NOVEL 1,2,4-TRIAZOLE-3-MERCAPTOACETIC ACID DERIVATIVES AS POTENTIAL ANTIMYCOBACTERIAL AND ANTIMICROBIAL AGENTS

2006 ◽  
Vol 29 (1) ◽  
pp. 127-136
Author(s):  
Nawal El-Koussi ◽  
Hamdy Abdel-Rahman
Keyword(s):  
Antimicrobial Agents ◽  
Mercaptoacetic Acid

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO (INDOLE-THIAZOLIDINE) DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 71-74
Author(s):  
PRIYANKA NIVRUTTI SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Mercaptoacetic Acid ◽  
Ir Absorption ◽  
Absorption Bands ◽  
Synthesis And Biological Evaluation ◽  
Anhydrous Zncl2

Objective: The present study aims to synthesize and biological evaluation of Spiro-[Indole-Thiazolidine] derivatives as antimicrobial agents. Methods: The reaction sequence involves microwave-induced preparation of N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene)pyridine-4-carbohydrazide [3] from isoniazid [1] and isatin [2] followed by the cyclo condensation of [3] and mercaptoacetic acid under microwave condition to achieve the synthesis of spiro-[indole-thiazolidine] derivatives [4]. The resulting compounds were then allowed to react with various aromatic and heterocyclic aromatic aldehydes to afford arylidene derivatives [5a-l]. Result: Isoniazid (1) on condensation with isatin (2) in the presence of catalytic amount of glacial acetic acid furnished N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene) pyridine-4-carbohydrazide (3), which showed characteristic IR, absorption bands. Compound (3) underwent Spiro cyclization upon its reaction with mercaptoacetic acid in the presence of anhydrous ZnCl2 to form spiro-[indole-thiazolidine] compound (4). Compound (4) was then condensed with aromatic aldehydes to give arylidene derivatives (5a-l), which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by the cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

Design and synthesis of novel thiopheno-4-thiazolidinylindoles as potent antioxidant and antimicrobial agents

2014 ◽  
Vol 68 (3) ◽  
Author(s):  
Jaiprakash Biradar ◽  
Parveen Rajesab ◽  
B. Sasidhar
Keyword(s):  
Antimicrobial Agents ◽  
Analytical Data ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Mercaptoacetic Acid ◽  
Antioxidant Power ◽  
Mass Spectral ◽  
Design And Synthesis ◽  
High Yields

AbstractA novel and convenient synthesis of thiopheno-4-thiazolidinyl indole analogues is presented (IVa-IVi), with the aim of obtaining biologically active compounds. 3,5-disubstituted indol-2-carboxyhydrazides (Ia-If) were allowed to react with 3-acetyl-2,5-dichlorothiophene (II) to yield the corresponding 3,5-disubstituted indol-2-carbohydrazides (IIIa-IIIf). The pre-formed indolecarbohydrazides (IIIa-IIIf) were allowed to react with 2-mercaptoacetic acid or 2-mercaptopropanoic acid to produce thiopheno-4-thiazolidinylindoles (IVa-IVi). This reaction protocol affords a simple, eco-friendly, non-hazardous, easier preparation and high yields. The antioxidant (free radical scavenging, total antioxidant capacity and ferric-reducing antioxidant power) and antimicrobial activities of the synthesised compounds were evaluated. The structures and purity of the products were confirmed by their IR, 1H NMR, 13C NMR and mass spectral and analytical data. Most of the compounds tested showed very significant scavenging, antioxidant and antimicrobial activities. Compounds containing electron donor group (CH3) at the fifth position of indole exhibit an excellent ferric-reducing activity. The present study suggests that compounds IIIa-IIIb, IIIf, IVa-IVc, IVf-IVi, may serve as promising lead scaffolds for antioxidant and antimicrobial agents.

scholarly journals Synthesis of sulfonamides bearing 1,3,5-triarylpyrazoline and 4-thiazolidinone moieties as novel antimicrobial agents

2020 ◽  
Vol 85 (2) ◽  
pp. 155-162
Author(s):  
Thi-Dan Thach ◽  
Thi Le ◽  
Thien-Annguyen Nguyen ◽  
Chi-Hien Dang ◽  
Van-Su Dang ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Significant Inhibition ◽  
Mercaptoacetic Acid ◽  
Bacterial Strains ◽  
Reference Drug ◽  
E Coli ◽  
Yeast Strains ◽  
Microbial Strains

Two series of sulfonamides were synthesized from 4-hydrazinylbenzenesulfonamide as the key starting material. 1,3,5-Triarylpyrazoline sulfonamides (2a?i) were obtained by cyclocondensation of various chalcones in 53? ?64 % yields, while 4-thiazolidinone derivatives (4a?e) were synthesized by cyclocondensation between mercaptoacetic acid and different phenylhydrazones in 43?62 % yields. The synthesized compounds were characterized based on FTIR, 1H-NMR, 13C-NMR and HRMS data. The sulfonamides were evaluated for their in vitro antimicrobial activities against four bacterial strains (E. coli, P. aeruginosa, B. subtillis and S aureus), two filamentous fungal strains (A. niger and F. oxysporum) and two yeast strains (C. albicans and S. cerevisiae). Seven pyrazolines, 2a?c and 2e?h, exhibited significant inhibition of different microbial strains. Among them, compound 2b displayed good antifungal activity against A. niger (MIC value at 12.5 ?g mL-1) over the reference drug.

Essential oil from Zanthoxylum tingoassuiba loaded into multilamellar liposomes useful as antimicrobial agents

2009 ◽  
pp. 1-8 ◽  
Author(s):  
C. B. Detoni ◽  
E. C. M. Cabral-Albuquerque ◽  
S. V. A. Hohlemweger ◽  
C. Sampaio ◽  
T. F. Barros ◽  
...  
Keyword(s):  
Essential Oil ◽  
Antimicrobial Agents ◽  
Multilamellar Liposomes

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

Vaccines for aquaculture overview

2020 ◽  
pp. 42-43
Author(s):  
Andrey S. Khishov ◽  
◽  
Galina I. Burlakova ◽  
Keyword(s):  
Antimicrobial Agents ◽  
Aquatic Organisms ◽  
Animal Husbandry ◽  
Well Being ◽  
Pharmaceutical Drugs ◽  
Short Development Time ◽  
The Creation ◽  
Basic And Applied Research ◽  
North And South America ◽  
Aquaculture Production

Aquaculture production is a promising direction for the development of food production. Like traditional types of animal husbandry, it needs effective medicines for veterinary use, which would ensure not only the well-being of farmed aquatic organisms, but also increase the safety of the fish products and non-fish objects of fishing. The development of measures to control epizootic processes in aquatic organisms is impossible without the creation of new immunological preparations. The development and use of immunobiological drugs will reduce the use of antimicrobial agents. The corresponding set of pharmaceutical drugs was transferred from the traditional veterinary medicine, but due to the peculiarities of the biology of aquatic animals, their immunity and the characteristics of specific pathogens, this could not be done with biological products. The short development time in the aquaculture industry poses current challenges in the form of a lack of basic and applied research for relatively poorly understood groups of new pathogens. The immunological processes associated with the development and intensity of the immune response in aquatic organisms require a detailed study. For domestic aquaculture producers, the analysis and dissemination of the experience accumulated by mankind and the application of advanced developments in this area are even more relevant, since Russia is just beginning its path of intensifying aquaculture production. At the same time, it is clear that the prohibition of the use and monitoring of antimicrobial agents in food products and feed requires a change in the approach to the problem and will lead to the creation of new immunobiological drugs. The market for immunobiological preparations for aquaculture is the most promising for development. In the article, the authors provide data on the development and registration of vaccines for aquaculture in Europe, North and South America.

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