Faculty Publications
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Item Anti-diarrheal potential of Aegle Marmelos Corr. root bark extract in rats(2007) Vrushabendra Swamy, S.B.M.; Nataraj, K.S.; Jayaveera, K.N.; Gopkumar, P.; Nayak, S.; Kumar, G.S.; Umachigi, S.P.A study was undertaken to evaluate the effect of methanolic extract of the rootbark of Aegle marmelos Corr. (MAMC) against several experimental models of diarrhoea in rats. MAMC treated animal's showed significant inhibitory effect against castor-oil induced diarrhea and PGE2 induced enteropooling in rats. The extract also showed a significant reduction in gastrointestinal motility in the charcoal meal test in rats. The results obtained to establish the efficacy and substantiate the folkare claim as an anti-diarrhoeal agent.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 and anticonvulsant activity of some new bishydrazones derived from 3,4-dipropyloxythiophene(2009) Kulandasamy, R.; Vasudeva Adhikari, A.V.; Stables, J.P.A series of new 3,4-dipropyloxy-N2,N5-bis(substituted)thiophene-2,5-dicarbohydrazides (4-30) were synthesized from ethyl thiodiglycolate and diethyloxalate through multistep reactions. Following Dieckmann-Komppa reaction, the required precursor 3,4-dihydroxythiophene-2,5-diester (1) was prepared. This was derivatized with propyl bromide and further converted to corresponding hydrazide (3), which was finally transformed to targeted hydrazones (4-30) by conventional methods. The newly synthesized compounds were characterized using FT-IR, 1H and 13C NMR, EI-MS and elemental analyses. The anticonvulsant activity of all the title compounds was investigated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scMET) models and their neurotoxicity was also evaluated. Some of the selected compounds were subjected to 6 Hz test in order to evaluate their uncover activities. Compound 3,4-dipropyloxy-N2,N5-bis[1-(2-thienyl)ethylidene]thiophene-2,5-dicarbohydrazide (15) has emerged as a lead in this series with less neurotoxicity. © 2009 Elsevier Masson SAS. All rights reserved.Item A new class of anticonvulsants possessing 6 Hz activity: 3,4-Dialkyloxy thiophene bishydrazones(2009) Kulandasamy, R.; Vasudeva Adhikari, A.V.; Stables, J.P.Thirty nine new 3,4-di(substituted)oxy-N2,N5-bis(substituted)thiophene-2,5-dicarbohydrazides were synthesized starting from ethyl thiodiglycolate through multi-step reactions. In the synthetic sequence, 3,4-dihydroxythiophene-2,5-diester (1) was obtained by condensing the ethyl thiodiglycolate with diethyl oxalate. It was derivatized using different alkyl halides to give disubstituted thiophene esters (2-5), which were then converted to corresponding hydrazides (6-9) following usual methods. Finally, these hydrazides, on treatment with various substituted carbonyl compounds underwent smooth condensation to yield target hydrazones (10-13). The new compounds were characterized using FT-IR, 1H NMR and 13C NMR, mass spectral and elemental analyses. The anticonvulsant activity of the title compounds was established after intraperitoneal (ip) administration in three seizure models, which include maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and 6 Hz screens and their neurotoxicity was also evaluated. Compound 11f has emerged as an active compound with no neurotoxicity in this series. Also, the structure-activity relationship of the tested compounds was discussed. © 2009 Elsevier Masson SAS. All rights reserved.Item Synthesis, characterization and biological activities of some new benzo[b]thiophene derivatives(2010) Isloor, A.M.; Kalluraya, B.; Pai, K.Benzo[b]thiophene molecules are found to be important tools in synthetic medicinal chemistry. They are of current interest due to their wide spectrum of pharmacological properties. In view of the biological activities of benzo[b]thiophene containing molecules, in this present research work, we propose the synthesis of some new benzo[b]thiophene derivatives such as thiadiazoles, oxadiazoles, pyrazolin & diaryl pyrazoles starting from 3-chlorobenzo[b]thiophene-2-carboxyl chloride. These newly synthesized compounds were characterized by elemental analyses, I.R, NMR and Mass spectral studies. Some of the selected compounds were screened for their antibacterial, antifungal and anti-inflammatory studies. Many of the molecules were found to be potent. © 2009 Elsevier Masson SAS. All rights reserved.Item Synthesis and antimicrobial activity of some new pyrazole containing cyanopyridone derivatives(2012) Malladi, S.; Isloor, A.M.; Peethambar, S.K.; Ganesh, B.M.; Goud, P.S.K.A series of new 4,6-disubstituted-3-cyano-2-pyridone derivatives (4a-o) were synthesized. The structures of all target molecules (4a-o) have been confirmed by various spectral techniques and elemental analyses. The newly synthesized compounds were screened for antibacterial and antifungal activity and most of the compounds showed significant activity comparable with that of the standard drug. The results revealed that 4b, 4c, 4d, 4g, 4m, 4n and 4o showed good antibacterial activity towards all bacterial strains (Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa) when compared to standard drug streptomycin. Amongst all the compounds, 4c showed moderate antifungal activity against Aspergillus flavus. The acute toxicity study has also been carried out for biologically active compounds and the experimental studies revealed that compounds were safe up to 2000 mg/kg and no deaths of animals were recorded.Item Synthesis, characterization and their anticonvulsant, anti-inflammatory studies of some novel chromeno oxadiazoles(2013) Ubaradka, S.R.; Isloor, A.M.; Shetty, P.; Shetty, P.; Isloor, N.A.In this study, a series of new 1,2,4-oxadiazole derivatives containing 3,4-dihydro-2H-chromen-2-amine moiety were synthesized by efficient microwave reaction of 2-amino-N?-hydroxychroman-3-carboxamidine and suitable aldehyde. Structures of all the synthesized compounds were confirmed by spectral studies and C, H, N analyses. Newly synthesized compounds were screened for their anticonvulsant and anti-inflammatory properties. Few of the compounds exhibited excellent anticonvulsant activity as compared to the standard drug Diazepam. Also compounds have exhibited moderate anti-inflammatory activity as compared to the standard drug Diclofenac sodium. © 2012 Springer Science+Business Media, LLC.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 New pyrazole derivatives containing 1,2,4-triazoles and benzoxazoles as potent antimicrobial and analgesic agents(2013) Vijesh, A.M.; Isloor, A.M.; Shetty, P.; Sundershan, S.; Fun, H.-K.Azole class of compounds are well known for their excellent therapeutic properties. Present paper describes about the synthesis of three series of new 1,2,4-triazole and benzoxazole derivatives containing substituted pyrazole moiety (11a-d, 12a-d and 13a-d). The newly synthesized compounds were characterized by spectral studies and also by C, H, N analyses. All the synthesized compounds were screened for their analgesic activity by the tail flick method. The antimicrobial activity of the new derivatives was also performed by Minimum Inhibitory Concentration (MIC) by the serial dilution method. The results revealed that the compound 11c having 2,5-dichlorothiophene substituent on pyrazole moiety and a triazole ring showed significant analgesic and antimicrobial activity. © 2012 Elsevier Masson SAS. All rights reserved.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.