About Author:
ANAND GAURAV, SMITA SINGH
M.Pharm,
Assistant Professor
Abstract:
The importance of the phthalazine as a nucleus with medicinal properties is well established, since many decades. This nucleus possess potent anticonvulsant activity with high protection index value that why this property is use for the treatment that are related to mental disorder, like seizures. Phthalazine and its derivatives possessing triazines nucleus has attracted great attention in recent years due to wide variety of biological activity particularly anticonvulsant activity keeping in view the continuing interest in phthalazine and its derivatives. The present study is aimed at synthesizing safer and effective anticonvulsant triazolo-phthalazine derivatives to evaluate them for anticonvulsant activity.
|
Compounds |
R2 |
R1 |
|
A |
Cyclooctanol |
Phenyl |
|
B |
Cyclooctanol |
Trifloromethyl benzene |
|
C |
Cyclooctanol |
Toluene |
|
D |
Cycloheptanol |
Phenyl |
|
E |
Cycloheptanol |
Trifloromethyl benzene |
|
F |
Cycloheptanol |
Toluene |
Experimental work-
For control group
Group 1: Normal control (NC) received normal saline (10 ml/kg, I .p)
Six Swiss albino mice (20-30 gm) were taken and Saline solution (dose 10 ml/kg) was administered I.P in each mice. After 30 min of administration of PTZ (dose 75 mg/kg, i.p) was administered and then the latency of tonic convulsion was recorded for 30 min.
For standard group
Group 2: NC rats treated with Diazepam (0.5 mg/kg, i.p)
Six Swiss albino mice (20-30 gm) were taken and Diazepam solution (dose 0.5 mg/kg) was administered i.p in each mice. After 30 min of administration of PTZ (dose 75 mg/kg, i.p) was administered and then the latency of tonic convulsion was recorded for 30 min.
For test group
Group 3: NC rats treated with (PEG 400+derivatives) solution (100 mg/kg)
Six Swiss albino mice (20-30 gm) were taken and derivatives solution (dose 0.5 mg/kg) was administered i.p in each mice. After 30 min of administration of PTZ (dose 75 mg/kg, i.p) was administered and then the latency of tonic convulsion was recorded for 30 min.
Result
|
S. No. |
Body Weight (gm.) |
Treatment |
No. of animals convulsed/ No. used |
Animals Protected (%) |
Latency of Tonic Convulsion (min.) |
|
A |
22.50 |
PTZ |
1/1 |
0 |
4.20 |
|
B |
20.50 |
PTZ |
1/1 |
0 |
5.20 |
|
C |
18.50 |
PTZ |
1/1 |
0 |
5.50 |
|
D |
21.00 |
PTZ |
1/1 |
0 |
4.00 |
|
E |
23.00 |
PTZ |
1/1 |
0 |
4.06 |
|
F |
19.00 |
PTZ |
1/1 |
0 |
5.00 |
|
S. No. |
Body Weight (gm.) |
Treatment
|
No. of animals convulsed/ No. used |
Animals Protected (%) |
Latency of Tonic Convulsion (min.) |
|
1 |
30.00 |
A+PTZ |
1/1 |
0 |
4.50 |
|
2 |
25.50 |
B+PTZ |
1/1 |
0 |
5.10 |
|
3 |
18.50 |
C+PTZ |
1/1 |
0 |
5.70 |
|
4 |
27.50 |
D+PTZ |
1/1 |
0 |
4.30 |
|
5 |
26.00 |
E+PTZ |
1/1 |
0 |
6.50 |
|
6 |
23.50 |
F+PTZ |
1/1 |
0 |
3.10 |
(A, B, C, D, E and F are derivatives that are synthesized)
Conclusion-
The importance of the triazolo nucleus is well established in the field of pharmaceutical chemistry. Different triazolo-phthalazine derivatives were prepared. In the present study synthesis and pharmacological screening of triazolo-phthalazine derivatives were carried out and substitution were made at position 3 and 6. The compounds B, C were found most active against the convulsion while compounds A, D, E and F found less active with in the dose 100mg/kg. All derivatives showed different effectiveness against the convulsion.
References:
Corelli, F.; et al, J. Med. Chem 2008, 51, pg.5125.
Quan, Z. S.; et al, European Journal of Medicinal Chemistry 2009, 44, pg.1265.
Yusun, X.; et al. European Journal of Medicinal Chemistry 2006, 29, pg.1080-1085.
Reference ID: PHARMATUTOR-ART-1028
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