Synthesis and H_1-Antihistaminic Activity of Some Novel 1-Substituted-4-(3-methylphenyl)-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones(Medicinal Chemistry)

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概要

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• A series of novel 1-substituted-4-(3-methylphenyl)-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones were synthesized by the cyclization of 2-hydrazino-3-(3-methylphenyl) quinazolin-4(3H)-one with various one carbon donors. The starting material 2-hydrazino-3-(3-methylphenyl)quinazolin-4(3H)-one, was synthesized from 3-methylaniline by a novel innovative route. When tested for their in vivo H_1-antihistaminic activity on conscious guinea pigs, all the test compounds protected the animals from histamine induced bronchospasm significantly, whereas the compound 1-methyl-4-(3-methylphenyl)-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-one II was found to be equipotent (percent protection 70.0%) with the reference standard chlorpheniramine maleate (percent protection 71%). Compound II show negligible sedation (7%) when compared to chlorpheniramine maleate (25%). Hence it could serve as prototype molecule for further development as a new class of H_1-antihistamines.

• 公益社団法人日本薬学会の論文
• 2005-08-01

著者

• Yadav Mangae

  Pharmacy Department The Ms University Of Baroda

• Giridhar Rajani

  Pharmacy Department The Ms University Of Baroda

• ALAGARSAMY Veerachamy

  Medicinal Chemistry Laboratory, Periyar College of Pharmaceutical Sciences for Girls

• Alagarsamy Veerachamy

  Medicinal Chemistry Laboratory J.s.s. College Of Pharmacy

関連論文

• Synthesis and H_1-Antihistaminic Activity of Some Novel 1-Substituted-4-(3-methylphenyl)-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones(Medicinal Chemistry)
• Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of Some Novel 2-Phenyl-3-substituted Quinazolin-4(3H) Ones
• Synthesis, Analgesic and Anti-inflammatory Activities of Some Novel 2,3-Disubstituted Quinazolin-4(3H)-ones
• Synthesis and Pharmacological Evaluation of Some 3-(4-Methoxyphenyl)-2-substitutedamino-quinazolin-4(3H)-ones as Analgesic and Anti-inflammatory Agents
• Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of Some Novel 2-Butyl-3-substituted Quinazolin-4-(3H)-ones(Medicinal Chemistry)
• Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of some Novel 2-Methylthio-3-Substituted Quinazolin-4-(3H)-ones (Medicinal Chemistry)
• Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of Some Novel 2-Methyl-3-substituted Quinazolin-4-(3H)-ones (Medicinal Chemistry)

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