Dharbhamulla S.,NGSM Institute of Pharmaceutical Science
European Journal of Medicinal Chemistry | Year: 2010
A series of 7-(2-substituted phenylthiazolidinyl)-benzopyran-2-one derivatives have been synthesized by reaction of 7-amino-4-methyl-benzopyran-2-one (1) with an appropriate substituted aldehydes to obtain various Schiff bases (3a-k) which on treatment with thioglycolic acid afforded the title compounds (4a-k). Purity of the compounds has been confirmed by TLC. Structure of these compounds were established on the bases IR, 1H NMR, 13C NMR and Mass spectral data. Schiff bases and title compounds were evaluated for antibacterial and antifungal activities against various bacterial and fungal strains. The results showed that compounds 3d, 3f, 4d, 4f and 4i (100 μg/ml) exhibited good antibacterial and antifungal activity as that of standard antibiotics Ciprofloxacin and Griseofulvin. © 2009 Elsevier Masson SAS. All rights reserved.
Ishwar B.K.,NGSM institute of pharmaceutical science
International Journal of ChemTech Research | Year: 2010
A series of aminobenzylated mannich bases of pyrazinamide (2a to 2j) have been prepared by mannich reaction of aromatic aldehydes with pyrazinamide and secondary amines. The chemical structure of all the synthesized compounds have been elucidated by spectral studies (IR, H1 NMR). Also they have been assayed in vitro for their biological activity against E.coli, B.substilis, S.aureas bacterial species and A. niger and C. albicans fungal micro organisms.
Shastry C.S.,NGSM Institute of Pharmaceutical science |
Shafeeque A.A.,NGSM Institute of Pharmaceutical science |
Ashwathnarayana B.J.,NGSM Institute of Pharmaceutical science
Indian Journal of Pharmacology | Year: 2013
Objectives: Aripiprazole, a new atypical antipsychotic drug extensively metabolized by enzyme CYP3A4, is found to produce asymptomatic elevation of serum transaminase levels on long-term treatment. The present study aims to evaluate the hepatotoxic effect of aripiprazole when coprescribed with carbamazepine and fluvoxamine. Materials and Methods: The rats were subjected to chronic treatment with two different doses, therapeutic dose (TD) and maximum therapeutic dose (MTD), of aripiprazole in combination with carbamazepine and fluvoxamine. The changes in hepatic function was assessed by various biochemical liver enzyme markers like serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), alkaline phosphatase (ALP), total bilirubin, histological studies, and physical parameters (liver weight, liver volume, and body weight). Results: The combination of aripiprazole with fluvoxamine at both TD and MTD showed the hepatic damage and significant elevation in serum transaminase level which is supported by histological reports. The coadministration of aripiprazole with carbamazepine leads to significant decrease in blood concentration of aripiprazole possibly due to induction of enzyme CYP3A4 resulting in loss or reduction of clinical efficacy. Conclusions: There would be an accumulation of aripiprazole when coadministered with fluvoxamine, a known inhibitor of CYP3A4, leading to hepatic damage and reduction in aripiprazole when administered along with carbamazepine. Therefore, aripiprazole with fluvoxamine and carbamazepine should be coprescribed with caution. The patients should be monitored for signs of adverse effects like hepatic damage or decreased efficacy of these drugs.
Jose J.,NGSM Institute of Pharmaceutical science |
Narayana Charyulu R.,NGSM Institute of Pharmaceutical science
Optoelectronics and Advanced Materials, Rapid Communications | Year: 2016
Clinical use of ketoconazole is limited by lipophilic nature of the drug molecule. PAMAM dendrimer provides an excellent carrier for encapsulating the drugs that has the capacity to attach and discharge drugs through various mechanisms. In this research work, the solubilization mechanism, in vitro release studies of ketoconazole- PAMAM complex were investigated. The experimental results suggested that an increase in dendrimer concentration and generation results in an increase in aqueous solubility of ketoconazole. In vitro release study revealed the sustained release of the drug from drug dendrimer complex. © 2016, National Institute of Optoelectronics. All rights reserved.
Anupama N.,Vellore Institute of Technology |
Madhumitha G.,Vellore Institute of Technology |
Rajesh K.S.,NGSM Institute of Pharmaceutical Science
BioMed Research International | Year: 2014
Inflammation plays an important role in various diseases with high prevalence within populations such as rheumatoid arthritis, ulcer, atherosclerosis, and asthma. Many drugs are available in the market for inflammatory diseases. They exhibit several unwanted side effects to humans. Therefore, alternative treatments with safer compounds are needed. Carissa carandas plant is used in traditional medicinal system for its various diseases curing property. In the present study, we examined the anti-inflammatory effects of dried fruit methanol extract on carrageenan-induced hind paw edema in rats. C. carandas was defatted with petroleum ether, followed by methanol extraction. The methanol extracts of the dried fruits of Carissa carandas were given orally to the experimental rats caused significant activity (P ≤ 0.05) when compared with the control group. The maximum inhibition of paw edema was found to be in Group V, that is, 76.12% with inhibition of paw volume in a dose-dependent manner. The anti-inflammatory activity of the methanol extract of the dried fruits shows that the presence of potential constituents present in this extract may provide assistance in the drug discovery process. The phytochemical compounds of the extract were screened by GC-MS analysis and it was found that 11 compounds are present in methanol extract of dried fruits of Carissa carandas. © 2014 N. Anupama et al.
Nairy H.M.,NGSM Institute of Pharmaceutical science |
Charyulu N.R.,NGSM Institute of Pharmaceutical science |
Shetty V.A.,KS Hegde Medical Academy |
Prabhakara P.,NGSM Institute of Pharmaceutical science
Trials | Year: 2011
Background: Oropharyngeal candidasis is a common opportunistic infection seen in immunocompromised patients. Fluconazole has a broad spectrum antifungal activity including a wide variety of candida species. Aim of the present investigation was to formulate and find out the relative efficacy of in situ gels of fluconazole.Method: The in situ gels were prepared using polymers which exhibited sol-to-gel phase transition due to change in specific physico-chemical parameters, such as ion triggered system using gellan gum (0.5% w/v) along with sodium carboxylmethylcellulose (0.35%w/v). The study design was bicenter, 'pseudo-randomised, single blind trial conducted in Mangalore., India, which includes 15 HIV positive patients, 15 patients with partial or completes dentures, and 15 patients who were treated with (active control) fluconazole tablets 100 mg/day for 14 days. Severity of disease was scored clinically before treatment and at clinical evaluations on day 3, 7, 14, 18, 21, 35, and 42. Semiquantitative microbiological cultures of oral swabs were also obtained on same days.Results: All patients had mycological documented oropharyngeal candidiasis and were treated with fluconazole (0.5%w/v) in situ gels for 14 days Severity of disease was scored clinically before treatment and at different predetermined time intervals along with semi quantitative culture of oral swabs. The clinical response rate showed 97% cure after 14 days in the treated with in situ gel. In comparison, the control group treated with fluconazole tablets showed 85% improvement in symptoms of oral candidiasis. The patients suffering from HIV infection showed relapse in oral candidiasis at the end of 21 days. The patients having oral candidiasis due to partial or complete dentures showed complete recovery and were free from signs and symptoms of oral candidiasis.Conclusions: The in situ gel formulation of fluconazole was well tolerated with no severe adverse reaction and offers a better alternative to tablet formulation in the treatment of oropharyngeal candidasis.Trial registration: Current Controlled Trails ISRCTN90634047. © 2011 Nairy et al; licensee BioMed Central Ltd.
Bhattacharjee A.,NGSM Institute of Pharmaceutical science |
Shashidhara S.C.,NGSM Institute of Pharmaceutical science |
Aswathanarayana,NGSM Institute of Pharmaceutical science
Asian Pacific Journal of Tropical Biomedicine | Year: 2012
Crataeva nurvala Buch-Hum (Varuna) is well known traditional Indian medicinal plant used to treat various ailments in particular urolithiasis. During last two decades, numerous ethno-pharmacological and scientific reports have been cited in the literature to support its multi-directional therapeutic potential. The plant is rich in alkaloids, saponins, triterpenes, tannins, flavanoid glycosides, glucosinolates and phytosterols. The review emphasizes primarily on folkloric uses, biological activities of isolated compounds, pharmacological activities of the extracts, clinical studies and safety profile of Crataeva nurvala to provide a comprehensive data for researchers to hit upon new chemical entity responsible for its claimed traditional uses. © 2012 Asian Pacific Tropical Biomedical Magazine.
Girisha K.S.,Mangalore University |
Kalluraya B.,Mangalore University |
Narayana V.,NGSM Institute of Pharmaceutical science |
Padmashree,NGSM Institute of Pharmaceutical science
European Journal of Medicinal Chemistry | Year: 2010
A series of 1-acetyl/propyl-3-aryl-5-(5-chloro-3-methyl-1-phenyl-1H- pyrazol-4-yl)-2-pyrazolines were synthesized in one step by condensing suitably substituted propenones, hydrazine and acetic/propionic acid. The newly synthesized pyrazolines were characterized by analytical and spectral data. The new compounds were screened for analgesic and anti-inflammatory activity and most of them showed good activity comparable with that of standard drugs Pentazocin and Diclofinac sodium respectively. © 2010 Elsevier Masson SAS. All rights reserved.
Nisha Shetty G.,NGSM Institute of Pharmaceutical science |
Charyulu R.N.,NGSM Institute of Pharmaceutical science
International Journal of Pharma and Bio Sciences | Year: 2013
This work describes the stability of the selected in situ solutions for ophthalmic delivery of naphazoline hydrochloride (FF17, FF18) and antazoline phosphate (GG17 and GG18) based on the pH triggered concept using Carbopol 940 and HPMC K4M. The formulations were evaluated for their pH, isotonicity, gelling capacity,rheological characteristics, in vitro drug release, sterility and in vivo studies in New Zealand rabbits' eyes. All the formulations showed satisfactory results at ocular pH environment that remains in contact with the eyes for few hours. The formulations were very stable throughout, at room temperature and at 40 °C. Higher amount of both the drugs were retained in the aqueous humour area over 8 hrs following instillation FF17, FF18, GG17& GG18. Therefore, in situ gelling system can be used to enhance the ocular retention time thereby increasing ocular bioavailability and reducing the frequency of dosing.
Hunashal R.D.,Karnataka Institute of Medical science |
Satyanarayana D.,NGSM Institute of Pharmaceutical science
International Journal of Pharma and Bio Sciences | Year: 2012
The reaction of thiocarbohydrazide with substitutedphenoxy acetic acid to obtained 3-substituted-4-amino-5-mercapto-1,2,4-triazoles (1) by condensing compound 1 with aromatic carboxylic acid and substituted phenoxy acetic acids resulted the title compound triazolothiadiazoles 2a-j. The purity of the newly synthesized compounds was confirmed by TLC. Structures of all the newly synthesized compounds were confirmed by spectral data. All the newly synthesized compounds were screened for their in-vitroantimicrobial activity.Among the series the compounds 2e, 2f and 2b, 2c, 2f, 2d, 2i were exhibited equipotent antibacterial and antifungal activity a MIC of 1 μg/mL when compared with standard drugs respectively. From the results the compounds 2c, 2f, 2j were showed comparable antitubercular activity againstM. tuberculosisH37Rv at MIC of 0.50 μg/mL, when compared with standard drug Rifampin and INH which showed MIC of 0.25 μg/mL.