New 2-chloro-7-methylquinoline amine analogues as possible antimycotic agents

A series of N-[(2-chloro-7-methylquinolin-3-yl)methyl]-(substituted)-aniline/butan-1-amine/cyclohexamine derivatives (4a-n) & N-benzyl-1-(2-chloro-7-methylquinolin-3-yl)methanamine (4o) was designed and synthesized based on the structural requirements essential for allylamine / benzylamine antimycotics. Compounds (4a-o) were synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-7- methylquinoline with substituted aromatic/aliphatic primary amine in absolute ethanol in presence of triethylamine. The structures of all new products were confirmed by IR, 1H & 13C-NMR and mass spectral data. The newly synthesized compounds were screened in-vitro for their antifungal activity against Aspergillus niger MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM 768 by cup plate method. Preliminary screening of compounds (4a-o) revealed that compounds viz. 4a, 4b, 4e, 4g, 4j and 4l showed excellent antifungal activity. Dihalogen and benzyl substituted compounds 4j, 4l & 4o exhibited potent antifungal activity. Replacement of phenyl ring with aliphatic groups like butyl or cyclohexyl causes substantial decrease in antifungal activity and activity decreases when phenyl ring is substituted with electron releasing groups.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis of Schiff’s bases of 8-methyl-tetrazolo[1,5-a]quinoline as potential anti-inflammatory and antimicrobial agents

142-145A series of 4-substituted–imino-methyltetrazolo[1,5-a]quinoline derivatives reported have been synthesized by condensation of 4-formyl-8-methyltetrazolo[1,5-a]quinoline with appropriate aromatic amine by refluxing in dioxane. All the compounds have been characterized by IR, ¹H NMR and mass spectroscopy and have been evaluated for their anti-inflammatory and antimicrobial activities

Syntheses and antiinflammatory activity of new α-pyronochalcones, α-pyronoflavones and related products from 8-acetylumbelliferone

1207-1214Fourteen new substituted α-pyronochalcones 4a-4n and five α-pyrononavanones 5a-5e have been obtained from 8-acetylumbelliferone. The enone function of substituted α-pyronochalcones has been further exploited for the syntheses of a pyronoflavones 6a-6c, pyrazolines <b style="mso-bidi-font-weight: normal">7a-7c, isoxazolines/isoxazoles 8a-8e. dihydroflavonol/flavonol 9a-9b, aminothiazole 11 and the Mannich base 12. Evaluation of these compounds for antiinflammatory activity against carrageenan induced rat's paw edema shows encouraging results

3-Chloro-4-fluoro-N-{[3-(4-methoxyphenyl)-1-phenyl-1H-pyrazol- 4-yl]methyl}aniline

A direct reductive amination of 3-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carbaldehyde 2 with 3-chloro-4-flouroaniline using NaBH4/I2 as a reducing agent is described. The reaction was carried out in MeOH under neutral conditions at room temperature to give the secondary amine, 3-chloro-4-fluoro-N-{[3-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl]methyl}aniline (3)

N-[(2-Chloro-6-methylquinolin-3-yl)methyl]aniline

Quinolinyl amines are important organic compounds which possess a variety of pharmacological activities such as antimalarial, antifungal, hypotensive and antidepressant activity

Mini review on tricyclic compounds as an inhibitor of trypanothione reductase

Trypanosomiasis and leishmaniasis are two most ruinous parasitic infectious diseases caused by Trypanosoma and Leishmania species. The disease affects millions of people all over the world and associated with high morbidity and mortality rates. The review discuss briefly on current treatment of these parasitic diseases and trypanothione reductase (TryR) as potential targets for rational drug design. The enzyme trypanothione reductase (TryR) has been identified as unique among these parasites and has been proposed to be an effective target against for developing new drugs. The researchers have selected this enzyme as target is due to its substrate specificity in contrast to human analogous glutathione reductase and its absence from the host cell which makes this enzyme an ideal target for drug discovery. In this review we have tried to present an overview of the different tricyclic compounds which are potent inhibitors of TryR with their inhibitory activities against the parasites are briefly discussed

Structural modifications of quinoline-based antimalarial agents: Recent developments

Antimalarial drugs constitute a major part of antiprotozoal drugs and have been in practice for a long time. Antimalarial agents generally belong to the class of quinoline which acts by interfering with heme metabolism. The recent increase in development of chloroquine-resistant strains of Plasmodium falciparum and failure of vaccination program against malaria have fuelled the drug discovery program against this old and widespread disease. Quinoline and its related derivative comprise a class of heterocycles, which has been exploited immensely than any other nucleus for the development of potent antimalarial agents. Various chemical modifications of quinoline have been attempted to achieve analogs with potent antimalarial properties against sensitive as well as resistant strains of Plasmodium sp., together with minimal potential undesirable side effects. This review outlines essentially some of the recent chemical modifications undertaken for the development of potent antimalarial agents based on quinoline