acta 2_2015

More documents

Recommendations

Info

276 VIOLETTA KRAJKA-KUèNIAK et al.41. B.A., Henneman. J.R., Rice J.M., Nims R.W.:Carcinogenesis 17, 37 (1996).42. Yang Y., Sharma R., Sharma A., Awasthi S.,Awasthi Y.C.: Acta Biochim. Pol. 50, 319(2003).43. Petermann A., Miene C., Schulz-Raffelt G.,Palige K., Hˆlzer J., Glei M., BˆhmerF.D.: Mol. Nutr. Food Res. 53, 1245 (2009).44. Krajka-Kuüniak V., Kaczmarek J., Baer-Dubowska W.: Food Chem. Toxicol. 46, 1097(2008).45. Nijhoff W.A., Groen G.M., Peters W.H.M.: Int.J. Oncol. 3, 1131 (1993).46. Aliya S., Reddanna P., Thyagaraju K.: Mol.Cell. Biochem. 253, 319 (2003).47. Shimamoto K., Hayashi H., Taniai E., MoritaR., Imaoka M., Ishii Y., Suzuki K. et al.: J.Toxicol. Sci. 6, 775 (2011).48. Krajka-Kuüniak V., Paluszczak J., Celewicz L.,Barciszewski J., Baer-Dubowska W.: FoodChem. Toxicol. 51, 202 (2013).49. Song Y., Manson J., Buring J., Session H. LinS.: J. Am. Coll. Nutr. 24, 376 (2005).50. Jang S.M., Kim M.J., Choi M.S., Kwon E.Y.,Lee M.K.: Metabolism 59, 512 (2010).51. Ross D.: Drug Metab. Rev. 36, 639 (2004).Received: 21. 03. 2014
Acta Poloniae Pharmaceutica ñ Drug Research, Vol. 72 No. 2 pp. 277ñ287, <strong>2015</strong> ISSN 0001-6837Polish Pharmaceutical SocietyDRUG SYNTHESIS1-[(IMIDAZOLIN-2-YL)AMINO]INDOLINE AND 1-[(IMIDAZOLIN-2-YL)AMINO]1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES:NEW INSIGHTS INTO THEIR CIRCULATORY ACTIVITIESFRANCISZEK S•CZEWSKI 1 , ALEKSANDRA WASILEWSKA 1 *, ALAN L. HUDSON 2 ,MEHNAZ FERDOUSI 2 , APOLONIA RYBCZY—SKA 3 , KONRAD BOBLEWSKI 3and ARTUR LEHMANN 31Department of Chemical Technology of Drugs, Faculty of Pharmacy,Medical University of GdaÒsk, DÍbinki 7, 80-211 GdaÒsk, Poland2Department of Pharmacology, University of Alberta, Edmonton, Canada3Department of Pathophysiology, Faculty of Pharmacy, Medical University of GdaÒsk, PolandAbstract: N-[(Imidazolin-2-yl)amino]indolines and N-[(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines,previously described in patent literature as hypertensive agents, were synthesized and tested in vitro for theiraffinities to α 1 - and α 2 -adrenoceptors as well as imidazoline I 1 and I 2 receptors. The compounds most potent ateither α 1 - or α 2 -adrenoceptors were administered intravenously to normotensive Wistar rats to determine theireffects on mean arterial blood pressure and heart rate. Upon intravenous administration at dose of 0.1 mg/kg tonormotensive male Wistar rats, the initial transient pressor effect was followed by long-lasting hypotension andbradycardia. In view of the above results the 1-[(imidazolin-2-yl)amino]indolines and [(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines are now found to possess circulatory profile characteristic of the centrallyacting clonidine-like hypotensive imidazolines.Keywords: imidazolines, indolines, 1,2,3,4-tetrahydroisoquinolines, α-adrenoceptors, imidazoline receptors,hypertensive effect, hypotensive effectImidazoline-containing agents acting at α 2 -adrenoceptors exhibit important pharmacologicaleffects including hypotension, bradycardia, analgesia,sedation, mydriasis, organ-protection, stimulationof growth hormone secretion and decreased outputof endocrine and exocrine secretory glands, suchas decreased insulin secretion and decreased salivation(1-11). On the other hand, the therapeuticpotential of agents which selectively interact withα 1 -adrenoceptors includes nasal congestion, urinaryincontinence as well as sexual, CNS and eating dysfunctions(12-16).It is well established that imidazoline derivativesof type A with methylene bridge between theimidazoline and the aryl ring (Figure 1, X = CH 2 )such as xylometazoline, oxymetazoline and naphazolineinduce an increase in blood pressure due toperipheral α 1 -adrenergic receptor stimulation, whileFigure 1. Imidazoline derivatives with circulatory activity* Corresponding author: e-mail: alwas@gumed.edu.pl277
Page 4:
PHARMACEUTICAL TECHNOLOGY347. £uka
Page 11: Impact of stress factors on optical
Page 14 and 15: 228 ZAHRA SAFAEI et al.the determin
Page 16 and 17: 230 ZAHRA SAFAEI et al.respectively
Page 18 and 19: 232 ZAHRA SAFAEI et al.Concetration
Page 21 and 22: Acta Poloniae Pharmaceutica ñ Drug
Page 23 and 24: Lipophilicity assessment of spirono
Page 31: Acta Poloniae Pharmaceutica ñ Drug
Page 34 and 35: 248 ASHFAQ AHMAD et al.Proposed mec
Page 36 and 37: 250 ASHFAQ AHMAD et al.Figure 5. Re
Page 38 and 39: 252 ASHFAQ AHMAD et al.4. Ha H., Pa
Page 40 and 41: 254 PRITESH DEVBHUTI et al.inversel
Page 42 and 43: 256 PRITESH DEVBHUTI et al.Figure 1
Page 44 and 45: 258 PRITESH DEVBHUTI et al.received
Page 46 and 47: 260 PRITESH DEVBHUTI et al.20. Khia
Page 48 and 49: 262 MARIOLA HERBET et al.The purpos
Page 50 and 51: 264 MARIOLA HERBET et al.rosuvastat
Page 55 and 56: Influence of cloudy apple juice on
Page 61: Influence of cloudy apple juice on
Page 65 and 66: 1-[(Imidazolin-2-yl)amino]indoline
Page 73: 1-[(Imidazolin-2-yl)amino]indoline
Page 76 and 77: 290 TOMASZ KOSMALSKI et al.the lite
Page 78 and 79: 292 TOMASZ KOSMALSKI et al.Antibact
Page 80 and 81: 294 TOMASZ KOSMALSKI et al.66.49(19
Page 85 and 86: Synthesis and in vitro antiprolifer
Page 91: Synthesis and in vitro antiprolifer
Page 94 and 95: 308 ASHRAF M. MOHAMED et al.Cevipab
Page 96 and 97: 310 ASHRAF M. MOHAMED et al.solvent
Page 98 and 99: 312 ASHRAF M. MOHAMED et al.Table 2
Page 100 and 101: 314 ASHRAF M. MOHAMED et al.Table 3
Page 102 and 103: 316 ASHRAF M. MOHAMED et al.teristi
Page 104 and 105: 318 ASHRAF M. MOHAMED et al.20. Che
Page 106 and 107: 320 MANSURAH A. ABDULAZEEZ et al.an
Page 108 and 109: 322 MANSURAH A. ABDULAZEEZ et al.GC
Page 110 and 111: 324 MANSURAH A. ABDULAZEEZ et al.Ta
Page 112 and 113:
326 MANSURAH A. ABDULAZEEZ et al.in
Page 114 and 115:
328 MANSURAH A. ABDULAZEEZ et al.34
Page 116 and 117:
330 SAMINA AFZAL et al.is used as a
Page 118 and 119:
332 SAMINA AFZAL et al.Detection of
Page 120 and 121:
334 SAMINA AFZAL et al.CONCLUSIONAm
Page 122 and 123:
336 BEATA PASKER et al.inhibitory o
Page 124 and 125:
338 BEATA PASKER et al.Figure 2. Ef
Page 126 and 127:
340 BEATA PASKER et al.In conclusio
Page 128 and 129:
342 NASER VAHED DEHKORDI et al.EXPE
Page 130 and 131:
344 NASER VAHED DEHKORDI et al.Anti
Page 133 and 134:
Acta Poloniae Pharmaceutica ñ Drug
Page 135 and 136:
Dissolution properties and kinetic
Page 137 and 138:
Page 139 and 140:
Page 141:
Page 144 and 145:
358 OLADAPO A. ADETUNJI et al.In th
Page 146 and 147:
360 OLADAPO A. ADETUNJI et al.that
Page 148 and 149:
362 OLADAPO A. ADETUNJI et al.Figur
Page 150 and 151:
364 OLADAPO A. ADETUNJI et al.Figur
Page 153 and 154:
Page 155 and 156:
In vitro antimicrobial activity of
Page 157 and 158:
Page 159 and 160:
Page 161:
Page 164 and 165:
378 SHENG LI et al.the developed an
Page 166 and 167:
380 SHENG LI et al.Fisherís exact
Page 168 and 169:
382 SHENG LI et al.Arabia and Jorda
Page 170 and 171:
384 MAGDALENA RATAJCZAK et al.g/mL.
Page 172 and 173:
386 MAGDALENA RATAJCZAK et al.ing d
Page 175 and 176:
Page 177 and 178:
Use of medicines among students of
Page 179 and 180:
Page 181 and 182:
Page 183 and 184:
Page 185 and 186:
Cytotoxicity and antiglucosidase po
Page 187:
Cytotoxicity and antiglucosidase po
Page 190 and 191:
404 ANNA CWYNAR et al.was used to r
Page 192 and 193:
406 ANNA CWYNAR et al.Consequently,
show all

acta 2_2015

Create successful ePaper yourself

Delete template?

Save as template?