Abstract
Ten substituted phenacyl derivatives of 4-hydroxypiperidine were synthesized and studied for their effects on the mean arterial blood pressure (MABP) in normotensive anaesthetized rats and smooth muscles contractions of isolated rabbit jejunum. Two derivatives caused fall in blood pressure at the dose of 10≈20 mg/kg and one rise in blood pressure at the dose of 20 mg/kg. Two compounds exhibited biphasic response (hypotensive followed by hypertensive) and one gave triphasic response at 10 mg/kg dose. Rest of four derivatives were found devoid of any effect on mean arterial blood pressure up to the dose of 30 mg/kg. All the derivatives except two caused relaxant effect on the spontaneous contraction of rabbit jejunum at the dose range of 0.1≈2 mg/kg.
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References Cited
Archibald, J. L., Baum, T. and Childress, S. J., 1,4-Bis (2-indol-3-ylethyl)piperidines.J. Med. Chem., 13, 138–40 (1970).
Bolton, T. B., Mechanism of action of transmitters and other substances on smooth muscles.Physiol. Rev., 59, 606–718 (1979).
Brading, A. F.,TIPS., How do drugs initiate contraction in smooth muscles? 2, 259–61 (1981).
Clark, R. D., Caroon, J. M., Kluge, A. F. and Okada, M. D., Synthesis and antihypertensive activity of '4-substituted spiro(4H-3,1-benzoxazine-4, '4-piperidine)-2(1H)-ones.J. Med. Chem., 26, 657–61 (1983).
Gilani, A. H., Janbaz, K. H., Lateef, A. and Zaman, M., Calcium channel blocking activity ofArtemisia scoparia extract.Phytother Res., 8, 161–65 (1994).
Maillard, J., Delaunary, P., Langlois, M. and Vo Van, T., Spiro-heterocyclic cycloalkane compounds-IV. Synthesis of '4-piperidine-5-spiro-2-oxazolidinones.Bull. Soc. Chim. Fr., 4, 1394–98 (1970).
Mailland, J., Langlois, M., Delaunary, P., Vo Van, T., Chenu, J., Morin, R., Benharkate, M., Manuel, C. and Motosso, F., Cycloalkane spiroheterocyclic compounds.J. Med Chem., 15, 1123–28 (1972).
Mauleon, D., Pujol, M. D. and Rosell, G., Synthesis and β-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols.J. Med. Chem., 31, 2122–26 (1988).
Mcleod, L. C. (1970).Pharmacological Experiments on Intact Preparations (E & S Livingstone, Edinburg) p. 63.
Saeed, M., Ahmad, M., Saify, Z. S., Zia, A., Ahmad, V. U. and Iqbal, Z., Synthesis and analgesic activity of 4-piperidinol derivatives.Pak. J. Pharm. Pb. Univ. Lahore 9, 37–42 (1996).
Saeed, M., Saify, Iqbal, Z. and Islam, N. Synthesis of 4-hydroxipiperidine derivatives and their screening for analgesic activity.Arch. Pharm. Res., 20, 338–341 (1997).
Saify, Z. S., Saeed, M., Khan, A. Moazzam, H., Ahmad, V. U., Zia, A. and Haleem, D. J. Synthesis of some piperidine derivatives of potential analgesic activity. Proceed.19th IUPAC Symp. on Chem. Nat. Products. Kar., Pak., 75–83 (1994a).
Saify, Z. S., Saeed, M., Moazzam, H., Yasmeen, A., Zafar, A. and Haleem, D. J., Studies on the effect of 4-hydroxy-4-phenylpiperidine derivative (4-HPPD) on mice brain dopamine metabolism.Proceed. ISBBP, Univ. Kar., Pak., 1, 36–39 (1994b).
Takai, H., Obase, H., Nakamizo, N., Teranishi, M., Kubo, K., Shuto, K. and Hashimoto, T., Synthesis and pharmacological evaluation of piperidine derivatives with various heterocyclic rings at the 4-position.Chem. Pharm. Bull., 33, 1104–1115 (1985a).
Takai, H., Obase, H., Teranishi, M., Karasawa, A., Kubo, K., Shuto, K., Kasuya, Y., Hashikami, M., Karashima, N. and Shigenobu, K., Spiropiperidines-1. Synthesis of '1-substituted spiropiperidine derivatives and evaluation of their antihypertensive activity.Chem. Pharm. Bull., 33, 1129–39 (1985b).
Weiner, N. (1985). In:Goodman and Gilman's Pharmacological Basis of Therapeutics, Gilman, A. G., Goodman, L. S., Rall, T. W., and Murad, F. ed. (MacMillan, New York), p. 145.
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Saeed, M., Saify, Z.S., Gilani, A.H. et al. Studies on the effects of piperidine derivatives on blood pressure and smooth muscles contractions. Arch. Pharm. Res. 21, 370–373 (1998). https://doi.org/10.1007/BF02974628
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DOI: https://doi.org/10.1007/BF02974628