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Saravanan G.,Jawaharlal Nehru Technological University | Alagarsamy V.,M.R.Research | Prakash C.R.,DCRM Pharmacy College
Bioorganic and Medicinal Chemistry Letters | Year: 2012

Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the preliminary screening in MES model and/or scPTZ model. Further all these five compounds were administered to rats, 5c and 5d showed better activity than Phenytoin in oral route. Among all the title compounds tested, the most active one was 5c that revealed protection in MES at a dose of 30 mg/kg (ip) after 0.5 and 4 h. This molecule also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h). © 2012 Elsevier Ltd. All rights reserved. Source


Saravanan G.,Jawaharlal Nehru Technological University | Alagarsamy V.,M.R.Research | Prakash C.R.,DCRM Pharmacy College
Medicinal Chemistry Research | Year: 2013

With the aim of developing potent analgesic, anti-inflammatory, and antimicrobial agents a series of novel quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, 1H-NMR, mass spectroscopy and bases of elemental analysis. Tail-flick technique, carrageenan-induced foot paw edema test, and agar streak dilution test were performed for screening analgesic, anti-inflammatory, and in vitro antimicrobial activity, respectively. Moreover, all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory, and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds were discussed. Compound 2-(2-(4-(trifluoromethyl)benzylidene)hydrazinyl)-N-(4-(2-methyl-4-oxoquinazolin- 3(4H)-yl) phenyl) acetamide 5e was determined to be the most active compound. © 2012 Springer Science+Business Media, LLC. Source


A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3- substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index (0.51 ± 1.63, 0.48 ± 1.28 and 0.50 ± 1.53, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3- pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5- hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene- hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities. Source


Prakash C.R.,DCRM Pharmacy College | Raja S.,Gandhi Institute of Technology and Management | Saravanan G.,Medicinal Chemistry Research Laboratory
Chinese Chemical Letters | Year: 2012

A new series of isatin semicarbazide derivatives (7a-7j) were synthesized and characterized by spectroscopic means and elemental analysis. Analgesic and anti-inflammatory screening was performed using tail-flick technique and the carrageenan-induced foot paw edema test respectively. The ulcerogenicity was also determined for all the compounds. Some of the compounds showed moderate enhancement of the activity. Among the synthesized derivatives, compound 7d showed higher analgesic, antiinflammatory and one-third of ulcer index of the reference drug. © 2012 Chinnasamy Rajaram Prakash. Source


Saravanan G.,Jawaharlal Nehru Technological University | Alagarsamy V.,M.R.Research | Prakash C.R.,DCRM Pharmacy College
Journal of Saudi Chemical Society | Year: 2015

A series of 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl) phenyl)semicarbazide derivatives were synthesized with the aim of developing potential antimicrobials. It was characterized by FT-IR, 1H NMR, Mass spectroscopy and elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique and agar streak dilution method. All title compounds showed activity against the entire strain of microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. Based on the results obtained, compound 5j was found to be very active compared to the rest of the compounds which were subjected to antimicrobial assay. © 2011. Source

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