Synthesis and Antimycobacterial Activity of 2 …
In according with our goal, we decide to study the influence concerning syntheses and biological activity of rationally substituted imidazols. The synthesis of the desired imidazolium salts occurred in several steps. In the first step we synthesize the dihydroxyacetophenone part, namely 2-chloro-3’,4`-dihydroxyacetophenone, using a Friedel – Crafts acylation reaction of pyrochatecol with haloacylchloride. In a subsequent step, we carried out the -cyanoethylation of the acidic nitrogen from imidazol derivatives (imidazole and benzimidazole) Michael addition of acrylonitrile.
Feyzmohammadi R, Kazemi M, Shafiee A
Similarly 1, 2, 4-triazole 96 coupled with halovinyl aldehyde 98 resulted in thiadizapine derivatives 100 (Scheme 27) .Scheme 26
Scheme 27Some of the synthesized compounds displayed good antifungal activity.Replacement of hydrogenThe reaction of 5-(1-adamantyl)-4-phenyl-1, 2, 4-triazoline-3-thione 101 with formaldehyde and 1-substituted piperazines yielded the corresponding N-Mannich bases 102 (Scheme 28) .1, 2, 4-triazole 101 was treated with piperizine and formaldehyde afforded N-Mannich base 102.
Taking into consideration the promising antimycobacterial activity of some fused pyridine derivatives, as well as our previous results in the field of anti-TB derivatives; we have focused on the design of novel structures that incorporate a bis-fused pyridine unit in the molecular scaffold. In this respect, we chose 4,4’-bipyridine heterocycle as main skeleton for synthesis of mono-indolizines, bis-indolizines and mono-indolizine mono-salts derivatives. In equal measure we were interested to study the influence of the fused-pyridine substituents concerning the antimycobacterial activity, Scheme 3.
28/05/2011 · The antimycobacterial activity ..
“Gold Medal”. Lucrare premiata: „Hybrid imidazole / pyridine (quinoline) derivatives with anticancer and antimycobacterial activity”, Euroinvent 2016, Iasi, Romania;
Synthesis, antimycobacterial, antiviral, antimicrobial activities, ..
Hybrid imidazole / pyridine (quinoline) derivatives with anticancer and antimycobacterial activity, European Exhibition of Creativity and Invovation, Euroinvent 2016, May 19-21 2016, Iasi, Romania.
Synthesis, antifungal and antimycobacterial activities of …
The compounds which have activity comparable to the standard drug ibuprofen were screened for their analgesic, ulcerogenic, lipid peroxidation and hepatotoxic effects.Preparation of diazonium salts and reaction with aromatic aminesGoyal et al. synthesized some new derivatives of 3-substituted-4H-1, 2, 4-triazoles 115 by the reaction of 5-alkyl/aryl diazo-substituted 4H-1, 2, 4-triazoles-3-thiol 114 with different aliphatic and aromatic amines (Scheme 31) .The anti-inflammatory activity of synthesized compounds 115 was determined against carrageenan induced acute paw edema in albino rats.Reaction with 3-substituted pyrazole acidArun M.
Antifungal and antimycobacterial activity of ..
Seven 4-Oxo-imidazolidin-2-thione derivatives have been synthesized. The mass spectral fragmentation patterns of prepared compounds have been investigated. antimicrobial activities of all synthesized compounds have been evaluated against five strains of bacterial culture and two fungi. Almost compounds show very good activity. All tested compounds showed high activity against human breast carcinoma cell line (MCF-7). Compounds 5 and 6 are most active members with Median Inhibition Concentration (IC50) 9.45 and 11.1 μg mL1, respectively.
Synthesis and anti(myco)bacterial activity ..
Condensed heterocyclic systems containing imidazole, benzimidazole, oxadiazole, thiadiazole, pyarazole, isoxazole, pyrimidine, diazepine, oxazepine, thiazepine nuclei have attracted the attention of chemists, on account of the significant medicinal properties associated with them. In view of the prodigious range of activities of these compounds, it was considered worthwhile in the present work to undertake investigation on the synthesis of condensed nitrogen-sulfur heterocyclic systems containing above nuclei fused to the s-Triazine neuleus. It was hoped that synthesis of these condensed heteocyclic systems and evaluation of their biological properties would provide a rational approach to the study of structure activity relationship of these molecules.