Antibacterial activity: The antibacterial activity of test compounds shows that the newly synthesized Benzylpiperazine derivatives (IVP a–e) exhibited mild to moderate antibacterial activity against the test organisms employed in the present investigation. However, the degree of inhibition varied with the test compound and the test bacterium.
Staack, R.F., Fritschi, G. and Maurer, H.H. (2002), ‘Studies on the metabolism and toxicological detection of the new designer drug N-benzylpiperazine in urine using gas chromatography-mass spectrometry’, Journal of Chromatography B, Analytical Technologies in the Biomedical and Life Sciences, Volume 773, No 1, pp. 35–46.
(z) "Manufacture" means the production, preparation, propagation,compounding, conversion or processing of a controlled substance other than methamphetamine, eitherdirectly or indirectly, by extraction from substances of natural origin,or independently by means of chemical synthesis, or by a combination ofextraction and chemical synthesis, and includes any packaging orrepackaging of the substance or labeling of its container, except thatthis term does not include: (1) by an ultimate user, the preparation or compounding of a controlled substance for his or her own use; or (2) by a practitioner, or his or her authorized agent under his or her supervision, the preparation, compounding, packaging, or labeling of a controlled substance: (a) as an incident to his or her administering or dispensing of a controlled substance in the course of his or her professional practice; or (b) as an incident to lawful research, teaching or chemical analysis and not for sale.
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Synthesis of α-Bromo ethyl aceto acetate (II): Mix 1.5 mM of ethyl aceto acetate (I), 7.5 mM of KBr, 7.5 ml of 1M HCl and 7.5 ml of tolune then stir them well at room temperature and add saturated solution of NaHCO3 sufficiently finally extracted with ethyl acetate.
INTRODUCTION: Benzylpiperazines and its derivatives are versatile type of ligands have attracted considerable pharmaceutical interest due to their antibacterial 1, 2, 3 antifungal 4, 5, 6 antitumor and anthelmintic 7 activities. Benzylpiperazines have drawn great interests for their high potential biological activity especially for their antitumor activity when linked with thiosemicarbazides increases their antimicrobial and antitumor activity 9.
Synthesis of Ethyl 2-(4-(4-substituted) benzyl piperazin-1-yl)-3-oxobutanoate (III): Mix 0.012M of Br-EAA (II) and 0.01M of substituted benzylpiperazine in ethanol and reflux for 1-2 hours finally compleation of reaction was confirmed by TLC and separate.
Synthesis of 4-(4-(4-substituted) Benzyl piperazin-1-yl)-5-methyl - 2, 4 - dihydro-3H-pyrazol-3-one (IV): Take 0.01M of Ethyl 2-(4-(4-substituted) benzyl piperazin-1-yl)-3-oxobutanoate (III) and excess of hydrazine hydrate in acetic acid and reflux to produce title compounds.
ABSTRACT: Synthesis of 6-Methyl-2, 4-dihydro-3H-pyrazol-3-one- 4- (4-substituted) Benzylpiperazine derivatives IVP a-e was carried out by bromination of Ethyl aceto acetate (I) with KBr. The reaction was carried out in the presence of Hydrochloric acid and tolune to produce Bromo-ethyl aceto acetate (II), it is further condensed with substituted Benzylpiperazines in presence of ethanol to obtain condensed compound (III). This upon cyclization with excess of hydrazine hydrate will produce title compounds. All the title compounds IVP a-e were screened for possible antibacterial activity against P. Vulgaris, S. Aureas, E. Coli, B. Subtillus and antifungal activity against Altenaria, Culvalaria, C. Albicans and A. Niger. Among the compounds synthesized IVPb and IVPc demonstrated good antibacterial activity, IVb, IVc, and IVe showed good antifungal activity. The activities of the synthesized compounds are compared with the standard and other test compounds. The structures of synthesized compounds were established by elemental analysis, IR, H NMR and Mass spectral data.
TABLE 1: PHYSICAL DATA OF 4-(4-SUBSTITUTED-4-BENZYLPIPERAZIN-1-YL)-5-METHYL-2,4-DIHYDRO-3H-PYRAZOL-3-ONE (IVP a-e)
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SYNTHESIS, CHARECTERIZATION AND ANTIMICROBIAL ACTIVITY OF 5-METHYL -2, 4-DIHYDRO-3H-PYRAZOL-3-ONE-4-(4-SUBTITUTED) BENZYLPIPERAZINE DERIVATIVES