scholarly journals SYNTHESIS AND CHARACTERIZATION OF 3-ARYL-5H,13AH-QUINOLINO(3,2-F) (1,2,4)TRIAZOLO(4,3-B)(1,2-DIAZA-4-SULPHO)AZEPINES: IN VITRO ANTIFUNGAL AND ANTIBACTERIAL ACTIVITY

2011 ◽  
Vol 11 (2) ◽  
pp. 148-153
Author(s):  
Hemant Panwar ◽  
Shishupal Singh

3-Aryl-5H,13aH-quinolino(3,2-f)(1,2,4)triazolo(4,3-b)(1,2-diaza-4-sulpho)azepines [2a-i] have been prepared by the cyclisation of 5-aryl-4-amino-3-mercapto-1,2,4-triazole by reaction with 2-chloro-3-formylquinoline in catalytic presence of p-toluene sulphonic acid. All the synthesized compounds have been characterized by elemental and spectral (IR, 1H- NMR and Mass) analysis. Furthermore, all compounds were evaluated for their antibacterial and antifungal activities against selected panel of pathogenic strains. Ampicillin trihydrate and fluconazole were used as standard drugs for antibacterial and antifungal activity, respectively. 3-(2-Chloro)phenyl-5H,13aH-quinolino(3,2-f)(1,2,4)triazolo(4,3-b)(1,2-diaza-4-sulpho)azepine [2h] was found, one of the most potent with lesser toxicity among the all prepared thiazepine derivatives.

Author(s):  
A. Raguraman ◽  
N. Santhi

A series of novel 1,3,5-trisubstituted pyrazoline derivatives (P1-P10) have been synthesized by the reaction of substituted chalcones (C1-C10) with 4-hydroxybenzhydrazide. The starting material, chalcones were prepared by claisen Schmidt condensation of 4-methylacetophenone with substituted aldehydes in the presence of sodium hydroxide in ethanol. 4-hydroxybenzhydrazide was synthesized by condensing methyl 4-hydroxybenzoate with hydrazine hydrate. The cycloaddition of chalcones with 4-hydroxybenzhydrazide gives 1, 3, 5-trisubstituted pyrazoline derivatives. The structures of synthesized derivatives were confirmed by IR, 1HNMR and 13C NMR spectrum. The synthesized compounds were screened for their antibacterial and antifungal activity.


2020 ◽  
Vol 1211 ◽  
pp. 128107 ◽  
Author(s):  
Akhilash Mohanan Pillai ◽  
Vishnu Sankar Sivasankarapillai ◽  
Abbas Rahdar ◽  
Jithu Joseph ◽  
Fardin Sadeghfar ◽  
...  

Author(s):  
Nirali S. Mewada ◽  
Dhruvin R. Shah ◽  
Kishor H. Chikhalia

Three series of some novel chalcone based urea, thiourea and acetamide derivatives were designed, synthesized and screened for their antimicrobial and antifungal activities. All the synthesized compounds are first reported. The structures of the compounds were elucidated with the aid of elemental analysis and spectral methods including IR, 1H-NMR spectral data. The prepared compounds were evaluated for antibacterial activity against two Gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus), two Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also investigated for their antifungal activity using the broth micro dilution method. The bioassay results showed that compounds a few compounds showed good to superior in vitro antibacterial and antifungal activity.


2009 ◽  
Vol 63 (5) ◽  
Author(s):  
Gülşah Kurt ◽  
Fatih Sevgi ◽  
Bedrettin Mercimek

AbstractIn this study, new benzoylthiourea derivatives, (E)-N-[(2-benzamidomethyleneamino)ethylcarbamothioyl]benzamide H3L′, N-(1-(3-benzoylthioureido)propan-2-ylcarbamothioyl)-benzamide H4L″, (E)-N-[4-(benzamidomethyleneamino)phenylcarbamothioyl]benzamide H3L‴, were synthesized. Structures of the compounds were identified by spectroscopic techniques. In addition, all synthesized compounds were evaluated for in vitro antibacterial and antifungal activity. Compound H3L‴ exhibited antibacterial activity.


Medicina ◽  
2011 ◽  
Vol 47 (6) ◽  
pp. 47
Author(s):  
Vilma Petrikaitė ◽  
Eduardas Tarasevičius ◽  
Alvydas Pavilonis

Objective. The aim of this study was to evaluate the influence of pharmacophores having naphthylamine and nitro groups on the antimicrobial (antibacterial and antifungal) activity of thiazolidinone derivatives. Materials and Methods. The initial 5-substituted-2-methylmercaptothiazolidin-4-ones were subjected to S-demethylation to yield 2-amino-substituted thiazolidinones. 4-Nitro-1-naphthylamine, nitrofuran aldehydes, and nitrobenzene aldehydes were used as pharmacophoric compounds having amino or aldehyde groups. Antimicrobial (antibacterial and antifungal) activity of the new compounds was tested in vitro against bacterial cultures – Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Klebsiella pneumoniae – and fungal cultures – Candida albicans, Candida glabrata, Candida krusei, Candida kefyr, Candida tropicalis, and Candida parapsilosis. Results. Microbiological analysis showed that all new thiazolidinone derivatives with nitronaphthylamine substituent possessed antibacterial and antifungal properties. New compounds 2a-b showed similar antibacterial activity in vitro against S. aureus and B. subtilis as aminopenicillins. The lowest antibacterial activity of all newly synthesized compounds was against capsule-forming bacteria K. pneumoniae and against gram-negative bacteria E. coli (minimum inhibitory concentration range, 500–1000 μg/mL). Conclusions. The minimum inhibitory concentration of naphthylamine derivatives varied in the range of 0.4–1000 μg/mL, and activity of some newly synthesized compounds was similar to the activity of aminopenicillins and fluconazole, an antifungal preparation. Based on the results, it is possible to separate the perspective group of potential antimicrobial compounds.


2021 ◽  
pp. 3307-3322
Author(s):  
Muath Jabbar Tarfa Al-Abbasee ◽  
Ahmood khalaf Jebur ◽  
Afraa Sabir Shihab

    Some new tropylidene derivatives were prepared in this work and their in vitro antibacterial and antifungal activities were studied. All the prepared compounds were characterized by their physical properties, such as melting point and color, and chemical properties, using the techniques of FT-IR, 1H-NMR and 13C-NMR.


2015 ◽  
Vol 80 (7) ◽  
pp. 839-852 ◽  
Author(s):  
Nina Bozinovic ◽  
Irena Novakovic ◽  
Sladjana Kostic-Rajacic ◽  
Igor Opsenica ◽  
Bogdan Solaja

A series of new 5H-pyridobenzazepine and pyridobenzothiepine derivatives was synthesized by Pd-catalyzed formation of C-N and C-S bonds. All synthesized compounds were tested for their in vitro antimicrobial activity. The 5H-pyridobenzazepine derivatives showed better antibacterial and antifungal activity than corresponding 5H-dipyridoazepine analogs. Among the synthesized azepines, derivative 8 displayed potent activity against tested bacteria (MIC = 39-78 ?g/mL), while azepine 12 showed promising antifungal activity (MIC = 156-313 ?g/mL). The synthesized thiepine derivatives exhibited weak antibacterial activity, but showed pronounced antifungal activity.


2005 ◽  
Vol 60 (9-10) ◽  
pp. 686-692
Author(s):  
Ismail Kiran ◽  
Semra Ilhan ◽  
Tamer Akar ◽  
Lacine Tur ◽  
Erdinc Erol

Abstract The in vitro antibacterial and antifungal activities of demethoxyviridin and some synthetic analogues were evaluated by the agar diffusion method. The minimum inhibitory concentrations (MIC) of the active compounds were also determined by the agar dilution method. Demethoxyviridin (1) showed moderate antibacterial activity against most of the strains tested. 1α-Hydroxydemethoxyviridin (3) showed antibacterial activity and the most potent in vitro antifungal activity with MIC of 20 μg/ml (0.062 mm) against Aspergillus niger, A. fumigatus, A. flavus, A. parasiticus, Fusarium solani, F. graminarum, Geotrichum candidum whereas 5′-methylfuro-(4′,3′,2′-4,5,6)androst-5-ene-3,17-dione (7) exhibited very weak antifungal activity against Candida albicans only.


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