scholarly journals Synthesis and Neuropharmacological Evaluation of Some Novel Quinoxaline 2, 3-Dione Derivatives

2012 ◽  
Vol 2012 ◽  
pp. 1-8
Author(s):  
Selvaraj Jubie ◽  
Rajamanickam Gayathri ◽  
Rajagopal Kalirajan
Keyword(s):  
Ethidium Bromide ◽  
Neuromuscular Disorders ◽  
Mannich Bases ◽  
Screening Methods ◽  
Walk Test ◽  
Test Beam ◽  
Curative Effect ◽  
H Nmr ◽  
Cyclocondensation Reaction ◽  
Test Grip Strength

Quinoxaline-2, 3-dione obtained from cyclocondensation reaction of o-phenylene diamine with oxalic acid was reacted with three different ketones and formaldehyde to give the corresponding Mannich bases in satisfactory yield. Their structures were confirmed by using1H NMR, IR, and mass analysis. In pharmacological evaluation, the synthesized compounds showed its curative effect against ethidium-bromide-induced demyelination in rats. For the purpose, different screening methods such as open field exploratory behavior test, rota rod test, grip strength test, beam walk test, and photo actometer test were performed. Ethidium bromide induction showed muscle weakness; muscle discoordination; loss of locomotor activity, and so forth, the synthesized drugs reversed all the above-mentioned neuromuscular disorders caused by ethidium bromide administration.

scholarly journals Synthesis, Characterization, and Biological Activity of Novel Schiff and Mannich Bases of 4-Amino-3-(N-phthalimidomethyl)-1,2,4-triazole-5-thione

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Uzma Yunus ◽  
Moazzam H. Bhatti ◽  
Naima Rahman ◽  
Nosheen Mussarat ◽  
Shazia Asghar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Enterobacter Cloacae ◽  
Mannich Bases ◽  
Fungal Strain ◽  
Fine Tuning ◽  
Antimicrobial Compounds ◽  
Gram Negative ◽  
H Nmr ◽  
Positive Strain ◽  
C Nmr

The present work describes the syntheses and antimicrobial activity studies of a series of novel Schiff bases (4a–4i) and their Mannich bases (5a–5h) starting from 4-amino-3-(N-phthalimido-methyl)-1,2,4-triazole-5-thione (3). All the synthesized compounds were characterized by IR,1H-NMR,13C-NMR, and MS. All the synthesized compounds were screened for four Gram-negative strains, one Gram-positive strain of bacteria, and one diploid fungal strain. In general the antimicrobial activity increased remarkably on the introduction of azomethine functionality in parent triazole (3). The antimicrobial activity further improved when morpholine group was added to them except forEnterobacter cloacae, where loss of activity was observed. The results are promising and show that the fine tuning of the structures (5a, 5b, 5e, 5f,and5h) can lead to some new antimicrobial compounds.

Zirconium(IV) chloride-catalyzed synthesis of 1,5-benzodiazepine derivatives

2007 ◽  
Vol 85 (3) ◽  
pp. 184-188 ◽  
Author(s):  
K Srinivasa Reddy ◽  
Ch. Venkateshwar Reddy ◽  
M Mahesh ◽  
K Rosi Reddy ◽  
P VK Raju ◽  
...  
Keyword(s):  
Structural Elucidation ◽  
High Yield ◽  
Zirconium Tetrachloride ◽  
H Nmr ◽  
Cyclocondensation Reaction ◽  
Benzodiazepine Derivatives

Zirconium tetrachloride efficiently catalyzes the cyclocondensation reaction of o-phenylenediamine and a ketone in refluxing 1,2-dichloroethane to afford the corresponding 2,3-dihydro-1H-1,5-benzodiazepine in high yield. The formation of specific regioisomers and their structural elucidation are reported for the first time.Key words: zirconium tetrachloride, o-phenylenediamines, ketones, 1,5-benzodiazepines, 1H NMR, regioisomers.

scholarly journals Synthesis and Anticonvulsant Activity of Various Mannich and Schiff Bases of 1,5-Benzodiazepines

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Surendra N. Pandeya ◽  
Neha Rajput
Keyword(s):  
Schiff Bases ◽  
Anticonvulsant Activity ◽  
Gaba Receptor ◽  
Antidepressive Agents ◽  
Mannich Bases ◽  
Appetitive Behavior ◽  
H Nmr ◽  
Zirconia Catalyst ◽  
Sulfated Zirconia Catalyst ◽  
Gaba Receptor Complex

Benzodiazepines have a various behavioral effects in addition to their anxiolytic action. There is every reason to believe that the BZ/GABA receptor complex is involved in these effects, since GABAmimetic manipulations modify the effect of BZ in tests of convulsive activity, motor function, and appetitive behavior. 1,5-Benzodiazepines are biologically important molecules and are extensively used clinically as analgesic, hypnotic, sedative, and antidepressive agents. Hence, 1,5-Benzodiazepines were synthesized by condensation of o-phenylenediamine and ketones, for example, cyclohexanone and acetone in presence of sulfated zirconia (catalyst). Mannich bases were synthesized with acetophenone, p-nitroacetophenone, p-chloroacetophenone, and formaldehyde. Schiff bases were synthesized using Mannich base of 1,5-benzodiazepines with p-chloroaniline and p-chlorophenylsemicarbazide in the presence of glacial acetic acid. All the synthesized compounds were characterized by 1H NMR and IR spectral analyses. All the synthesized derivatives were evaluated at the dose of 30 mg/kg b.w for anticonvulsant activity by isoniazid induced convulsion model, and the compounds NBZD-3 and NBZD-8 were found to be the most active among all compounds. Among all the synthesized derivatives, compounds NBZD-13 and NBZD-17 were found to be the most active among all compounds using thiosemicarbazide induced model. Although NBZD-8, NBZD-10, and NBZD-18 are the compounds which had shown good anticonvulsant activity and have an advantage over that, they were not sedative.

scholarly journals Synthesis and Antimicrobial Activity of Some New Thiazolidin-4-one Derivatives of 4-(6-methylbenzo[d]thiazol-2-yl)benzamine

2013 ◽  
Vol 2013 ◽  
pp. 1-6
Author(s):  
Awaz Jamil Hussein ◽  
Hashim Jalal Azeez
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Significant Activity ◽  
Gram Negative ◽  
H Nmr ◽  
Cyclocondensation Reaction ◽  
Ft Ir ◽  
High Yields ◽  
Derivatives Of ◽  
C Nmr

A number of derivatives of 2-(substituted phenyl)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl) thiazolidin-4-one (3a–j) have been synthesized from the reaction of 4-(6-methylbenzo[d]thiazol-2-yl)benzenamine(1), with different substituted benzaldehydes (2a–j), followed by cyclocondensation reaction of the prepared imines with 2-meraptoacetic acid in high yields. Furthermore, the structures of the newly synthesized compounds were confirmed by FT-IR,13C-NMR,13C-DEPT, and1H-NMR spectral data. The imines and thiazolidin-4-one derivatives were evaluated for their antibacterial activity againstEscherichia colias gram negative andStaphylococcus aureusas gram positive, the results have shown significant activity against both types of bacteria.

scholarly journals RNA-Targeted Therapies and High-Throughput Screening Methods

2020 ◽  
Vol 21 (8) ◽  
pp. 2996 ◽  
Author(s):  
Siran Zhu ◽  
Saul Rooney ◽  
Gracjan Michlewski
Keyword(s):  
High Throughput ◽  
Targeted Therapies ◽  
High Throughput Screening ◽  
Rna Binding ◽  
Rna Binding Proteins ◽  
Neuromuscular Disorders ◽  
Rna Metabolism ◽  
Survival Motor Neuron ◽  
Screening Methods ◽  
Dramatic Shift

RNA-binding proteins (RBPs) are involved in regulating all aspects of RNA metabolism, including processing, transport, translation, and degradation. Dysregulation of RNA metabolism is linked to a plethora of diseases, such as cancer, neurodegenerative diseases, and neuromuscular disorders. Recent years have seen a dramatic shift in the knowledge base, with RNA increasingly being recognised as an attractive target for precision medicine therapies. In this article, we are going to review current RNA-targeted therapies. Furthermore, we will scrutinise a range of drug discoveries targeting protein-RNA interactions. In particular, we will focus on the interplay between Lin28 and let-7, splicing regulatory proteins and survival motor neuron (SMN) pre-mRNA, as well as HuR, Musashi, proteins and their RNA targets. We will highlight the mechanisms RBPs utilise to modulate RNA metabolism and discuss current high-throughput screening strategies. This review provides evidence that we are entering a new era of RNA-targeted medicine.

scholarly journals Analysis by RP-HPLC and Purification by RP-SPE of the C-Tetra(p-hydroxyphenyl)resorcinolarene Crown and Chair Stereoisomers

2019 ◽  
Vol 2019 ◽  
pp. 1-6 ◽  
Author(s):  
Alver A. Castillo-Aguirre ◽  
Zuly Jenny Rivera Monroy ◽  
Mauricio Maldonado
Keyword(s):  
High Performance ◽  
Solid Phase ◽  
Reverse Phase ◽  
Formation Reaction ◽  
H Nmr ◽  
Rp Hplc ◽  
Cyclocondensation Reaction ◽  
Nmr Techniques ◽  
Ft Ir ◽  
C Nmr

A method for the separation of stereoisomer mixture of the octol C-tetra(p-hydroxyphenyl)calix[4]resorcinarene that was obtained by an acid cyclocondensation reaction between resorcinol and benzaldehyde is reported in this paper. A crude product from octol formation reaction was analyzed by reverse-phase high-performance liquid chromatography (RP-HPLC), and two well-resolved signals corresponding to the crown and chair isomers were found. A reverse phase in solid-phase extraction (RP-SPE) protocol allowed the separation of the two stereoisomers with high purity of each isomer. Finally, the crude and purified stereoisomers were characterized by using FT-IR, 1H-NMR, and 13C-NMR techniques, confirming the chemical identity of the two isomers and the efficiency in the separation process.

scholarly journals Design and microwave-assisted synthesis of a novel Mannich base and conazole derivatives and their biological assessment

2021 ◽  
Vol 27 (1) ◽  
pp. 100-111
Author(s):  
Yıldız Uygun Cebeci ◽  
Şengül Alpay Karaoğlu
Keyword(s):  
Mannich Base ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
Biological Assessment ◽  
Microwave Assisted Synthesis ◽  
One Pot ◽  
H Nmr ◽  
Microwave Assisted ◽  
New Compounds ◽  
C Nmr

Abstract 4-Amino-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one (1) was converted to the corresponding Schiff base (2) by treatment with salicylaldehyde. 1,2,4-Triazoles were then converted to the corresponding Mannich bases containing fluroquinolone core using a one-pot three-component procedure. Moreover, the synthesis of six compounds, which can be considered as conazole analogues, was performed starting from 1,2,4-triazole-3-one compounds via three steps by either conventional or microwave-mediated conditions. All the newly synthesized compounds were screened for their antimicrobial activities. Most exhibited good to moderate antibacterial and/or antifungal activity. The structural assignments of the new compounds were based on elemental analysis and spectral (IR, 1H NMR, 13C NMR, and LC-MS) data.

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