Background: Objective: The current study is aimed at the synthesis of these quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their analgesic activity. Method: The condensation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride yielded the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which further produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were unequivocally confirmed by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis.The synthesized compounds were screened for their analgesic activity.Compounds 1,2 and 3 showed significant analgesic activity. Discussion: Compound 1 was characterized by the absence of methyl group and the presence of methyl group for compound 2. The test investigated compounds exhibited significant analgesic activity when compared with the control test sample. The compounds synthesized exhibited promising analgesic activities against . Conclusion: The compounds have high analgesic activity. Compound 3 has a higher activity compared to Compound 2 and compound 2 has a higher analgesic activity compared to compound 1. Compound 3 has a higher analgesic activity compared to the standard drugs Aspirin and Indomethacin. Keywords: quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one quinazolin-4(3H)-one, analgesic activity.
Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride produced the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which also produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were assuredly validated by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis. The synthesized compounds were tested for their antibacterial activity.Compounds 1,2 and 3 showed significant antibacterial activities. Discussion: Compound 1 was identified by the absence of methyl group and the presence of methyl group for compound 2. The test analysed compounds exhibited significant antibacterial activities. The compounds synthesized exhibited promising antibacterial activities against the tested organisms. Conclusion: The compounds have high antibacterial activities. Compound 2 has a higher activity compared to Compound 1 and 3. Compound 2 has a higher antibacterial against Escherichia coli, Klebsiella pneumonia and Pseudomonas aeuriginosa
Abstract. Problem:In sub-Saharan Africa, malaria remains one of the leading health problems. This situation has been aggravated by the increasing spread of drug-resistant Plasmodium falciparum strains. The study was conducted to determine the chemosuppressive activities in in vivo studies of Plasmodium falciparum-infected mice with isolated oil of Stigmaphyllon ovatum leaves used in the traditional treatment of malaria in Nigeria. Methodology: The plant leaves were collected, dried, pulverized and extracted in Soxhlet extractor with hexane solvent. The crude extract was concentrated using a rotary evaporator and phytochemical screening performed using standard methods. Isolation of oil from hexane extract was done using vacuum liquid chromatography while characterization was done by gas chromatography-mass spectrometry (GC-MS). Chemosuppressive activities were conducted along with quinine to determine the antimalarial potency in Plasmodium falciparum-infected BALB/c albino mice. Findings: Glycosides, saponins, phenolics, and alkaloids among others were present. Components detected from the isolated yellow oil of S. ovatum were 9-octadecenoic acid (oleic acid) (Rt:20.0, 19.37%), an unsaturated fatty acid, squalene (Rt:25.6, 4.58%), a terpene; 7-tetradecenal (Rt:22.6, 2.40%), an aldehyde and alicyclic compounds like bicycle (3,10) hexan-3-one (Rt:16.7, 0.22%). Quinine-treated mice exhibited the lowest parasite counts of 0.27±0.01 (83.82% mean chemosuppression) at day 4 of therapy while the lowest parasite counts for the isolated oil was 0.95±0.05 (42.92% mean chemosuppression) at day 4 of therapy. Conclusion:The chemosuppressive activities revealed that the isolated oil exhibit significant suppression (P<0.05) of Plasmodium falciparum when compared with the standard, quinine which was evident by the photomicrograph results. This work corroborates the local use of the plants for the treatment of malaria in Southern Nigeria.
Diacyl triazene-N-oxides were synthesized by reaction of p-nitroso, N,N-dimethyl aniline with some acyl hydrazines. The product yield varied from 56%-80.8%. The conditions for optimum yields and spectral characteristics of the products are reported.
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