Microwave Assisted Synthesis of Novel N-(Benzo[d]Thiazol-2-yl)-2-((2,4'-Dioxospiro[Indoline-3,2'-Thiazolidin]-3'-yl)Amino)Acetamide Derivatives as Potent Antibacterial Agents

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.

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.


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.


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.


1998 ◽  
Vol 42 (4) ◽  
pp. 911-915 ◽  
Author(s):  
Wenqiu Liu ◽  
Xuejun Liu ◽  
David Knaebel ◽  
Linda Luck ◽  
Yuzhou Li

ABSTRACT A set of new water-soluble organic peroxides has been synthesized and evaluated for in vitro antibacterial activity as part of an effort to develop new antibacterial agents for the treatment of acne vulgaris. The water solubility of these new dialkyl peroxides and peroxyesters was achieved by incorporating either a quaternary ammonium group or a polyethylene glycol moiety. These peroxides are effective against both gram-positive and gram-negative bacteria and have a prolonged activity compared to that of benzoyl peroxide and other peroxide-type antiseptic agents. Among them 4-[[(tert-butylperoxy)carbonyl]benzyl]triethylammonium chloride and [10-(tert-butylperoxy)decyl]trimethylammonium bromide have the broadest antimicrobial spectrums. We have shown that the oxidizing properties of the dioxy group of these compounds are responsible for their antibacterial activities.


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