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Ahmadābād, India

Thakar A.,Zydus Research Center | Joshi K.,Navjivan Science College | Pandya K.,P.A. College | Pancholi A.,Navjivan Science College
E-Journal of Chemistry

Transition metal complexes of Cr(III), Mn(II), Fe(II), Co(II), Ni(II) and Cu(II) metal ions with general stoichiometry [ML2.2H2O] and [ML3], where M= Mn(II), Cr(III), Fe(II), Co(II), Ni(II) and Cu(II), L= Schiff base derived from the condensation of 2-amino-4(4'-phenyl/methylphenyl)-5- methyl-thiazole with 4-acetyl-1(3-chloro phenyl)-3-methyl-2-pyrazoline-5- ones, have been synthesized and structurally characterized by elemental analysis, molar conductance measurements, magnetic susceptibility measurements and spectral techniques like IR, UV, 1H NMR, 13C NMR and Mass Spectra. All the complexes were found to be octahedral geometry. The ligand and its complexes have been screened for their antifungal and antibacterial activities against three fungi, i.e. Alternaria brassicae, Aspergillus niger and Fesarium oxysporum and two bacteria, i.e. Xanthomonas compestris and Pseudomonas aeruginosa. © Copyright E-Journal of Chemistry 2004-2011. Source

Maheshwari R.,Sumandeep Vidyapeeth | Sailor G.,Sumandeep Vidyapeeth | Patel L.,Zydus Research Center | Balaraman R.,Sumandeep Vidyapeeth
Indian Journal of Pharmacology

Objectives: This study aimed to investigate the protective effect of simvastatin (SIM) and rosuvastatin (RST) on cisplatin (CIS)-induced nephrotoxicity. Materials and Methods: Adult female Wistar rats were divided into six groups: Control group (Group 1) received 0.5% sodium carboxy methyl cellulose, group 2 and group 3 received SIM and RST for 10 days, respectively, and group 4 was injected single dose of CIS (7 mg/kg, i.p.). Group 5 and 6 were treated with SIM (10 mg/kg, p.o.) and RST (10 mg/kg, p.o.) for 10 days, respectively. All groups received cisplatin on the 5 th day of treatment. Renal function tests like serum creatinine, urea, BUN, albumin, calcium, uric acid and magnesium, serum lipids, and markers of oxidative stress such as renal malondialdehyde (MDA) level and superoxide dismutase (SOD) and catalase (CAT) activities were measured. All tissues were investigated for histopathological changes. Result: CIS reduced the renal function, which was reflected with significant increase in serum urea, BUN, serum creatinine, uric acid and also significant decrease serum calcium, magnesium, albumin levels. In addition, cisplatin caused renal tubular damage with a higher MDA level, depletion of SOD and CAT activity, and elevation of serum lipids. SIM or RST ameliorate CIS induced renal damage due to improvement in renal function, oxidative stress, suppression of serum lipids, and histological alteration. Conclusions: This finding suggests that simvastatin and rosuvastatin may have a protective effect against cisplatin-induced kidney damage via amelioration of lipid peroxidation as well as due to improvement of renal function, and lipid-lowering effects. Source

Thakar A.S.,Zydus Research Center | Singh K.K.,Zydus Research Center | Joshi K.T.,Navjivan Science College | Pancholi A.M.,Navjivan Science College | Pandya K.S.,P.A. College
E-Journal of Chemistry

4-Acyl-1-phenyl-3-methyl-2-pyrazolin-5-ones condensed with 2-amino-4(4'-methylphenyl)-thiazole to form Schiff base. These Schiff bases from complexes of type ML2.2H2O (M=Mn, Fe, Co, Ni and Cu). Elemental analysis, magnetic susceptibility, electrical conductance, electronic and Infrared spectral data suggested octahedral structure for the complexes. All the compounds were tested for their antibacterial activity. The result indicates that the growth of the tested organism was inhibited by most of the compounds. These Schiff bases are characterized by elemental analysis, mass spectra, 1HNMR spectra, 13C NMR spectra and FT IR spectra. Source

Vaidya H.B.,Narsee Monjee Institute of Management and Higher Studies | Giri S.,Zydus Research Center | Jain M.,Zydus Research Center | Goyal R.K.,Narsee Monjee Institute of Management and Higher Studies
Experimental and Clinical Cardiology

Diabetes mellitus encompasses a group of chronic metabolic conditions associated with cardiovascular complications such as atherosclerosis, cardiomyopathy and nephropathy. In the present study, the authors investigated the beneficial effects of swertiamarin in diabetes and its associated cardiovascular complications in Zucker fa/fa rats. Six male Zucker fa/fa rats in each group were treated for 28 days with swertiamarin (75 mg/kg/day, intraperitoneally) or pioglitazone (30 mg/kg orally). Blood samples were collected and evaluated for several parameters. Elevated serum glucose, triglyceride, nonesterified free-fatty acid and cholesterol levels were found in untreated Zucker fa/fa rats. Serum matrix metalloproteinase (MMP)-9 and MMP-3 levels were also found to be significantly higher in untreated Zucker fa/fa rats. Treatment with swertiamarin significantly (P<0.05) reduced serum glucose, triglyceride, nonesterified free-fatty acid and cholesterol levels, and also reduced serum MMP-9 and MMP-3 levels compared with untreated rats. Swertiamarin also significantly (P<0.05) decreased serum levels of urea compared with untreated Zucker fa/fa rats. Overall, the data suggest that swertiamarin produced beneficial effects with respect to diabetes-induced cardiovascular complications such as atherosclerosis and nephropathy. A swertiamarin-induced decrease in serum MMP-9 and MMP-3 levels is one of the possible mechanisms responsible for improvement of these complications. ©2012 Pulsus Group Inc. All rights reserved. Source

Patel D.,Zydus Research Center | Patel D.,M. S. University of Baroda | Jain M.,Zydus Research Center | Shah S.R.,M. S. University of Baroda | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters

A novel series of pTyr mimetics containing triaryl-sulfonamide derivatives (5a-r) are reported as potent and selective PTP1B inhibitors. Some of the test compounds (5o and 5p) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro). The lead compound 5o showed potent antidiabetic activity (in vivo), along with improved pharmacokinetic profile. These preliminary results confirm discovery of highly potent and selective PTP1B inhibitors for the treatment of T2DM. © 2011 Elsevier Ltd. All rights reserved. Source

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