scholarly journals New Urea and Thiourea Derivatives of Piperazine Doped with Febuxostat: Synthesis and Evaluation of Anti-TMV and Antimicrobial Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Reddivari Chenna Krishna Reddy ◽  
Syed Rasheed ◽  
Devineni Subba Rao ◽  
Shaik Adam ◽  
Yellala Venkata Rami Reddy ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Biological Data ◽  
Thiourea Derivatives ◽  
Biological Interest ◽  
Antiviral Activities ◽  
High Yields ◽  
Selective Reagent ◽  
Substituted Urea

A series of new 4-(5-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-2-carbonyl)-N-(substituted phenyl)piperazine-1-carboxamides8(a–e)/carbothioamides8(f–j)were accomplished for biological interest by the simple addition of active functionalized arylisocyanates7(a–e)/arylisothiocyanates7(f–j)with 2-isobutoxy-5-(4-methyl-2-(piperazine-1-carbonyl)thiazol-5-yl)benzonitrile(4). Compound4was synthesized in high yields (94%) by the condensation reaction of febuxostat (1) with piperazine using a selective reagent such as propylphosphonic anhydride (T3P). Antiviral activity againstTobacco mosaic virus(TMV) and antimicrobial activity of the synthesized compounds were evaluated. Biological data revealed that 4-nitrophenyl substituted urea8d, and 3-bromophenyl substituted thiourea8fexhibited promising antiviral activities. Moreover, 4-fluorophenyl substituted urea8a, 4-nitrophenyl substituted urea8d, 3-bromophenyl substituted thiourea8f, and 2,4-dichlorophenyl substituted thiourea8jexhibited potent antimicrobial activity.

scholarly journals Multicomponent Reactions: Microwave-assisted Efficient Synthesis of Dihydropyrimidinones (thiones) and Quinazolinones under Green Chemistry Protocol as Probes for Antimicrobial Activities

2011 ◽  
Vol 4 (1) ◽  
pp. 143 ◽  
Author(s):  
M. H. Bhuiyan ◽  
H. Nessa ◽  
M. M. Mahmud
Keyword(s):  
Antimicrobial Activity ◽  
Multicomponent Reactions ◽  
Biginelli Reaction ◽  
Salmonella Typhi ◽  
Antimicrobial Activities ◽  
Shigella Dysenteriae ◽  
Dicarbonyl Compound ◽  
Solvent Free Conditions ◽  
High Yields ◽  
Diammonium Hydrogen

Microwave promoted diammonium hydrogen phosphate, (NH4)2HPO4, catalyzed three-component Biginelli reaction between an aldehyde, a 1,3-dicarbonyl compound and urea or thiourea under solvent-free conditions afforded the corresponding dihydropyrimidinones and quinazolinones in high yields. The synthesized compounds have been screened for their antimicrobial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Vibrio choloriae, Shigella dysenteriae, Salmonella typhi bacteria and Aspargilllus flavus, Saccharomyces cerevisiae and Candida albicans fungi respectively. Some of the synthesized compounds exhibited pronounced antimicrobial activities.Keywords: Multicomponent reactions; Dihydropyrimidinone; Microwave irradiation; Antimicrobial activity.© 2012 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v4i1.8688J. Sci. Res. 4 (1), 143-153 (2012)

scholarly journals Eco-friendly and simple synthesis of some non-natural flavones through chalcones

2018 ◽  
Vol 9 (3) ◽  
pp. 236-240
Author(s):  
Mohammad Saidur Rahman ◽  
Sayeda Shakila Alam ◽  
Kamrunnahar Happy ◽  
Mohammad Mamun Hossain ◽  
Mohammad Khademul Islam ◽  
...  
Keyword(s):  
Sulfuric Acid ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Simple Synthesis ◽  
Minimal Amount ◽  
Important Class ◽  
High Yields ◽  
Antioxidant And Antimicrobial Activities

A distinctive feature of polyphenolics is the possession of biological properties such as antioxidant and antimicrobial activities. Simple synthesis and study about such important class of compounds and their analogs are very important to enhance the understanding of their role in human health and diseases. Accordingly, a series of chalcones (2a-f) have been synthesized by Claisen-Schmidt condensation reaction with required acetophenones and aromatic aldehydes in high yields. The conversion of chalcones to the corresponding flavones (1a-g) taking minimal amount of dimethyl sulfoxide with iodine in presence of sulfuric acid was carried out under microwave conditions in high yields.

scholarly journals Synthesis, spectral characterization, antimicrobial activity and docking studies against DNA Gyrase-A of new 4-chloro-3-nitrobenzene sulfonamide derivatives

2020 ◽  
Vol 13 (4) ◽  
pp. 155-164
Author(s):  
K. Pushpa Kumar ◽  
Reddi Mohan Naidu Kalla ◽  
Mavallur Varalakshmi ◽  
Chintha Venkataramaiah ◽  
K.Swetha Kumari ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Sulfonyl Chloride ◽  
Dna Gyrase ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Amino Acid Esters ◽  
Elemental Analyses ◽  
Gyrase A ◽  
High Yields ◽  
Acid Esters

A series of new 4-chloro-3-nitrobenzene sulfonamide derivatives 3(a-j) were synthesized from 4-chloro-3-nitrobenzene sulfonyl chloride by reacting various amino acid esters and amines 2(a-j) in high yields. The structures of all the synthesized compounds were characterized by the IR, NMR (1H & 13C), mass and elemental analyses. Further, all the synthesized compounds were tested for the antimicrobial activity and docking studies were carried out with DNA Gyrase-A. Most of the compounds showed good to moderate antimicrobial activities and binding affinity towards DNA Gyrase-A structure.

ANTIMICROBIAL ACTIVITIES OF METHANOL EXTRACT FROM UNIDENTIFIED SPONGE ASSOCIATED BACTERIA IN LEMUKUTAN ISLAND, KALIMANTAN BARAT

2009 ◽  
Vol 1 (2) ◽  
Author(s):  
Risa Nofiani ◽  
Siti Nurbetty ◽  
Ajuk Sapar
Keyword(s):  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Pathogenic Bacteria ◽  
Methanol Extract ◽  
Agar Medium ◽  
Antimicrobial Activities ◽  
Antimicrobial Compounds ◽  
Associated Bacteria ◽  
Minimum Inhibitory Concentrations ◽  
Sponge Associated Bacteria

<p>The increase of issues on the antibiotics resistant pathogenic bacteria has triggered high exploration for new antimicrobial compounds. One of the potential sources is sponge-associated bacteria. The aim of this study was to get sponge-associated bacteria extract containing antimicrobial activities. On the basis screening of antimicrobial activity using by streaking on agar medium, there were two potential isolates with antimicrobial activities namely LCS1 and LCS2. The two isolates were cultivated,then secondary metabolite product were extracted using methanol as a solvent. Minimum inhibitory concentrations (MICs) of extract LCS 1 were 1,000 μg/well for S. aureus, 950 μg/well for Salmonella sp.and 800 μg/well for Bacillus subtilis. Minimum inhibitory concentrations of extract LCS 2 were 500 μg/well for S. aureus, 1,050 μg/well for Salmonella sp., 750 μg/well for Bacillus subtilis, 350 μg/well for P. aeruginosa, 750 μg/sumur terhadap B. subtilis. Based on the MIC values, the two assay extracts have a relatively low antimicrobial activity.</p> <p>Keywords:Antimicrobial,Sponges associated bacteria,MICs</p>

Synthesis, characterization and antimicrobial activities of 1,5-dimethyl-2-phenyl-4-(pyrolidin-2-ylideneamino)-pyrazolidin-3-one and complex with iron(II)

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Condensation Reaction ◽  
Physical Method ◽  
Antimicrobial Activities ◽  
Multifunctional Ligand

A multifunctional ligand derivative of pyrrolidone has been synthesized by condensation reaction between 4-aminoantipyrine and 2-pyrrolidinone. The ligand and its Iron(II) complex were characterized using physical method and UV and IR techniques. The ligand and Fe(II) complex were tested against broad spectrums of bacterial organisms and the results show that both the ligand and complex were active against various organisms tested.

Synthesis of 3-(Cyclohexylamino)-2-arylimidazo[1,2-a]pyridine-8- carboxylic Acids Via an Efficient Three-component Condensation Reaction between Cyclohexylisocyanide and 2-Aminopyridine-3-carboxylic Acid in the Presence of Aromatic Aldehyde

2018 ◽  
Vol 21 (4) ◽  
pp. 298-301 ◽  
Author(s):  
Ghasem Marandi
Keyword(s):  
Biological Sciences ◽  
Carboxylic Acid ◽  
Carboxylic Acids ◽  
High Performance ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
New Materials ◽  
One Pot ◽  
High Yields ◽  
Benzaldehyde Derivatives

Aim and Objective: The reaction of cyclohexylisocyanide and 2-aminopyridine-3- carboxylic acid in the presence of benzaldehyde derivatives in ethanol led to 3-(cyclohexylamino)-2- arylimidazo[1,2-a]pyridine-8-carboxylic acids in high yields. In a three component condensation reaction, isocyanide reacts with 2-aminopyridine-3-carboxylic acid and aromatic aldehydes without any prior activation. Material and Methods: The synthesized products have stable structures which have been characterized by IR, 1H, 13C and Mass spectroscopy as well as CHN-O analysis. Results: In continuation of our attempts to develop simple one-pot routes for the synthesis of 3- (cyclohexylamino)-2-arylimidazo[1,2-a]pyridine-8-carboxylic acids, aromatic aldehydes with divers substituted show a high performance. Conclusion: In conclusion, this study introduces the art of combinatorial chemistry using a simple one-pot procedure for the synthesis of new materials which are interesting compounds in medicinal and biological sciences.

Punica granatum as a Source of Natural Antioxidant and Antimicrobial Agent; a Comprehensive Review on Related Investigations

2020 ◽  
Vol 17 ◽  
Author(s):  
Atefeh Jalali ◽  
Mohammadreza Kiafar ◽  
Masih Seddigh ◽  
Mohammad M. Zarshenas
Keyword(s):  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Natural Antioxidants ◽  
Punica Granatum ◽  
Antimicrobial Activities ◽  
Natural Antioxidant ◽  
Antiviral Activities ◽  
Natural Foods

Background: The consumption of natural antioxidants is increasing due to the demand and tendency to natural foods. Punica granatum L. [Punicaceae] is a fruit with various bioactive ingredients. The effectiveness of this plant has been proved against various disorders such as hyperglycemia, hyperlipidemia, blood coagulation, infections, cancer, and dentistry. Among them, there are numerous researches on antimicrobial and antioxidant properties. Subsequently, the present study aimed to compile a review of those properties to outline this herb as a possible natural antioxidant and preservative. Methods: Synchronically, keywords "Punica granatum" with antimicrobial, or antibacterial, antifungal, antiviral, antioxidant and radical scavenging were searched through "Scopus" database up to 31st September 2019. Papers focusing on agriculture, genetics, chemistry, and environmental sciences were excluded and also related papers were collected. Results: Among 201 papers focusing on related activities, 111 papers have dealt with antioxidant activities focusing based on DPPH assay, 59 with antibacterial, on both gram+ and gram- bacteria, 24 with antifungal effects, mostly on Aspergillus niger and Candida albicans, and 7 papers with antiviral activities. There were about 50 papers focusing on in-vivo antioxidant activities of this plant. Conclusion: Taken together, botanical parts of P. granatum have possessed notable radical scavenging and antimicrobial activities that with these properties, this plant can be introduced as a natural safe source of preservative and antioxidant. Accordingly, P. granatum can be applied as excipient with the aforementioned properties in the pharmaceutical and food industries.

New Potential Biologically Active Compounds: Synthesis and Characterization of Urea and Thiourea Derivativpes Bearing 1,2,4-oxadiazole Ring

2020 ◽  
Vol 17 (7) ◽  
pp. 525-534 ◽  
Author(s):  
Nevin Arıkan Ölmez ◽  
Faryal Waseer
Keyword(s):  
Microwave Irradiation ◽  
Room Temperature ◽  
Antimicrobial Activities ◽  
Phenyl Isocyanate ◽  
Single Step ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Thiourea Derivatives ◽  
Acyl Chlorides

Background: Urea, thiourea, and 1,2,4-oxadiazole compounds are of great interest due to their different activities such as anti-inflammatory, antiviral, analgesic, fungicidal, herbicidal, diuretic, antihelminthic and antitumor along with antimicrobial activities. Objective: In this work, we provide a new series of potential biologically active compounds containing both 1,2,4-oxadiazole and urea/thiouprea moiety. Materials and Methods: Firstly, 5-chloromethyl-3-aryl-1,2,4-oxadiazoles (3a-j) were synthesized from the reaction of different substituted amidoximes (2a-j) and chloroacetyl chloride in the presence of pyridine by conventional and microwave-assisted methods. In the conventional method, 1,2,4-oxadiazoles were obtained in two steps. O-acylamidoximes obtained in the first step at room temperature were heated in toluene for an average of one hour to obtain 1,2,4-oxadiazoles. The yields varied from 70 to 96 %. 1,2,4-oxadiazoles were obtained under microwave irradiation in a single step in a 90-98 % yield at 160 °C in five minutes. 5-aminomethyl-3-aryl-1,2,4- oxadiazoles (5a-j) were obtained by Gabriel amine synthesis in two steps from corresponding 5-chloromethyl-3- aryl-1,2,4-oxadiazoles. Finally, twenty new urea (6a-j) and thiourea (7a-j) compounds bearing oxadiazole ring were synthesized by reacting 5-aminomethyl-3-aryl-1,2,4-oxadiazoles with phenyl isocyanate and isothiocyanate in tetrahydrofuran (THF) at room temperature with average yields (40-70%). Results and Discussions: An efficient and rapid method for the synthesis of 1,2,4-oxadiazoles from the reaction of amidoximes and acyl halides without using any coupling reagent under microwave irradiation has been developed, and twenty new urea/thiourea compounds bearing 1,2,4-oxadiazole ring have been synthesized and characterized. Conclusion: We have synthesized a new series of urea/thiourea derivatives bearing 1,2,4-oxadiazole ring. Also facile synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from amidoximes and acyl chlorides under microwave irradiation was reported. The compounds were characterized using FTIR, 1H NMR, 13C NMR, and elemental analysis techniques.

Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Antimicrobial Agents ◽  
Pyrimidine Ring ◽  
Antimicrobial Activities ◽  
Screening Methods ◽  
Chlorpheniramine Maleate ◽  
In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

scholarly journals Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety

RSC Advances ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 2905-2916
Author(s):  
Mounir A. A. Mohamed ◽  
Adnan A. Bekhit ◽  
Omyma A. Abd Allah ◽  
Asmaa M. Kadry ◽  
Tamer M. Ibrahim ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Amino Acid ◽  
Green Chemistry ◽  
Antimicrobial Activities ◽  
Amino Acid Derivatives ◽  
Acid Moiety ◽  
Amino Acid Moiety

A new series of [1,2,4]-triazole bearing amino acid derivatives were synthesized under green chemistry conditions and evaluated for their antimicrobial activities.

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