scholarly journals Design, Synthesis, Spectroscopic Characterization of New Pyrazole Carbothioamides as Antifungal and Antibacterial Candidates

2021 ◽  
Vol 11 (3) ◽  
pp. 3689-3699
Keyword(s):  
Room Temperature ◽  
Antimicrobial Agents ◽  
Spectroscopic Analysis ◽  
Spectroscopic Characterization ◽  
Efficient Synthesis ◽  
Design Synthesis ◽  
Amberlyst 15 ◽  
New Compounds

In a sustained search for novel antimicrobial agents as weaponry in the war against infectious diseases, resulting in improved survivability for both humans and their domestic animals, the present study demonstrates an efficient synthesis of N,N-dimethylaminophenyl substituted pyrazole carbothioamide derivatives. The synthesis involves (3+2) cycloaddition of chalcones with hydrazinecarbothioamide hydrochloride in the presence of the amberlyst-15 catalyzed at room temperature. The structures of new compounds were characterized by spectroscopic analysis. Furthermore, the synthesized new compounds 5(a-g) were assessed in vitro for their antimicrobial susceptibilities. The results indicate that compounds 5a found potent against tested bacteria species; 5b and 5c show excellent inhibition against the tested fungi and bacteria species. Therefore, these could act as antifungal and antibacterial leads for further investigations.

scholarly journals Synthesis and NMR spectroscopic characterization of Si-substituted 1-silacyclobutene derivatives

2011 ◽  
Vol 9 (1) ◽  
pp. 126-132 ◽  
Author(s):  
Ezzat Khan ◽  
Bernd Wrackmeyer
Keyword(s):  
Magnetic Resonance ◽  
Room Temperature ◽  
Spectroscopic Characterization ◽  
The Other ◽  
Resonance Spectroscopy ◽  
29Si Nmr ◽  
Reaction Conditions ◽  
New Compounds ◽  
Substituted 1

AbstractHydroboration of trialkyn-1-yl(organo)silanes with one equivalent and two equivalents of 9-borabicyclo[3.3.1]nonane, 9-BBN afford dialkyn-1-ylsilanes and alkyn-1-ylsilanes, respectively. The alkyn-1-ylsilane derivatives are stable at room temperature and can be store under dry argon for prolong period of time. These compounds are attractive materials for further rearrangements to afford novel 1-silacyclobutene derivatives bearing Si-alkenyl or Si-alkynyl functionalities. The hydroboration reaction is well controlled by the Si-R1 function, i.e., the starting silanes with R1 = Ph selectively afford hydroboration of one Si-C≡C bond with one equivalent of 9-BBN, leaving the other two functionalities untouched. Under mild reaction conditions (25°C), the starting silanes with R1 = Me lead to mixture containing dialkyn-1-ylsilane, alkyn-1-ylsilane and their respective 1-silacyclobutene derivatives. All new compounds are sensitive towards air and moisture and were studied by multinuclear magnetic resonance spectroscopy (1H, 13C, 11B, 29Si NMR) in solution.

scholarly journals An Efficient Synthesis of Thiophene Conjugated Benzothiazepines: in vitro Screening for their Antimicrobial Activity

2020 ◽  
Vol 32 (10) ◽  
pp. 2601-2605
Author(s):  
K.R. Raghavendra ◽  
P. Sudeep ◽  
K. Ajay Kumar ◽  
H.P. Jayadevappa
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Spectroscopic Studies ◽  
In Vitro Screening ◽  
Efficient Synthesis ◽  
Citrus Juice ◽  
E Coli ◽  
Antimicrobial Evaluation ◽  
New Compounds

A series of novel thiophene conjugated benzothiazepines were synthesized by the reaction of chalcones with 2-aminobenzenethiol in citrus juice medium. The new compounds were characterized by spectroscopic studies. Results of in vitro antimicrobial evaluation of newly synthesized compounds 5a-j shows that the compounds 5a and 5c have excellent antimicrobial inhibition in the range of 12.5-25.0 μg/mL against bacteria S. aureus, E. coli, P. aeruginosa and fungi A. niger, A. flavus organisms comparable to ciprofloxacin and nystatin and therefore these compounds might acts as lead molecules as antimicrobial agents.

scholarly journals An efficient synthesis and spectroscopic characterization of Schiff bases containing 9,10-anthracenedione moiety

2013 ◽  
Vol 78 (4) ◽  
pp. 477-482
Author(s):  
Ghulam Fareed ◽  
Ali Versiani ◽  
Nighat Afza ◽  
Nazia Fareed ◽  
Irfan Ali ◽  
...  
Keyword(s):  
Green Chemistry ◽  
Schiff Bases ◽  
1H Nmr ◽  
13C Nmr ◽  
Room Temperature ◽  
Spectroscopic Characterization ◽  
Efficient Synthesis ◽  
Tungstosilicic Acid ◽  
Solvent Free Conditions

A new method has been developed for the synthesis of novel Schiff bases containg anthraquinone moiety using dodeca-Tungstosilicic acid/P2O5 under solvent free conditions at room temperature. The reaction was completed in 1-3 minutes with excellent yields. This method was found to be more efficient, easy and hazardous free for the synthesis of azomethines. The development of these type of methadologies in synthetic chemistry may contribute to green chemistry. The structures of synthesized novel Schiff bases was elucidated using 1H-NMR, 13C-NMR, LCMS, FTIR and CHN analysis.

scholarly journals Design, synthesis, in vitro and in silico characterization of new 2‐quinolone‐ L ‐alaninate‐1,2,3‐triazoles as novel antimicrobial agents

ChemMedChem ◽  
2022 ◽  
Author(s):  
Oussama Moussaoui ◽  
Rajendra Bhadane ◽  
Riham Sghyar ◽  
Janez Ilaš ◽  
El Mestafa El Hadrami ◽  
...  
Keyword(s):  
In Silico ◽  
Antimicrobial Agents ◽  
Design Synthesis ◽  
In Silico Characterization

Design, synthesis and characterization of new 1,2,3-triazolyl pyrazole derivatives as potential antimicrobial agents via a Vilsmeier–Haack reaction approach

RSC Advances ◽  
2016 ◽  
Vol 6 (64) ◽  
pp. 59375-59388 ◽  
Author(s):  
Manjunatha Bhat ◽  
Nagaraja G. K. ◽  
Reshma Kayarmar ◽  
Peethamber S. K. ◽  
Mohammed Shafeeulla R
Keyword(s):  
Antimicrobial Agents ◽  
Synthesis And Characterization ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Anti Oxidant ◽  
Anti Fungal

A new series of 1,2,3-triazolyl pyrazole derivatives were synthesisedviaa Vilsmeier–Haack reaction approach and screened for theirin vitroanti-bacterial, anti-fungal and anti-oxidant activities.

scholarly journals Chemical Derivatization and Characterization of Novel Antitrypanosomals for African Trypanosomiasis

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4488
Author(s):  
Aboagye Kwarteng Dofuor ◽  
Temitayo Samson Ademolue ◽  
Cynthia Mmalebna Amisigo ◽  
Kwaku Kyeremeh ◽  
Theresa Manful Gwira
Keyword(s):  
Structural Modification ◽  
Spectroscopic Analysis ◽  
Microscopic Analysis ◽  
The Novel ◽  
Chemical Derivatization ◽  
African Trypanosomiasis ◽  
Chemical Structures ◽  
Normal Ratio

The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.

Design, Synthesis and Evaluate In Vitro Antifungal Activity of Novel Benzamide Derivatives

2019 ◽  
Vol 41 (3) ◽  
pp. 549-549
Author(s):  
Xuesong Wang and Xiaorong Tang Xuesong Wang and Xiaorong Tang
Keyword(s):  
Antifungal Activity ◽  
Pathogenic Fungi ◽  
Gibberella Zeae ◽  
Design Synthesis ◽  
Carboxylic Acid Amides ◽  
Almost All ◽  
Negative Controls ◽  
New Compounds ◽  
Benzamide Derivatives

A series of novel benzamide derivatives according to fluopicolide were designed and synthesized following the rule of combination carboxylic acid amides and amines derivatives together. The antifungal activity of the 15 new compounds were evaluated in vitro against five pathogenic fungi, including Sclerotinia sclerotiorum, Gibberella zeae, Rhizoctonia solani, Helminthosporium maydis and Botrytis cinerea. Almost all the structure have not been reported, except compounds 3, 5 and 6. A surprising finding is that all the five tested fungi breed faster than negative controls when supplementary with compound 715 , respectively.

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