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Ugale, Vinod G.
- Design, Development and Screening of Some Novel Quinazolinones for Anticonvulsant Activity
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Authors
Affiliations
1 Pharmaceutical Chemistry Division, Smt. S.K. Bhoyar College of Pharmacy, Kamptee, Nagpur University, Nagpur-440010 (M.S.), IN
1 Pharmaceutical Chemistry Division, Smt. S.K. Bhoyar College of Pharmacy, Kamptee, Nagpur University, Nagpur-440010 (M.S.), IN
Source
Asian Journal of Research in Chemistry, Vol 4, No 11 (2011), Pagination: 1717-1721Abstract
A series of 6-substituted 2-ethyl-3-[substituted benzothiazol-2-yl]-4(3H)-quinazolinones have been synthesized. The structure of all these newly synthesized compounds was confirmed by their elemental(C, H, N) and spectral (IR and 1H NMR) data. The anti-convulsant activity of the title compounds was evaluated by using MES (Maximal Electroshock Method) and subcutaneous pentylenetetrazole (scPTZ) test models in mice. All the test compounds were administered intraperitoneally at a dose 20 mg/Kg body weight and percentage protection were determined. All the experimental protocols were approved by the institutional animal ethical committee (IAEC) and experiments were conducted in accordance with the guidelines provided by the committee for the purpose of control supervision of experimental animals (CPCSEA). All the test compounds showed most prominent anti-convulsant activity with low side effects compared with the reference drug Phenytoin sodium in MES test and Diazepam in scPTZ test.
Keywords
2-Ethyl-3-[Substituted-Benzothiazol-2-yl]-4(3H)-Quinazolinone, 6-Iodo, 2-Ethyl-3-[Substitutedbenzothiazol-2-yl]-4(3H)-Quinazolinone, Anti-Convulsant Activity, Maximal Electroshock Seizure Test, Pentylenetetrazole Test.
- Anti-Inflammatory Potentials of Some Novel Murrayanine Containing 1,3,4-Oxadiazole Derivatives
Abstract Views :480 |
PDF Views:1
Authors
Affiliations
1 Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur - 440037, Maharashtra, IN
2 Department of Pharmaceutical Chemistry, Kamla Nehru College of Pharmacy, Nagpur - 441108, Maharashtra, IN
3 Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur - 425405, Dist. Dhule, Maharashtra, IN
1 Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur - 440037, Maharashtra, IN
2 Department of Pharmaceutical Chemistry, Kamla Nehru College of Pharmacy, Nagpur - 441108, Maharashtra, IN
3 Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur - 425405, Dist. Dhule, Maharashtra, IN
Source
Asian Journal of Pharmacy and Technology, Vol 8, No 1 (2018), Pagination: 47-51Abstract
Based on the assumption that designing compounds with all the three features; a natural product, a synthetic component, and a functional Schiff’s base will surely lead to the development of more potent and safe analogs. The present research endeavors at designing a novel molecule from a previously reported starting material (E)-2-((1-methoxy-9H-carbazol-3-yl)methylene) hydrazinecarboxamide that comprised of a natural product (murrayanine, a carbazole alkaloid present in the Indian curry plant Murraya koenigii L.), a synthetic component (oxadiazole, a well-known versatile heterocycle which has potential for treating numerous ailments), and a functional Schiff’s base attaching a substituted aromatic portion. The produced derivatives were studied for exploration of their in vivo anti-inflammatory activity using carrageenan-induced paw edema method. The sophisticated analytical techniques established the structures of murrayanine-oxadiazole hybrids. The acute toxicity studies highlighted their certain degree of safety. The compound 4e containing 3,5-OCH3 and 4-OH expressed the highest biological activity after 3 hrs, which may be due to the interaction of the substituents with the active sites of inflammation targets like cyclooxygenase (COX) and lipoxygenase (LOX). A structural influence on the biological activity cannot be predicted very clear, however, it might be plausibly expressed that the hydrophilic groups or electron-donating substituents at 3 to 5 positions have a vital role. This research will be an emerging perspective towards the fabrication of natural and synthetic components in one hybridized form which results in synergistic pharmacological activity. The fabricated products have the potential of usage as future therapeutic agents with good safety profile.Keywords
Murrayanine, Murraya koenigii, Oxadiazole, Inflammation, Hybrid, Schiff's Base.References
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