Browsing by Author "Kumar, Deependra"

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    Microwave-assis synthesis of pyrazolo[1,5c] quinazolines and their derivatives
    (Elsevier, 2014) Kumar, Deependra; Kumar, Raj
    Microwave accelerated and expedited cyclocondensation reactions of 2-(3-aryl-1H-pyrazol-5-yl)anilines (4) with diverse aryl aldehydes/triethyl orthoformate in water/MeCN (route D) and internal cyclocondensation and aromatization of 5-(2-aminophenyl)-4,5-dihydro-3-arylpyrazole-1-carbaldehyde (7) under MeOH (route E) for the synthesis of a series of pyrazolo[1,5-c]quinazolines and their derivatives (1a–1q) are reported.
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    Microwave-assisted synthesis of pyrazolo[1,5-c]quinazolines and their derivatives
    (Elsevier, 2014) Kumar, Deependra; Kumar, Raj
    Microwave accelerated and expedited cyclocondensation reactions of 2-(3-aryl-1H-pyrazol-5-yl)anilines (4) with diverse aryl aldehydes/triethyl orthoformate in water/MeCN (route D) and internal cyclocondensation and aromatization of 5-(2-aminophenyl)-4,5-dihydro-3-arylpyrazole-1-carbaldehyde (7) under MeOH (route E) for the synthesis of a series of pyrazolo[1,5-c]quinazolines and their derivatives (1a–1q) are reported.
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    Synethesis and biochemical screening of novel non-purine based xanthine oxidase inhibitors
    (Central University of Punjab, 2013) Kumar, Deependra; Kumar, Raj
    Xanthine oxidase (XO), or xanthine oxidoreductase (XOR), is a complex molybdoflavoenzyme which, in humans, is recognized as the terminal enzyme of purine catabolism, catalysing the hydroxylation of purines to uric acid, overproduction of which usually leads to a pathological condition called hyperuricemia and gout. XO inhibitors (XOI) are proved to be promising urate lowering agents. Purine based XOI (allopurinol) however, are associated with various lethal side effects like hypersensitivity syndrome (Stevens Johnson syndrome and Tissue Epidermal Necrolysis), bone marrow depression, rash etc. On the other hand non-purine based XOI (febuxostat) are found to be safer and effective antihyperuricemic and antigout agents. Present investigation describes synthesis, characterization of some non-purine based compounds and their evaluation for xanthine oxidase inhibitory activity
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    Synthesis and xanthine oxidase inhibitory activity of 5,6 dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives
    (Elsevier, 2014) Kumar, Deependra; Kaur, Gagandeep; Negi, Arvind; Kumar, Sanjeev; Singh, Sandeep; Kumar, Raj
    Some 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives were rationally designed, synthesized and evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Some notions about structure activity relationships are presented. The compounds 6g, 6h and 6e were found to be significantly active against XO. The compound 6g emerged as the most potent XO inhibitor as compared to allopurinol and free radical scavenger. The molecular docking of 6g into the XO active site highlighted its mode of binding and important interactions such as hydrogen bonding, π–π stacking with amino acid residues like Ser876, Thr1010, Phen914, Phe1009 and Phe649 and its close proximity to dioxothiomolybdenum (MOS).