani Rachel
Keyword(s):  
Antibacterial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
E Coli ◽  
Zones Of Inhibition ◽  
In Vitro Antibacterial Activity ◽  
Myrsine Africana

The determination of the antibacterial activity (zone of inhibition) and minimum inhibitory concentration of medicinal plants a crucial step in drug development. In this study, the antibacterial activity and minimum inhibitory concentration of the ethanol extract of Myrsine africana were determined for Escherichia coli, Bacillus cereus, Staphylococcus epidermidis and Streptococcus pneumoniae. The zones of inhibition (mm±S.E) of 500mg/ml of M. africana ethanol extract were 22.00± 0.00 for E. coli,20.33 ±0.33 for B. cereus,25.00± 0.00 for S. epidermidis and 18. 17±0.17 for S. pneumoniae. The minimum inhibitory concentration(MIC) is the minimum dose required to inhibit growth a microorganism. Upon further double dilution of the 500mg/ml of M. africana extract, MIC was obtained for each organism. The MIC for E. coli, B. cereus, S. epidermidis and S. pneumoniae were 7.81mg/ml, 7.81mg/ml, 15.63mg/ml and 15.63mg/ml respectively. Crude extracts are considered active when they inhibit microorganisms with zones of inhibition of 8mm and above. Therefore, this study has shown that the ethanol extract of M. africana can control the growth of the four organisms tested.

scholarly journals Development and Evaluation of Rifampicin Loaded Alginate–Gelatin Biocomposite Microfibers

Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1514
Author(s):  
Ameya Sharma ◽  
Vivek Puri ◽  
Pradeep Kumar ◽  
Inderbir Singh ◽  
Kampanart Huanbutta
Keyword(s):  
Wound Healing ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Tissue Proliferation ◽  
Naturally Occurring ◽  
Reinforcing Material ◽  
Vitro Release

Various systematic phases such as inflammation, tissue proliferation, and phases of remodeling characterize the process of wound healing. The natural matrix system is suggested to maintain and escalate these phases, and for that, microfibers were fabricated employing naturally occurring polymers (biopolymers) such as sodium alginate, gelatin and xanthan gum, and reinforcing material such as nanoclay was selected. The fabrication of fibers was executed with the aid of extrusion-gelation method. Rifampicin, an antibiotic, has been incorporated into a biopolymeric solution. RF1, RF2, RF3, RF4 and RF5 were coded as various formulation batches of microfibers. The microfibers were further characterized by different techniques such as SEM, DSC, XRD, and FTIR. Mechanical properties and physical evaluations such as entrapment efficiency, water uptake and in vitro release were also carried out to explain the comparative understanding of the formulation developed. The antimicrobial activity and whole blood clotting of fabricated fibers were additionally executed, hence they showed significant results, having excellent antimicrobial properties; they could be prominent carriers for wound healing applications.

Antimicrobial Screening, in Silico Studies and QSAR of Chalcone-based 1,4-disubstituted 1,2,3-triazole Hybrids

Drug Research ◽  
2020 ◽  
Author(s):  
Pinki Yadav ◽  
Kashmiri Lal ◽  
Ashwani Kumar
Keyword(s):  
Topoisomerase Ii ◽  
Antimicrobial Properties ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Binding Modes ◽  
E Coli ◽  
Structure Activity ◽  
In Silico Studies ◽  
Microbial Strains

AbstractThe in vitro antimicrobial properties of some chalcones (1a–1c ) and chalcone tethred 1,4-disubstituted 1,2,3-triazoles (2a–2u) towards different microbial strains viz. Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Candida albicans are reported. Compounds 2g and 2u exhibited better potency than the standard Fluconazole with MIC values of 0.0063 µmol/mL and 0.0068 µmol/mL, respectively. Furthermore, molecular docking was performed to investigate the binding modes of two potent compounds 2q and 2g with E. coli topoisomerase II DNA gyrase B and C. albicans lanosterol 14α-demethylase, respectively. Based on these results, a statistically significant quantitative structure activity relationship (QSAR) model was successfully summarized for antibacterial activity against B. subtilis.

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