Journal Articles
Permanent URI for this collectionhttps://idr.nitk.ac.in/handle/123456789/19884
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Item Synthesis of some new 4-styryltetrazolo[1,5-a]quinoxaline and 1-substituted-4-styryl[1,2,4]triazolo[4,3-a]quinoxaline derivatives as potent anticonvulsants(2009) Wagle, S.; Vasudeva Adhikari, A.V.; Suchetha Kumari, N.S.4-Methyltetrazolo[1,5-a]quinoxaline (3) was prepared by the azide cyclocondensation of 2-chloro-3-methylquinoxaline (2). The reaction of 3 with aromatic aldehydes furnished 4-styryltetrazolo[1,5-a]quinoxalines (4a-f). Compound 2, on treatment with hydrazine hydrate gave 2-hydrazino-3-methylquinoxaline (5). The ring closure of 5 was achieved by the reaction of orthoesters and trifluoroacetic acid to yield 4-methyl-1-(substituted)[1,2,4]triazolo[4,3-a]quinoxalines (7a-c). Further, reaction of 7a-c with different aromatic aldehydes furnished the title compounds, 4-styryl-1-(substituted)[1,2,4]triazolo[4,3-a]quinoxalines (8a-i) in good yield. In another scheme, the hydrazino compound 5 was treated with different aromatic aldehydes to yield corresponding N-arylidenehydrazino quinoxalines (6a-d). Further, the oxidative cyclization of hydrazones by nitrobenzene yielded 1-aryl-4-methyl[1,2,4]triazolo[4,3-a]quinoxalines (7d-g), which on condensation with aromatic aldehydes gave the title compounds, 1-aryl-4-styryl[1,2,4]triazolo[4,3-a]quinoxalines (8j-u). The newly synthesized compounds have been characterized by FTIR, 1H NMR, 13C NMR and mass spectral data, followed by elemental analysis. Some of the compounds were screened for in vivo anticonvulsant activity. Few of them exhibited promising results. © 2008 Elsevier Masson SAS. All rights reserved.Item Synthesis, anticonvulsant and anti-inflammatory studies of new 1,4-dihydropyridin-4-yl-phenoxyacetohydrazones(Elsevier Masson SAS infos@masson.fr 62 rue Camille Desmoulins Issy les Moulineaux Cedex 92442, 2013) Ulloora, S.; Shabaraya, R.; Ranganathan, R.; Vasudeva Adhikari, A.V.The present work involves design and synthesis of new substituted 1,4-dihydropyridin-4-yl-phenoxyacetohydrazones (4a-s, 5a-h), starting from 4-hydroxybenzaldehyde. The final compounds were screened for their in vivo anticonvulsant activity by MES, scPTZ and 6 Hz methods, while their anti-inflammatory screening was performed by Carrageenan induced Paw Edema method. The results indicated that compounds carrying electron donating groups are anticonvulsant active, while most of the tested compounds exhibited significant anti-inflammatory activity. Compounds 4k, l, 4p-s, and 5c showed rapid anti-inflammatory activity within 30 min and appeared as lead compounds. Further, Neurotoxicity study revealed that all the tested compounds are non-toxic up to 300 mg/kg doses. Selected compounds were also subjected to analgesic screening following Tail immersion method and they exhibited good activity. © 2013 Elsevier Masson SAS. All rights reserved.Item New imidazo[1,2-a]pyridines carrying active pharmacophores: Synthesis and anticonvulsant studies(2013) Ulloora, S.; Shabaraya, R.; Aamir, S.; Vasudeva Adhikari, A.V.Five new series of imidazo[1,2-a]pyridines carrying biologically active pyrazoline (4a-e), cyanopyridone (5a, b), cyanopyridine (6a-f), 2-aminopyrimidine (7a-f) and pyrimidine-2-thione (8a-d) systems were designed and synthesized as prominent anticonvulsant agents. The target compounds were screened for their in vivo anticonvulsant activity following maximal electroshock (MES) and subcutaneous pentylene tetrazole (scPTZ) methods at a small test dose of 10 mg/kg. Further, Rotarod toxicity method was used to study the toxicity profile of selected compounds. Compounds 4b, 5a, 5b, 6a, 7e and 8d possessing 4-fluorophenyl substituent at 2nd position of imidazo[1,2-a]pyridine ring displayed potent anticonvulsant activity without displaying any toxicity. Enhanced activity profile was observed for new compounds in PTZ method over MES method. © 2012 Elsevier Ltd. All rights reserved.Item New dihydropyridine derivatives: Anti-inflammatory, analgesic and docking studies(2013) Ulloora, S.; Kumar, S.; Shabaraya, R.; Vasudeva Adhikari, A.V.The present article describes synthesis of new diethyl 2,6-dimethyl-4-(4- (2-substituted amino-2-oxoethoxy) phenyl)-1,4-dihydropyridine-3,5-dicarboxylates (6a-10b) following multistep synthetic route. Structures of newly synthesized intermediates and title compounds were established by spectral and elemental analyses. The final compounds were screened for their in vivo anti-inflammatory and analgesic activities by carrageenan-induced paw oedema and tail immersion methods, respectively. Moreover, molecular docking studies were carried out for active compounds 6c, 6d, 7d, 8 and 10b to study their mode of action, meanwhile in vivo results indicated that these compounds displayed rapid onset of anti-inflammatory action and exhibited prominent activity when compared with the standard drug. Compounds 6d and 7d carrying amide functionality showed the highest anti-inflammatory as well as analgesic activities. The molecular docking results emphasised the in vivo data and all docked molecules were found to display very low binding constant values in nanomolar scale. © 2012 Springer Science+Business Media, LLC.Item Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition(2013) Panathur, N.; Udayakumar, U.; Koushik, P.V.; Alvala, M.; Yogeeswari, P.; Sriram, D.; Kumar, V.In our pursuit to develop new potential anticancer leads, we designed a combination of structural units of indole and substituted triazole; and a library of 1-{1-methyl-2-[4-phenyl-5-(propan-2-ylsulfanyl)-4H-1,2,4-triazol-3- yl]-1H-indol-3-yl}methanamine derivatives was synthesized and characterized. Cytotoxic evaluations of these molecules over a panel of three human cancer cell lines were carried out. Few molecules exhibited potent growth inhibitory action against the treated cancer cell lines at lower micro molar concentration. An in vitro assay investigation of these active compounds using recombinant human SIRT1 enzyme showed that one of the compounds (IT-14) inhibited the deacetylation activity of the enzyme. The in vivo study of IT-14 exemplified its promising action by reducing the prostate weight to the body weight ratio in prostate hyperplasia animal models. A remarkable decrease in the disruption of histoarchitecture of the prostate tissues isolated from IT-14 treated animal compared to that of the positive control was observed. The molecular interactions with SIRT1 enzyme were also supported by molecular docking simulations. Hence this compound can act as a lead molecule to treat prostatic hyperplasia. © 2013 Elsevier Masson SAS. All rights reserved.Item New 6-bromoimidazo[1,2-A]pyridine-2-carbohydrazide derivatives: Synthesis and anticonvulsant studies(Birkhauser Boston, 2014) Ulloora, S.; Shabaraya, R.; Vasudeva Adhikari, A.V.In the present work, we report the facile synthesis and anticonvulsant study of new imidazo[1,2-A]pyridines carrying biologically active hydrazone functionality (3a-3e) and suitably substituted 1,2,4-triazole moieties (4, 5a-5d, 6, and 7a-7d). The newly synthesized intermediates and final compounds were characterized by various spectral techniques such as FTIR, 1H NMR, 13C NMR, and mass spectral and elemental analysis studies. The in vivo anticonvulsant study of the target compounds were carried out following maximal electroshock seizure and subcutaneous pentylene tetrazole methods, while their toxicity study was performed following rotarod method by taking 20, 40, and 100 mg/kg dose levels. Most of the new compounds displayed remarkable anticonvulsant properties at these doses. Particularly, compounds 3b and 4 carrying hydrogen bond donor groups, viz. hydroxyl and amine moieties respectively, exhibited complete protection against seizure and their results are comparable to that of standard drug diazepam. Further, the motor impairment study revealed that all the compounds are nontoxic upto 100 mg/kg. © 2013 Springer Science+Business Media New York.Item Nisin gold nanoparticles assemble as potent antimicrobial agent against Enterococcus faecalis and Staphylococcus aureus clinical isolates(Editions de Sante editions.de.sante@wanadoo.fr, 2017) Pradeepa, n.; Bhat, K.U.; Vidya, S.M.Enterococci and staphylococci have the potency to acquire resistant to antibiotics and have emerged as serious nosocomial pathogens responsible for various diseases. The continuous seeking of new antimicrobials against these pathogens is the only way to avoid the rapid spreading of diseases. Controlled fabrication of existing antimicrobials with nanoparticles offers an alternative strategy to combat against these pathogens with an effective manner. In the present study, gold nanoparticles (AuNPs) were functionalized with nisin to kill a wide range of clinically isolated Enterococcus faecalis and Staphylococcus aureus strains. Nisin functionalized gold nanoparticles (NAuNPs) exhibited good inhibitory activity against all seven multidrug resistant (MDR) and eight non-MDR E. faecalis and S. aureus strains. Minimum inhibitory concentration of NAuNPs was >8–32 fold lower than nisin. Interestingly, antibiotic resistant was not observed by these pathogens up to 8 generation. TEM and AFM investigation revealed that, the antimicrobial action of NAuNPs appears to act in three sequential stages: membrane destabilization, pore formation, followed by intracellular fluid leakage. In addition, NAuNPs were non toxic and showed less hemolytic activity. These findings indicated that, the NAuNPs can be served as an alternative antimicrobial agent to treat a wide range of enterococcal and staphylococcal infections. © 2016 Elsevier B.V.Item Effect of Surface Chemistry on Hemolysis, Thrombogenicity, and Toxicity of Carbon Nanotube Doped Thermally Sprayed Hydroxyapatite Implants(American Chemical Society, 2024) Shankar, D.; Jambagi, S.C.; Gowda, N.; Lakshmi, K.S.; Jayanthi, K.J.; Chaudhary, V.K.Assessing blood compatibility is crucial before in vivo procedures and is considered more reliable than many in vitro tests. This study examines the physiochemical properties and blood compatibility of bioactive powders ((0.5-2 wt % carbon nanotube (CNT)/alumina)-20 wt %)) produced through a heterocoagulation colloidal technique followed by ball milling with hydroxyapatite (HAp). The 1 wt % CNT composite demonstrated a surface charge ∼5 times higher than HAp at pH 7.4, with a value of −11 mV compared to −2 mV. This increase in electrostatic charge is desirable for achieving hemocompatibility, as evidenced by a range of blood compatibility assessments, including hemolysis, blood clotting, platelet adhesion, platelet activation, and coagulation assays (prothrombin time (PT) and activated partial thrombin time (aPTT)). The 1 wt % CNT composite exhibited hemolysis ranging from 2 to 7%, indicating its hemocompatibility. In the blood clot investigation, the absorbance values for 1-2 wt % CNT samples were 0.927 ± 0.038 and 1.184 ± 0.128, respectively, indicating their nonthrombogenicity. Additionally, the percentage of platelet adhered on the 1 wt % CNT sample (∼5.67%) showed a ∼2.5-fold decrement compared to the clinically used negative control, polypropylene (∼13.73%). The PT and aPTT experiments showed no difference in the coagulation time for CNT samples even at higher concentrations, unlike HAC2 (80 mg). In conclusion, the 1 wt % CNT sample was nontoxic to human blood, making it more hemocompatible, nonhemolytic, and nonthrombogenic than other samples. This reliable study reduces the need for additional in vitro and in vivo studies before clinical trials, saving time and cost. © 2024 American Chemical Society.Item Ensemble Machine Learning Approaches for Automated Fungal Keratitis Diagnosis Using In Vivo Confocal Microscopy Images(John Wiley and Sons Inc, 2025) Sowmya Kamath, S.; Reji, S.; Vaibhava Lakshmi, V.; Supreetha, S.; Gawas, P.; Mayya, V.; Hazarika, M.Fungal keratitis (FK) is a severe ocular infection that can lead to significant vision problems or blindness if not diagnosed and treated promptly. Early and accurate detection of FK is essential for effective management. Traditional diagnostic methods are often time-consuming and require specialized laboratory resources. Recently, advances in artificial intelligence and computer vision have enabled automated diagnosis of FK using slit-lamp images. In this article, a comprehensive evaluation of state-of-the-art techniques adopted for classifying FK using in vivo confocal microscopy (IVCM) images is presented. Detailed experiments and performance evaluation of various machine learning models are systematically performed, with a focus on evaluating the effect of diverse techniques for image processing, data augmentation, hyperparameters and model finetuning to assess each model's strengths and limitations. Experiments revealed that applying green channel preprocessing with a 12-feature set achieved 99% accuracy using Random Forest, highlighting its effectiveness in FK detection, while complex techniques like histogram modelling reduced accuracy to 64%. Robust models like AdaBoost and RUSBoost maintained high F1-scores, demonstrating adaptability to imbalanced medical datasets, and to real-world clinical scenarios. © 2025 The Author(s). Healthcare Technology Letters published by John Wiley & Sons Ltd on behalf of The Institution of Engineering and Technology.