scholarly journals Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

Author(s):  
Manoj N. Bhoi ◽  
Mayuri A. Borad ◽  
Hitesh B. Parmar ◽  
Hitesh D. Patel

As part of ongoing studies in developing new antibacterial agent, a novel series of N-(benzo[d]thiazol-2-yl)-2-(2-(6-chloroquinolin-4-yl)hydrazinyl)acetamide derivatives was synthesized by sequencing reaction of 2-aminobenzothiazole with chloroacetylchloride, hydrazine hydrate and 4,7-dichloroquinoline. The novel heterocycles were characterized by elemental analyses and various spectroscopic techniques. The synthesized compounds were tested in-vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial activity against the tested microorganisms.

Author(s):  
Mayuri A. Borad ◽  
Manoj N. Bhoi ◽  
Jagruti A. Parmar ◽  
Hitesh D. Patel

As part of continuing studies in emerging new antibacterial agent, a novel series of N-(benzo[d] thiazol-2-yl)-2-((2,4’-dioxospiro[indoline-3, 2’-thiazolidin]-3'-yl)amino)acetamide derivatives were synthesized by sequencing reaction of 2-aminobenzothiazole with chloroacetyl chloride, hydrazine hydrate, isatin and Thioglycolic acid. The novel heterocycles were characterized by elemental analyses and various spectroscopic techniques. The synthesized compounds were tested in-vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria. Bacteriological results showed that compound 5c possessed a broad spectrum of antibacterial activity against the tested microorganisms.


2016 ◽  
Vol 13 (3) ◽  
pp. 568-577
Author(s):  
Baghdad Science Journal

In this paper some chalcones (C1-C8) are prepared based on the reaction of one mole of substituted acetophenone with one mole of substituted benzaldehydes in the presence of (40%) sodium hydroxide as a base. Pyrazolines (P1–P8) are prepared from the reaction of chalcones (C1-C8) with hydrazine hydrate. Isoxazoline (I1-I8) is prepared from the reaction of chalcones (C1-C8) with hydroxyl amine hydrochloride in the presence of (10%) sodium hydroxide as a base. These compounds are characterized by using various physical and spectral methods. The compounds are screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria. Several derivatives of pyrazolines and isoxazolines are produced well to moderate activities against number of bacteria.


Author(s):  
K Sunand ◽  
K Vinay Kumar ◽  
K Ashwini ◽  
P Suresh Kumar ◽  
S Vishnu ◽  
...  

Aim: To synthesize and evaluate 4-aminoantipyrine related schiff’s bases as antibacterial agents. Objective: To synthesize, purify, characterize and evaluate 4-aminoantipyrine. Method: Schiff bases derived from 4-aminoantipyrine play a vital role in biological and pharmacological activities. Knowing the importance of 4-aminoatipyrine schiff bases and their analogues wide varieties of bioactivities like analgesic, antiviral, antipyretic, anti-rheumatic, antimicrobial and anti-inflammatory activities have been widely studied. 4-aminoantipyrine compounds C1 (anisaldehyde), C2 (p-hydroxybenzaldehyde) and C3(vanillin) were prepared by condensation between 4-amino antipyrine and substituted aromatic benzaldehydes. The products were purified by recrystallization by using ethanol, characterized by IR spectroscopy. The N-H stretching in 4-aminoantipyrine is shown at 3430 cm-1 and -3325 cm-1. The -HC=N- stretching is observed in the range of 1508-1504 cm-1 The –OCH3 stretching is found at 1888 cm-1. 4-amino antipyrine related schiff’s bases evaluated their activity as antimicrobials in-vitro by spread plate method against E.coli. Schiff bases have potent antibacterial activity with gram negative bacteria E.coli. Results: Synthesis and characterization of a schiff bases derived from substituted benzaldehydes and 4-aminoantipyrine was evaluated and characterized with the IR spectroscopic techniques and schiff bases have shown potent antibacterial activity against E.Coli.


2009 ◽  
Vol 4 (7) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Flor D. Mora ◽  
María Araque ◽  
Luis B. Rojas ◽  
Rosslyn Ramírez ◽  
Bladimiro Silva ◽  
...  

Chemical constituents of the essential oil from the leaves of Minthostachys mollis (Kunth) Griseb Vaught var. mollis collected in January 2008 at Tuñame, Trujillo State, Venezuela, were separated and identified by GCMS analysis. The essential oil was obtained by hydrodistillation and thirteen components (98.5% of the sample) were identified by comparison with the Wiley GCMS library data base. The two major components were pulegone (55.2%) and trans-menthone (31.5%). The essential oil showed a significant inhibitory effect against Gram-positive and Gram-negative bacteria, especially Bacillus subtilis and Salmonella typhi (4 μg/mL).


Author(s):  
Na Li ◽  
Jiang-Kun Dai ◽  
Dan Liu ◽  
Jin-Yi Wang ◽  
Jun-Ru Wang

Natural products are an important source of antibacterial agents. Canthin-6-one alkaloids have displayed potential antibacterial activity based on our previous work. In order to improve the activity, twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by double dilution method. Four compounds (6f, 6i, 6p and 6t) displayed 2-fold superiority (minimum inhibitory concentration (MIC) = 3.91 µg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae than agrochemical propineb. Moreover, the structure–activity relationships (SARs) were also carefully summarized in order to guide the development of antibacterial canthin-6-one agents.


2020 ◽  
Vol 7 (1) ◽  
pp. 1-9
Author(s):  
Nuke Annisa Nasution ◽  
I Made Artika ◽  
Dodi Safari

Antibacterial resistance in Streptococcus pneumoniae has been increasing and is one of ongoing global concern.  The need to find new antibacterial agents against Streptococcus pneumoniae is of paramount importance. Medicinal plants are prospective sources of antibacterial agents. The aims of the present study were to determine the activity of leaf extraxt of Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. against Streptococcus pneumoniae.  Leaves of Anredera cordifolia (Ten.) Steenis were extracted using 96% ethanol, while the leaves of Muntingia calabura L were extracted using 100% methanol.  The leaf extracts of the two plants obtained were bioassayed for antibacterial activity against Streptococcus pneumoniae ATCC 49619 and a clinical isolate Streptococcus pneumoniae PU 067.  Results showed that leaf extracts of both Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. have antibacterial activity in vitro against Streptococcus pneumoniae ATCC 49619 at crude extract concentrations of 25%, 50%, 75% and 100% (w/v). Both plants extracts showed strongest activity against S. pneumoniae ATCC 49619 at extract concentration of 75%.   In addition, the extracts of both plants have inhibitory activity against growth of the clinical isolate Streptococcus pneumoniae PU 067. Both plant extracts showed strongest activity against S. pneumoniae PU 067 at extract concentration of 100%.  Therefore, leaf extracts of Anredera cordifolia (Ten.) Steenis and Muntingia calabura L. can potentially be used as a source of antibacterial agent for Streptococcus pneumoniae. Keywords: Antibacterial agent, Anredera cordifolia (Ten.) Steenis, Muntingia calabura L., Streptococcus pneumoniae.


2021 ◽  
Vol 33 (11) ◽  
pp. 2707-2714
Author(s):  
P. Uma ◽  
J. Suresh ◽  
Revathi Selvaraj ◽  
A. Arun

This work is focused on the synthesis and characterization of versatile acrylate polymer of chalcone based triazine for their antibacterial activity and cumulative drug release behaviour studies. The novel acrylate monomer 4-(3-(4-((4-(4-(3-(4-((7-chloroquinolin-4-yl)amino)-phenyl)-3-oxoprop-1-en-1- yl)phenoxy)-6-((4-nitrophenyl)amino)-1,3,5-triazin-2-yl)oxy)phenyl)-3-oxoprop-1-en-1- yl)phenylacrylate (SCP) is from novel chalcone and acryloyl chloride. Homo and copolymers of SCP were prepared using acrylic acid and hydroxyethyl acrylate. Physical characterization confirms the formation of the above compounds. Prepared drug molecules possess chalcone moiety as well as quinoline so it has the greater effect to inhibit the growth of the Gram-negative bacteria (15.63 ± 0.4 μg/mL) was confirmed by MIC method. The weight average molecular weight of the polymer is 10,000 g/mol. The polymer decomposes at 325 ºC. Drug releasing in vitro behaviour of the synthesized drug is controlled by the nature of comonomer, pH and the temperature.


2021 ◽  
Vol 34 (1) ◽  
pp. 209-215
Author(s):  
Pravin S. Kulkarni ◽  
Swapnil R. Sarda ◽  
Amol U. Khandebharad ◽  
Mazahar Farooqui ◽  
Brijmohan R. Agrawal

A new series of 5-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole (6a-o) have been synthesized by a cyclocondensation reaction of ethyl 5-(4-chlorophenyl)-1-phenyl-1H-pyrazole-3- carboxylate (3a-c) with aryl imidoxime (5a-e). The newly synthesized pyrazolyl-1,2,4-oxadiazole (6a-o) derivatives were characterized by spectroscopic techniques and screened for in vitro antibacterial activity against Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178), Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) and in vitro antifungal activity against Aspergillus niger (ATCC 504) Candida albicans (NCIM 3100).


2020 ◽  
Vol 11 (6) ◽  
pp. 5257-5265
Author(s):  
Samia Rabah ◽  
Kahina Kouachi ◽  
Patrícia A. B. Ramos ◽  
Ana Peixoto Gomes ◽  
Adelaide Almeida ◽  
...  

Allium triquetrum L. bulbs, flowers and leaves are proved to be valuable sources of value-added lipophilic compounds, specifically as antibacterial agents against methicillin-resistant Staphylococcus aureus.


2019 ◽  
Vol 16 (3) ◽  
pp. 284-290
Author(s):  
Nayan M. Panchani ◽  
Hitendra S. Joshi

Background:Several strategies have been reported for the synthesis of thiazole derivatives.Methods:However, many of these methods suffer from several drawbacks. Several modifications have been made to counter these problems. Here, we have synthesized a new series of 2-(2-((1HImidazol- 4-yl)methylene)hydrazinyl)-4-(4-substitutedphenyl)thiazoles without using the catalyst at room temperature.Results:The structures of synthesized compounds have been confirmed by spectral analysis, such as Mass, IR, 1H NMR and 13C NMR. All synthesized compounds were screened for in vitro antibacterial activity against some gram-positive and gram-negative bacteria.Conclusion:The thiazole derivatives, with a pharmacologically potent group, discussed in this article may provide valued therapeutic important in the treatment of microbial diseases, especially against bacterial and fungal infections.


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