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العنوان
Synthesis of certain quinazoline derivatives of pharmaceutical interest /
المؤلف
Abo Dya, Nader El-Maghwry Mostafa.
الموضوع
Pharmaceutical chemistry.
تاريخ النشر
2006.
عدد الصفحات
115 p. :
الفهرس
Only 14 pages are availabe for public view

from 126

from 126

Abstract

Antiinflammatory activity: The obtained results (Table 12) revealed that all the test compounds as well as the standard drug(diclofenac sodium) possess a significant antiinflammatory activity when compared with the control group(given only carrageenin) during the entire period of the experiment. After one hour the rank order of potency as antiinflammatory was as follows;compound number XIVb2> XVIb1> VIII> XIVa1> XVIa2, standard> XIIIb1
Whereas the rank order of potency after two hours was as follows; Compound number VIII, XIVa1> XVIb1> XVIa2>standard> XIVb2, XIIIb1 while at the end of the experiment the rank order of potency was as follows; Compound number XIVa1> VIII, XVIb1> XIIIb1, ,XIVb2, XVIa2> standard indicating that all the test compounds possess antiinflammatory activity more than the standard drug especially compound number (XIVa1) where its antiinflammatory activity was more significantly greater than the standard drug and the other test compounds. However compound (XIVb2) appears toxic since one rat died after two hours and two more rats died after three hours so the dose of this compound should be reduced.Table(12); the antiinflammatory activity of the test compounds as well as diclofenac sodium given intraperitoneally in a dose of 1.0 mg/100gm. of rats.
(Mean S.E) n= 5 rats Group< treatment Initial thickness of rate paws(mm). Initial thickness of rate paw(mm) afterOne hour Two hours Three hours
1 Control (carrageenin only)5.5 a ±0.54 7.25 a ±0.25 7.75 a ±0.47 6.37 a ±0.47
2 Compound no VIII (1.0mg/100gm.b.wt) +carrageenin 4.6 a ±0.23 4.25 bc ±0.14 3.75 c ±0.14 3.37 bc ±0.23. 3 Compound noXIIIb1 (1.0mg/100gm.b.wt) +carrageenin 5.25 a ±0.62 5.25 b ±0.47 4.5 c ±0.28 4.0 bc ±0.28<.4 Compound no XIVa1 (1.0mg/100gm.b.wt) +carrageenin 5.5 a ±0 .28 4.37 bc ±0.2 3.75 c ±0.14 3.12 c ±0.12< -5 Compound no XIVb2 (1.0mg/100gm.b.wt) +carrageenin 4.75 a ±0.77 3.8 c
±0.6 5.25 b ±0.5 4.0 bc ±0.2
6 Compound no XVIa2 (1.0mg/100gm.b.wt) +carrageenin 4.62 a ±0.23 4.4 bc ±0.24 4.0 c
±0.2 4.0 bc ±0.28- 7Compound noXVIb1 (1.0mg/100gm.b.wt) +carrageenin 4.8 a ±0.14 3.87 c ±0.12 3.87 c ±0.12 3.37 bc ±0.23
8 Diclofenac sodium(standard) (1.0mg/100gm.b.wt) +carrageenin 5.7 a ±0.25 4.5 bc ±0.28 4.25 c ±0.25 4.1 b±0.1
Means within the same column bearing different superscripts are significantly at(p ). Antihypertensive activity Table (13) illustrates that all the test compounds together with the standard drug significantly lowered the mean arterial blood pressure of phenobarbitone anaesthetized dogs, with the rank order of potency as follows. Standard drug>Vh>Vd>Ve>Vb. The antihypertensive activity of the standard drug was more significantly higher than that of the test compounds Table(13); The antihypertensive activity of the test compounds and standard (doxazosin
mesylate) in phenobarbitone anaesthetized dogs (Mean S.E) n= 4 dogs Group Treatment Mean arterial blood pressure Control Medodrine HCl 2.5 mg/20kg.of dog. 167.5±1.42 a Vb 2.5 mg compound (Vb)/20kg. of dog. 150±2.01 b
Vd br>2.5 mg compound (Vd)/20kg. of dog.148.5±1.42 b Ve
2.5 mg compound (Ve)/20kg. of dog.
< b Vh < 2.5 mg compound (Vh)/20kg. of dog. < 146.25±1.98 b standard < 2.5 mg doxazosin mesylate/20kg.