You are on page 1of 1

Abstract :- Depression is potentially life-threatening disease popular worldwide. It is neither restricted to age or social boundaries.

If left untreated, it may lead even to committing suicide. There are different chemical moieties showing
antidepressant properties such as benzodiazepines, hydrazones, imidazoles, indoles, piperazines, piperidines, pyrazolines, pyrimidines, pyrrolidones, quinazolines, quinolines, thiadiazoles and triazoles. Among all these chemical moieties, the pyrazolines possess a broad spectrum of pharmacological activities such as analgesic, antipyretic, anti-inflammatory, insecticide, uricosuric, antiepileptic, antidepressant, antimicrobial, anticancer, antitubercular, hypotensive, antinociceptive and antioxidant activity. The current presentation highlights on the pyrazoline derivatives having antidepressant property. It has been found that most of the substitutions are taking place in the 1st, 2nd, 3rd and 5th position to exhibit antidepressant property. The various substitutions are 3-(2-thienyl)pyrazolines derivatives; 1,3,5-triphenyl-2-pyrazolines; 3-(2-hydroxy naphthalen-1-yl)-1,5-diphenyl-2-pyrazolines; 3,5-diphenyl-2-pyrazolines; 1,3,5trisubstituted pyrazolines and 3-(2-furyl)-pyrazolines. Among the various substituted pyrazolines derivatives, antidepressant activity was found to be the best in 3,5-diphenyl-2-pyrazolines and the least in 3-(2-furyl) derivatives. Although rest of the derivatives show moderate activity. These conclusions were drawn on the basis of results obtained from Duration of Immobility Test.

Introduction :- Depression is a major heterogeneous mood disorder. Chronic and acute depression interfere
severely in ones healthy life, consequently causing a discontinuation in the normal physical, mental and social well-being of the affected patient and the family from which he belongs, drives him even to commit suicide. It is a state of low mood. Chemically pyrazolines can be characterized by a five-membered heterocyclic ring structure containing two nitrogen atoms in it along with a double bond. They are classified as an important class of heterocyclic compounds due to their pronounced biological and pharmacological activities.

Among the trisubstituted pyrazolines; 1,3,5-Trisubstituted Pyrazolines were the best to exhibit antidepressant property as synthesized by Ozan Ruhoglu et al.4 Derivative mentioned below reported to have duration of immobility time of 4.572.92 sec against standard drug Tranylcypromine sulfate with duration of immobility time of 49.712.11 sec.

Ten new 3,5-Diphenyl-2-pyrazoline derivatives were synthesized by reacting 1,3-Diphenyl-2-propen-1-one with hydrazine hydrate by Erhan Palaska et al and for the evaluation of the antidepressant property, these compounds were subjected to the Porsolt Behavioral Despair Test on SwissWebster mice.1 The most potent was derivative with duration of immobility time of 22.36.0 sec whereas the standard drug Tranylcypromine sulfate (20mg/kg) has duration of immobility time of 9.62.6 sec.

Zahul Ozmedin et al designed and synthesized a set of derivatives of 3-(2-Thienyl) pyrazolines, out of which the given derivative was found to be the most potent having duration of immobility time of 4315.3 sec whereas standard drug Tranylcypromine sulfate showed duration of immobility time of 5711.6 sec.5

Five new 1,3,5-Triphenyl-2-pyrazolines were synthesized by reacting 1,3-Diphenyl-2-propene-1-one with phenyl hydrazine hydrochloride and another five new 3-(2-Hydroxynaphthalen-1-yl)-1,5-diphenyl-2-pyrazolines were synthesized by reacting 1-(2-Hydroxynaphthyl)-3-phenyl-2-propene-1-one with phenyl hydrazine hydrochloride. The experiments were performed by Y. Rajendra Prasad et al.2 The most potent derivative mentioned below has duration of immobility time of 22.954.21 sec and the standard drug Clomipramine (20mg/kg) has immobility time of 18.682.25 sec.

Twelve 1-Phenyl-, 1-thiocarbamoyl- and 1-N-substituted thiocarbamoyl-3-(2-furyl)-5-phenyl/(2-furyl)-2pyrazoline derivatives were synthesized by Zuhal Ozdemir et al.6 The nonselective MAO inhibitory activity of the compounds were investigated by Duration of Immobility test on albino mice and the most potent compound shown below has duration of immobility time of 13912 sec and the standard drug Tranylcypromine sulfate(10mg/kg, ip) with duration of immobility time of 5711.6 sec.

P. Iyidogan et al further investigated the 1,3,5-Trisubstituted pyrazolines and came across synthesizing a new set of derivatives.3 Major portion of the derivatives possess low potency but mention is necessary for the given derivatives with duration of immobility time of 73.10 sec and the standard drug Tranylcypromine sulfate with duration of immobility time of 246.6 sec.

Conclusion :- Among the various substituted pyrazolines derivatives, antidepressant activity determined by
immobility time was found to be the best in 3,5-Diphenyl-2-pyrazolines and the least in 3-(2-Furyl) derivatives. Although rest of the derivatives show moderate activity. The conclusions were obtained form the results of Duration of Immobility Tests.

References :1. Palaska, Erhan; Aytemira, Mutlu; Tayfun Uzbay, I.; Erol, Dilek. Synthesis and antidepressant activities of some 3,5-diphenyl-2pyrazolines. Eur. J. Med. Chem., 2001. 36, 539543. 2. Rajendra Prasad, Y.; Lakshmana Rao, A.; Prasoona,L.; Murali, K. and Ravi Kumar, P. Synthesis and antidepressant activity of some 1,3,5-triphenyl-2-pyrazolines and 3-(2-hydroxy naphthalen-1-yl)-1,5-diphenyl-2-pyrazolines. Bioorg. Medicinal Chem. Lett. 2005, 15, 50305034. 3. Iyidogan, P.; Ozdemir, Z.; Kandilci, B.; Gumusel, B.; ali, U.; Bilgin, A. A. Synthesis of some new 1, 3, 5-trisubstituted pyrazolines with antidepressant and anticonvulsant activities. J. Fac. Pharm. , 2005, 38(1), 47-56. 4. Ruhoglu, Ozan; Ozdemir, Zuhal; alis Unsal; Gumuelb, Buent; and Bilgin, A. A. Synthesis of and pharmacological studies on the antidepressant and anticonvulsant activities of some 1, 3, 5-trisubstituted pyrazolines. Arzneim.-Forsch./Drug Res. 2005, 55, 43124336. 5. Ozdemir, Zuhal; Kandilc, Buraki H.; Gumusel, Bulent; Calis, Unsal; and Bilgin, A. A. Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-thienyl) pyrazoline derivatives. Arch. Pharm. Chem. Life Sci., 2008, 341, 701 707. 6.Ozdemir, Zuhal; Burak Kandilci, H.; Gumus xel, Bulent; Unsal C; alsx, A.; Bilgin, Altan. Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-furyl)-pyrazoline derivatives. Eur. J. Med. Chem., 2007, 42, 373-379.

Acknowledgement :- The authors are sincerely thankful to Dr.Monika Gulati, Dean, Lovely School of Pharmaceutical Sciences, Lovely Professional University for her kind support which led to the fruitful completion of the proposed
presentation.