Genotoxicity, antifungal and antibacterial activity of newly synthesized<i>N</i>-(3-phthalidyl)amines and<i>o</i>-benzoyl benzamide derivatives

Maslat, Ahmed O.; Al-Hamdany, R.; Fataftah, Zacharia A.; Mahrath, Alaa J.; Abussaud, Mahmoud J.

doi:10.1080/02772240410001665490

Cited by 5 publications

(5 citation statements)

References 14 publications

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“…However, one might be able to trap it by participation of a neighboring nucleophilic group. To this end, sodium 2-formylbenzoate was reacted with one equivalent of en 2 N 3 in CD 3 CN/D 2 O (7:3 v/v) and compared to the reaction with propylamine and C 2 -DA (see SI, part 6 for experimental details) . While propylamine and C 2 -DA give only imine, a new peak appeared at 5.12 ppm in the reaction with en 2 N 3 (Figure .).…”

Section: Resultsmentioning

confidence: 99%

Merging Constitutional and Motional Covalent Dynamics in Reversible Imine Formation and Exchange Processes

2012

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The formation and exchange processes of imines of salicylaldehyde, pyridine-2-carboxaldehyde, and benzaldehyde have been studied, showing that the former has features of particular interest for dynamic covalent chemistry, displaying high efficiency and fast rates. The monoimines formed with aliphatic α,ω-diamines display an internal exchange process of self-transimination type, inducing a local motion of either "stepping-in-place" or "single-step" type by bond interchange, whose rate decreases rapidly with the distance of the terminal amino groups. Control of the speed of the process over a wide range may be achieved by substituents, solvent composition, and temperature. These monoimines also undergo intermolecular exchange, thus merging motional and constitutional covalent behavior within the same molecule. With polyamines, the monoimines formed execute internal motions that have been characterized by extensive one-dimensional, two-dimensional, and EXSY proton NMR studies. In particular, with linear polyamines, nondirectional displacement occurs by shifting of the aldehyde residue along the polyamine chain serving as molecular track. Imines thus behave as simple prototypes of systems displaying relative motions of molecular moieties, a subject of high current interest in the investigation of synthetic and biological molecular motors. The motional processes described are of dynamic covalent nature and take place without change in molecular constitution. They thus represent a category of dynamic covalent motions, resulting from reversible covalent bond formation and dissociation. They extend dynamic covalent chemistry into the area of molecular motions. A major further step will be to achieve control of directionality. The results reported here for imines open wide perspectives, together with other chemical groups, for the implementation of such features in multifunctional molecules toward the design of molecular devices presenting a complex combination of motional and constitutional dynamic behaviors.

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Section: Resultsmentioning

confidence: 99%

Merging Constitutional and Motional Covalent Dynamics in Reversible Imine Formation and Exchange Processes

2012

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“…Ketals of this type have recently been shown to have antibacterial, antifungal and even mild genotoxic activity. 19 The presence of an electrophilic aldehyde in the above reaction adds the possibility of a cascade cyclisation to eventually form a seven-membered lactone, but such a product was not observed. The use of the dicarboxylic acids -phthalic and succinic -was taken up next; both reactions led to the formation of interesting bis-adducts 3n and 3o, with the aromatic acid proving much more efficient than the aliphatic analogue.…”

Section: Syn Lettmentioning

confidence: 98%

A Nucleophilic Activation of Carboxylic Acids by Proline: Oxa-Michael Addition to Methyl Vinyl Ketone under Solvent-Free Conditions

Jha

Inani

2017

Synlett

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A serendipitous nucleophilic activation of carboxylic acids by proline helped to achieve a direct hydrocarboxylation of methyl vinyl ketone at 60 °C under solvent-free conditions. A variety of carboxylic acids were used successfully in this oxa-Michael addition, affording useful 4-acyloxy-2-butanones in moderate yields. The reactions are carried out under solvent-free conditions, and the products are isolated in high purity by a simple work-up procedure without any need for column chromatographic purification, imparting a green quotient to the protocol. A heterodimeric non-covalent interaction between the amino acid and the carboxylic acid appears to be the most plausible mechanistic interpretation for the nucleophilic activation; additionally, the possible activation of the Michael acceptor by iminium ion formation presents an interesting case of proline acting as a bifunctional catalyst.

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“…All the compounds are evaluated for their antibacterial activity against Escherichia coli, Staphylococcus aureus, Micrococcus luteus and Klebsiella pneumonia and antifungal activity against Candida albicans and C. neoformansat 100µg/ml concentration. The zone of inhibition of each compound was determined and compared with standard drug fluconazole [44] . The compounds exhibited good antimicrobial activity [45] .…”

Section: Antimicrobial Activitymentioning

confidence: 99%

Synthesis, Evaluation and Pharmacological action of Oxadiazole derivatives

Meher¹,

Nayak²,

Singh³

et al. 2020

J Pharmacogn Phytochem

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Impacted numerous drug discovery programs including-muscarinic antagonists, benzodiazepine receptor partial agonists, Dopamine transporters, antirhinovirals, growth hormone secretagogues, 5-HT antagonists, antispasmodics. Heterocyclic compounds possess diverse biological properties that have led to intense study and research of these compounds. One of these compounds is Oxadiazole which has been found to exhibit various pharmacological activities. 1, 3, 4-oxadiazole having heterocyclic nucleus is a novel molecule which attract the chemist to search for a new therapeutic molecule. 1,3,4-oxadizole exhibited a wide range of biological activities which includes antibacterial, anti-tubercular, anticonvulsant, hypoglycemic, anti-allergic, enzyme inhibitor, vasodialatory, antifungal, cytotoxic, antiinflammatory, analgesic, hypolipidemic, anticancer, insecticidal, ulcerogenic activities etc. Out of the various derivative 2, 5-Disubstituted-1, 3, 4-oxadiazole is a widely exploited for various application. A large number of drugs used clinically have oxadiazole ring as a structural building block. The capacity of 1,3,4-oxadiazole nucleus to undergo variety of chemical reactions including electrophilic substitution, nucleophilic substitution, thermal and photochemical which make it medicinal backbone on which a number of potential molecules can be constructed. This review has basic information about 2, 5disubstituted-1, 3, 4-oxadiazole derivatives published in various journals for further development in the field. Oxadiazole derivatives are a class of heterocyclic compounds. The titled compounds were synthesized according to the procedures as given in the methodology. The reactions were monitored by TLC. The physical constants like melting point and solubility were determined for all the intermediates and final products. The compounds were further characterized by IR and 1H NMR and mass spectra. All the titled compounds were evaluated for their Anticonvulsant, Anti-inflammatory, Antibacterial, Antitubercular and Antioxidant activity.

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Genotoxicity, antifungal and antibacterial activity of newly synthesizedN-(3-phthalidyl)amines ando-benzoyl benzamide derivatives

Cited by 5 publications

References 14 publications

Merging Constitutional and Motional Covalent Dynamics in Reversible Imine Formation and Exchange Processes

Merging Constitutional and Motional Covalent Dynamics in Reversible Imine Formation and Exchange Processes

A Nucleophilic Activation of Carboxylic Acids by Proline: Oxa-Michael Addition to Methyl Vinyl Ketone under Solvent-Free Conditions

Synthesis, Evaluation and Pharmacological action of Oxadiazole derivatives

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