728-97-2Relevant academic research and scientific papers
Synthesis, characterization, and biologic activity of new acyl hydrazides and 1,3,4-oxadiazole derivatives
Bleotu, Coralia,Diaconu, Carmen Cristina,Hanganu, Anamaria,Ionita, Petre,Limban, Carmen,Matei, Lilia,Nemes, Roxana Maria,Nicolau, Ioana,Nuta, Diana Camelia,P?un, Anca,Radulescu, Cristiana,Tatibou?t, Arnaud,Zarafu, Irina
, (2020/08/28)
Starting from isoniazid and carboxylic acids as precursors, thirteen new hydrazides and 1,3,4-oxadiazoles of 2-(4-substituted-phenoxymethyl)-benzoic acids were synthesized and characterized by appropriate means. Their biological properties were evaluated in terms of apoptosis, cell cycle blocking, and drug metabolism gene expression on HCT-8 and HT-29 cell lines. In vitro antimicrobial tests were performed by the microplate Alamar Blue assay for the anti-mycobacterial activities and an adapted agar disk diffusion technique for other non-tubercular bacterial strains. The best antibacterial activity (anti-Mycobacterium tuberculosis effects) was proved by 9. Compounds 7, 8, and 9 determined blocking of G1 phase. Compound 7 proved to be toxic, inducing apoptosis in 54percent of cells after 72 h, an effect that can be predicted by the increased expression of mRNA caspases 3 and 7 after 24 h. The influence of compounds on gene expression of enzymes implicated in drug metabolism indicates that synthesized compounds could be metabolized via other pathways than NAT2, spanning adverse effects of isoniazid. Compound 9 had the best antibacterial activity, being used as a disinfectant agent. Compounds 7, 8, and 9, seemed to have antitumor potential. Further studies on the action mechanism of these compounds on the cell cycle may bring new information regarding their biological activity.
Synthesis and evaluation of biological and nonlinear optical properties of some novel 2,4-disubstituted [1,3]-thiazoles carrying 2-(aryloxymethyl)-phenyl moiety
Naveena, Channamata Shankar,Poojary, Boja,Arulmoli, Thangavelu,Manjunatha, Kumshi,Prabhu, Ashwatanarayana,Kumari, Nalilu Sucheta
, p. 1925 - 1937 (2013/07/26)
A series of 2,4-disubstituted-[1,3]-thiazoles (4a-p and 6a-l) was synthesized from 2-(aryloxymethyl)benzoic acids (1a-d) through a multistep reaction sequence in good yield. The structures of the new compounds were established on the basis of their elemen
Synthesis and biological evaluation of some [1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles and [1,2,4]triazolo[3,4-b][1,3,4]thiadiazines
Naveenaa, Channamata Shankara,Poojary, Boja,Chandrashekhar, Chikkanna,Kumari, Nalilu Suchetha
experimental part, p. 189 - 200 (2012/02/14)
The reaction of 2-(aryloxymethyl)benzoic acid hydrazide with carbon disulfide in the presence of potassium hydroxide followed by hydrazine hydrate afforded 4-amino-3{2-(aryloxymethyl)pheny}[1,2,4]triazole-5-thiol (5a-d). The cyclo-condensation of 5a-d with various aromatic carboxylic acids in the presence of phosphorous oxychloride and with phenacyl bromides afforded two series of fused heterocycles namely; 6-substituted-3-{2-(aryloxymethyl)phenyl}- 1,2,4- triazolo[3,4-b][1,3,4]thiadizoles (6a-t) and 6-substituted-3-{2- (aryloxymethyl)phenyl)}[1,2,4]triazolo[3,4-b][1,3,4] thiadiazines (7a-p) respectively. The structures of these newly synthesized compounds were established on the basis of their IR, 1H-NMR 13C-NMR and Mass spectral data. All the title compounds were screened for their antimicrobial and antiinflammatory activities. Preliminary results indicated that some of them exhibit promising activities and they deserve more consideration as potential antimicrobial and anti-inflammatory agents.
Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivatives
Limban, Carmen,Marutescu, Luminita,Chifiriuc, Mariana Carmen
scheme or table, p. 7593 - 7607 (2011/11/06)
A number of acylthioureas, 2-((4-methylphenoxy)methyl)-N- (arylcarbamothioyl) benzamides (aryl = 3,5-dichlorophenyl, 2,3-dichlorophenyl, 3,4-dichlorophenyl, 2,4,5-trichlorophenyl, 3,4,5-trichlorophenyl, 2-bromophenyl, 2,4-dibromophenyl, 2,5-dibromophenyl,
Synthesis, characterization and antimicrobial activity of some disubstituted 1,3,4-oxadiazoles carrying 2-(aryloxymethyl)phenyl moiety
Naveena, Channamata Shankara,Boja, Poojary,Kumari, Nalilu Sucheta
experimental part, p. 4708 - 4719 (2010/11/16)
Disubstituted 1,3,4-oxadaiazoles (4a-z, 4a′-f′), Mannich bases (6a-p) and S-alkylated derivatives (7a-t) have been synthesized from 2-(aryloxymethyl)benzoic acids (1a-d) through a multi-step reaction sequence. The structures of new compounds were established on the basis of their elemental analyses, IR, 1H NMR, 13C NMR and mass spectral data. All the synthesized compounds were screened for their in vitro antibacterial and antifungal activity and some of them exhibited good activity.
New thioureides of 2-(4-methyl-phenoxymethyl)-benzoic and 2-(4-methoxy-phenoxymethyl)-benzoic acids with biological activity
Limban, Carmen,Missir, Alexandru-Vasile,Chirita, Ileana Cornelia,Badiceanu, Carmellina Daniela,Draghici, Constantin,Balotescu, Mariana Carmen,Stamatoiu, Oana
experimental part, p. 595 - 602 (2010/02/16)
The present application is a continuation of our research concerning the synthesis and characterization of thioureides of 2-(4-methyl-phenoxymethyl)- benzoic acid and 2-(4-methoxy-phenoxymethyl)-benzoic acid with biological activities. The new compounds,
Amide derivatives and nociceptin antagonists
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, (2008/06/13)
The present invention relates to a compound of the formula [1′] wherein R2is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.
4-Aminoquinolines: Novel nociceptin antagonists with analgesic activity
Shinkai,Ito,Iida,Kitao,Yamada,Uchida
, p. 4667 - 4677 (2007/10/03)
Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL1 receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated. Elucidation of structure - Activity relationships eventually led to the optimum compounds. One of these compounds, N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride (11) not only antagonized nociceptin-induced allodynia in mice but also showed analgesic effect in a hot plate test using mice and in a formalin test using rats. Its analgesic effect was not antagonized by the opioid antagonist naloxone. These results indicate that this nociceptin antagonist has the potential to become a novel type of analgesic that differs from μ-opioid agonists.
Antipsychotically useful quinolizidylidene derivatives of xanthenes, thioxanthenes and dibenzoxepins
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, (2008/06/13)
Tricyclic quinolizidine derivatives administered internally to an animal host, in therapeutically effective amounts, produce antipsychotic activity essentially free of extrapyramidal symptoms.
