Paper Search Console

Home Search Page About Contact

Journal Title

Title of Journal: Med Chem Res

Search In Journal Title:

Abbravation: Medicinal Chemistry Research

Search In Journal Abbravation:

Publisher

Springer US

Search In Publisher:

DOI

10.1002/ijch.201100019

Search In DOI:

ISSN

1554-8120

Search In ISSN:
Search In Title Of Papers:

Synthesis of Emphasis Type="Italic"N/Emphasis

Authors: Satheesh Krishna Balam Suresh Kumar Krishnammagari Jayaprakash Soora Harinath Siva Prasad Sthanikam Syama Sundar Chereddy Visweswara Rao Pasupuleti Nanda Kumar Yellapu Vasu Govardhana Reddy Peddiahgari Suresh Reddy Cirandur
Publish Date: 2014/08/06
Volume: 24, Issue: 3, Pages: 1119-1135
PDF Link

Abstract

Inhibition of 11βHSD1 enzymatic action is perceived as a potential target for the treatment of metabolic syndromes like cardiovascular diseases obesity and diabetes In an attempt to formulate potential organophosphorus compounds against 11βHSD1 enzyme inhibition we report novel 6bromo36methyl2pyridyl2alkyl/arylamino34dihydro2H132λ5benzoxazaphosphinin2ones 22a–22n as good in vitro inhibitors of HEK 293 cell lines The in vivo acute and subacute investigations sustain them as good antidiabetic compounds The computational docking studies performed on them also supported the binding mode of compounds 22a and 22h with 11βHSD1 protein The blood glucose level lowering effect of the target compounds 22a–22n screened on the streptozotocininduced diabetic rats revealed that the target compounds are potential by antidiabetic when compared to the potency of standard glibenclamide drug In addition the calculated QSAR parameters predicted ADMET properties evaluated bioactivity properties and toxicity risk studies authorize drug like properties to the synthesized compoundsWe thank University Grants Commission UGC New Delhi INDIA for providing financial support through UGCBSRRFSMS Research Fellowship In Sciences For Meritorious Students Fellowship F41/2011 BSRRFSMSBSK and for providing financial assistance through the Major Research Project F No 42281/2013 SR Dated 12032013 We also thank Dr V Koteswara Rao Post doctoral Fellow Kansas University Kansas USA for providing MOE software for QSAR and Molecular docking studies


Keywords:

References


.
Search In Abstract Of Papers:
Other Papers In This Journal:

  1. Synthesis and anti-inflammatory activity evaluation of novel 3-alkyl-6-(4 H -1,2,4-triazol-4-yl)-3,4-dihydro-2 H -benzo[ e ][1,3]oxazine derivatives
  2. Antimalarial and free radical scavenging activities of rhizomes of Polygonatum verticillatum supported by isolated metabolites
  3. Design, synthesis, and in vitro antimicrobial activities of novel azetidinyl-3-quinazolin-4-one hybrids
  4. Novel GABA-AT inhibitors: QSAR and docking based virtual screening of phenyl substituted β-phenyl ethylidene hydrazine analogues
  5. Synthesis and anticancer activity study of indolyl hydrazide–hydrazones
  6. Ulcerogenicity devoid novel non-steroidal anti-inflammatory agents (NSAIDS): syntheses, computational studies, and activity of 5-aryliden-2-imino-4-thiazolidinones
  7. Synthesis, characterization, and SAR studies of new (1 H -indol-3-yl)alkyl-3-(1 H -indol-3-yl)propanamide derivatives as possible antimicrobial and antitubercular agents
  8. Synthesis, characterization, and SAR studies of new (1 H -indol-3-yl)alkyl-3-(1 H -indol-3-yl)propanamide derivatives as possible antimicrobial and antitubercular agents
  9. Synthesis, characterization, and anticancer studies of S and N alkyl piperazine-substituted positional isomers of 1,2,4-triazole derivatives
  10. Expedient synthesis of some novel pregnane derivatives and their evaluation as anti-oxidant and anti-dyslipidemic agents
  11. Liquid chromatographic analysis of halofantrine from dosage form and its metal interaction studies
  12. Porphyrin interaction with the membrane: the use of membrane models to elicit the diverse partition in normal and neoplastic tissue
  13. 2D and 3D QSAR analyses to predict favorable substitution sites in anilino-monoindolylmaleimides acting as PKCβII selective inhibitors
  14. Synthesis and neuroprotective evaluation of ( E )-3,4-dihydroxystyryl p -substituted-phenethyl ketone derivatives against inflammatory and oxidative injury
  15. Synthesis of some novel triazoloquinazolines and triazinoquinazolines and their evaluation for anti-inflammatory activity
  16. Magnetic resonance assays of haloperidol in human serum albumin
  17. Synthesis of hydrophobic N -acylated isonicotinic acid hydrazide derivatives as potential enoyl–acyl carrier protein reductase (InhA) inhibitors
  18. Bioactive chemical constituents from the root of Clerodendrum phlomidis
  19. An efficient anticancer histone deacetylase inhibitor and its analogues for human HDAC8
  20. Mannich base derivatives of 1,3,4-oxadiazole: synthesis and screening against Entamoeba histolytica
  21. Antimicrobial and cytotoxic evaluation of eugenol derivatives
  22. Synthesis and cytotoxic evaluation of 7-chloro-4-phenoxyquinolines with formyl, oxime and thiosemicarbazone scaffolds
  23. Novel metal complexes, their spectrophotometric and QSAR studies
  24. Novel derivatives of 5-amino-1-cyclopropyl-7-[(3 R ,5 S )3,5-dimethylpiperazine-1-yl]-6,8-difluoro-4-oxo-quinoline-3-carboxylic acid: their synthesis, antimicrobial, antifungal, and urease inhibitory studies
  25. Synthesis of novel 4,6-diaryl-2-aminopyrimidines as potential antiplasmodial agents
  26. 2-(2′-Pyridyl) benzimidazole derivatives and their urease inhibitory activity
  27. Structure-based predictive model for some benzimidazole inhibitors of hepatitis C virus NS5B polymerase
  28. Synthesis, anti-inflammatory evaluation, and docking studies of some new thiazole derivatives
  29. A QSAR classification study on inhibitory activities of 2-arylbenzoxazoles against cholesteryl ester transfer protein
  30. Synthesis of novel 4-hydroxycoumarin derivatives: evaluation of antimicrobial, antioxidant activities and its molecular docking studies
  31. Synthesis and evaluation of some semicarbazone- and thiosemicarbazone-based cathepsin B inhibitors
  32. Pharmacophore modeling, virtual screening, and 3D-QSAR studies on a series of non-steroidal aromatase inhibitors
  33. Synthesis and antimalarial evaluation of novel pyridine quinoline hybrids
  34. In vitro and in silico exploration of IL-2 inhibition by small drug-like molecules
  35. Quantum chemical QSAR study of flavones and their radical-scavenging activity
  36. Synthesis and biological evaluation of novel pyrimidine-2(1 H )-ones/thiones as potent anti-inflammatory and anticancer agents
  37. Microwave-assisted synthesis of novel 4 H -chromene derivatives bearing 2-aryloxyquinoline and their antimicrobial activity assessment
  38. Indazole: a medicinally important heterocyclic moiety
  39. Effect of garlic and cabbage on healing of gastric ulcer in experimental rats
  40. Structure and toxicity of clozapine and olanzapine on agranulocytosis
  41. Comparative QSTR study of saturated alcohols based on topological, constitutional, geometrical, and getaway descriptors
  42. Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of nitrendipine analogues
  43. Simultaneous determination of seven active ingredients in rat plasma by UPLC-MS/MS and application in pharmacokinetic studies after oral administration of scutellaria-coptis herb couple
  44. Green synthesis and biological evaluation of some new benzothiazolo [2,3- b ] quinazolin-1-ones as anticancer agents
  45. Analysis of the essential oil from the aerial parts of Psoralea pubescence (Miq.) Standl and its antibacterial activity
  46. Synthesis, toxicity and chemo-sensitization of HeLa cells to etoposide, of some 2-methyl amino acid ester-substituted-1,3-benzoxazines
  47. Three-dimensional quantitative structure–activity relationship (3D-QSAR) analysis and molecular docking of ATP-competitive triazine analogs of human mTOR inhibitors
  48. Design and synthesis of new (bis)trifluoromethyl-promoted N -aryl biquinoline derivatives as antitubercular and antimicrobial agents
  49. Synthesis, characterization, and in vitro anti- Mycobacterium tuberculosis activity of terpene Schiff bases
  50. Phytochemical characterization and effect of Calendula officinalis , Hypericum perforatum , and Salvia officinalis infusions on obesity-associated cardiovascular risk
  51. Synthesis and in vitro antimicrobial evaluation of novel 2-amino-6-(phenylthio)-4-(2-(phenylthio)quinolin-3-yl)pyridine-3,5-dicarbonitriles
  52. Synthesis and cytotoxic evaluation of novel 2,3-di- O -alkyl derivatives of l -ascorbic acid
  53. Solvent- and catalyst-free synthesis of bis-adducts of 3-formylchromone as potential antimicrobial agents
  54. Synthesis of novel 2-(3′-aryl-sydnon-4′-ylidene)-5′-substituted-[1,3,4]-thiadiazolylamines and [1,3,4]-thiadiazol-2′-yl-3-oxo-[1,2,4]-triazoles as antimicrobial agents
  55. Molecular modeling design, synthesis, and anti-hyprglycemic evaluation of certain 5-(aryl-alkoxy-benzylidine)-imidazolidine-2,4-dione derivatives as potential PPARγ agonists
  56. Design, synthesis and neuraminidase inhibitory activity of N -(5-benzyl-4-( tert -butyl)thiazol-2-yl)benzamides
  57. Synthesis, characterization and in vitro hydrolysis studies of ester and amide prodrugs of dexibuprofen
  58. Transformations of naproxen into pyrazolecarboxamides: search for potent anti-inflammatory, analgesic and ulcerogenic agents
  59. Antituberculosis activity of hydrazones derived from 4-fluorobenzoic acid hydrazide
  60. Indolizine: a biologically active moiety
  61. Design, synthesis, and evaluation of the anticonvulsant and antidepressant activities of pyrido[2,3- d ]pyrimidine derivatives
  62. Synthesis and evaluation of novel benzene-ethanol bearing 1,2,4-triazole derivatives as potential antimicrobial agents
  63. Synthesis, anti-inflammatory activity, and QSAR study of some Schiff bases derived from 5-mercapto-3-(4′-pyridyl)-4 H -1,2,4-triazol-4-yl-thiosemicarbazide

Search Result: