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Malavalli Madaiah, Bidarur K Jayanna, Arakere S Manu, Maralekere K Prashanth, Hosakere D Revanasiddappa, Bantal Veeresh
Acetylcholinesterase (AChE) inhibitors are currently the most widely prescribed drugs for Alzheimer's disease. The high potential of indole compounds in medicinal chemistry led us to discover a novel series of fluoroindole compounds. The synthesis and pharmacological analysis of the difluoropyrido[4,3-b]indoles 11-34 are described. Compounds 11-34 were tested for AChE inhibition activity using a rat brain homogenate. Compounds 25-29 display a promising in vitro profile with an IC50 value range of 46-51.6 nM and show significant protective effect on scopolamine-induced amnesia...
April 2017: Archiv der Pharmazie
Hemavathi N Deepakumari, Bidarur K Jayanna, Maralekere K Prashanth, Hosakere D Revanasiddappa, Bantal Veeresh
A series of new N-(substituted)-1-methyl-2,4-dioxo-1,2-dihydroquinazoline-3(4H)-carboxamides were designed, synthesized, and evaluated for their anticonvulsant activity. Most of the synthesized compounds exhibited potent anticonvulsant activities in the maximal electroshock (MES) and pentylenetetrazol (PTZ) test. The most promising compound 4c showed significant anticonvulsant activity with a protective index value of 3.58. The compounds 4a-c were also found to have encouraging anticonvulsant activity in the MES and PTZ screen when compared with the standard drugs, valproate and methaqualone...
July 2016: Archiv der Pharmazie
Malavalli Madaiah, Maralekere K Prashanth, Hosakere D Revanasiddappa, Bantal Veeresh
A series of novel 1'-[2-(difluoromethoxy)benzyl]-2'H,5'H-spiro[8-azabicyclo[3.2.1]octane-3,4'-imidazolidine]-2',5'-dione substituted hydantoins (5-32) were synthesized using an appropriate synthetic route and characterized by elemental analysis and spectral data. The novel molecules were screened for anticonvulsant activity in mice by maximal electroshock (MES) and subcutaneous pentylenetetrazol (ScPTZ)-induced seizure tests. The neurotoxicity was assessed using the rotarod method. Compounds 9, 10, 18, 30, and 31 exhibited anticonvulsant potency against MES seizure and in the ScPTZ model, with lesser neurotoxicity...
May 2014: Archiv der Pharmazie
Kikkeri P Harish, Kikkeri N Mohana, Lingappa Mallesha, Bantal Veeresh
A series of new 2-methyl-2-[3-(5-piperazin-1-yl-[1,3,4]oxadiazol-2-yl)-phenyl]-propionitrile derivatives 8a-o, 9a-c, 10a-d, and 11a-d were synthesized to meet the structural requirements essential for anticonvulsant property. The structures of all the synthesized compounds were confirmed by means of (1)H NMR, (13)C NMR, and mass spectral studies. The purity of the novel compounds was confirmed by elemental analyses. All the compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method and their neurotoxic effects were determined by rotorod test...
April 2014: Archiv der Pharmazie
Malavalli Madaiah, Maralekere K Prashanth, Hosakere D Revanasiddappa, Bantal Veeresh
New 3-[(2,4-dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile derivatives 8-37 were synthesized and their pharmacological activities were determined with the objective to better understand their structure-activity relationship (SAR) for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) and pentylenetetrazole (PTZ) test. Compounds 11, 18, 31, and 32 showed significant and protective effect on seizure, when compared with the standard drug valproate...
March 2013: Archiv der Pharmazie
Lingappa Mallesha, Kikkeri N Mohana, Bantal Veeresh, Ravi Alvala, Alvala Mallika
A series of new 2-methyl-3-(2-piperazin-1-yl-ethyl)-pyrido[1,2-a]pyrimidin-4-one derivatives 6a-j were synthesized by a nucleophilic substitution reaction of 2-methyl-3-(2-piperazin-1-ylethyl)-pyrido[1,2-a]pyrimidin-4-one with various sulfonyl chlorides. The compounds were characterized by different spectral studies. All the compounds were evaluated for their antiproliferative effect using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay method against four human cancer cell lines (K562, Colo-205, MDA-MB 231, IMR-32) for the time period of 24 h...
January 2012: Archives of Pharmacal Research
Bart P Van Putte, Nabil Bantal, Repke Snijder, Wim J Morshuis, Wim-Jan Van Boven
Acute massive pulmonary embolism is a life threatening medical emergency resulting in a high mortality rate. Usually, urgent thrombo-embolectomy is performed using double venous cannulation without circulatory arrest. We describe a patient suffering from acute massive pulmonary embolism that was treated by emergency thrombo-embolectomy. Due to back-bleeding the view into the lobar and segmental pulmonary arteries was severely compromised. In order to achieve complete thrombo-embolectomy, intermittent deep hypothermic circulatory arrest was performed...
May 2008: Interactive Cardiovascular and Thoracic Surgery
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