Synthesis, Characterization and Pharmacological Evaluation of Thiosalicylamide Derivative as a Class of Calcium Channel Blocker

Authors

  • Anirudh Joshi B. R. Nahata College of Pharmacy, Mandsaur (M.P.)
  • Dinanath Shrivastava B. R. Nahata College of Pharmacy, Mandsaur (M.P.)
  • Chain Singh Base Jodhpur National University, Jodhpur Rajasthan, India

DOI:

https://doi.org/10.7439/ijpc.v6i1.2874

Keywords:

Preeclampsia, Pregnancy, Alkaline phosphatase, Placenta, Ischemia

Abstract

Objective: Hypertension is one of the major causes of the cardiovascular diseases and in the later stages, it also damages the brain, kidneys, eyes and coronary arteries. It is also life threatening as it causes heart strokes and attacks. The calcium channels regulates blood pressure by muscle contraction triggered by neurotransmitter release to electrical excitation.

Method: Calcium channel blocker drugs reduce intracellular calcium transfer to limit ATP release to reduce muscle cell contractility. They act, especially on the nodal tissues in the heart and arterial smooth muscle cells in which only slow calcium channel blockers opens without triggering of fast sodium ion channels. Pharmacophore approach is employed to generate novel thiosalicylamide derivatives having calcium channel blocking activity for treatment of hypertension.

Result: These novel thiosalicylamide derived lead molecules are synthesized and tested for their in-vivo pharmacological activity by using isolated guinea-pig ileum muscles.

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Author Biographies

  • Anirudh Joshi, B. R. Nahata College of Pharmacy, Mandsaur (M.P.)

    Assistant Professor,

    Department of Pharmaceutical and Medicinal Chemistry

  • Dinanath Shrivastava, B. R. Nahata College of Pharmacy, Mandsaur (M.P.)

    Professor,

    Department of Pharmacology

  • Chain Singh Base, Jodhpur National University, Jodhpur Rajasthan, India

    Professor,

    Department of Pharmaceutical and Medicinal Chemistry

References

James S. A development of a database analysis that provides putative metabolic enzyme reactions for Ligand-based drug design. CompBio and Chem 2009; 149

Larsen PK. Text book of Drug Design and Discovery, published by British Library Cataloguing Publication; first Indian reprint 2004: 1-33.

Tripathi KD. Antihypertensive drugs in the Essentials of Medical Pharmacology. Jaypee brothers medical publishers Pvt. Ltd., New Delhi, 2003;5: 503-504.

Kishor SJ. Recent advances in selective a1-adrenoreceptor antagonists as antihypertensive agents. Bioorg and Med chem 2008;16: 4759-4800.

Williams and Wilkins. Illustrated Reviews: Pharmacology. 2006;2: pp 213-214.

www.google.com / www.neurosearch.com on 23/03/2010.

Rang HP, Dale MM, Ritter JM, Flower RJ. The Heart. Pharmacology. Elsevier publisher. 2007;6: 54-58.

Striggow F. Verapamil and diltaizem inhibit receptor-operated calcium channels and intracellular calcium oscillations in rat hepatocytes. Federation of European, Biochemical science, 1993;318: 341-344.

Snutch TP. Chronic and Neuropathic Pain: The N-type Calcium Channel Comes of Age.J Amer Sci Exp Neurotherap 2005;2(4): 662-670.

www.wikipedia.org/T-type_calcium_channel on 23/03/2010

www.online-medicaldictionary.org/L+Calcium+Channel on 15/03/2010.

www.google.com / www.neurosearch.com on 23/03/2010.

Rang HP, Dale MM, Ritter JM, Flower RJ. The Heart. Pharmacology Elsevier 2007;6: 54-58.

Remington. Calcium channel blocker. The science and practice of pharmacy.2000;20: 1290.

Barar FSK. Antianginal drug Essential of pharmacotherapeutics 2000;3: 271.

Mehanna AS, Kim JY Kim JT. United States Patent 2003;6: 541,479 B1.

Lee JY. Growth inhibition of human cancer cells in vitro by T-type Calcium channel blockers. J bioorg and med chem 2006;16: 5014-5017.

Mehanna A, Kim JY. Design, Synthesis, and Biological testing of thiosalicylamide as a novel class of calcium channel blocker. J bioorg and med chem 2005;13: 4323-4331.

Pergament E. Calcium channel blockers and pregnancy. Illinois Teratogen Information Service 1996;5.

www.wikipedia.org/Calcium_Channel_Blocker on 24/03/2010.

Parks R. Calcium channel blockers for coronary artery disease, Heath home 2008.

www.en.worldlifeexpectancy.com/sort.php on 24/03/2010

Silverberg MA. Toxicity and Calcium Channel Blocker. Medicine Specialties 2009.

www.yourtotalhealth.ivillage.com/calcium-channel-blockers on 24/03/2010.

Horowitz BZ. Toxicity, Calcium Channel Blocker.Medicine Specialties 2008.

Tripathi KD. Antihypertensive Drugs Essentials of Medical Pharmacology. 2003;5: 504-506.

www.texasheart.org/HIC/Topics/Meds/calciumchannelblockermedicinalchemistry.com. on 24/03/2010.

www.srspharma.com/calcium-channel-blockers.htm. on 25/03/2010.

Klabunde RE. Calcium channel blocker cardiovascular pharmacology concepts. 2008.

Craig RC, Stitzel RE. Calcium Channel Blocker. Modern Pharmacology with Clinical Application, 2008;5: 218-224.

Bahl BS and Bahl A. Text Book of Advanced Organic Chemistry. Published by S. Chand & Company 2004;19: 202-204.

March J. Advanced Organic Chemistry and Reaction, Mechanism and Structure. A Wiley

Pavia, D.L.; Lampman, G. M.; Kriz, G.S.; Vyvyan, J. R. ;

Silverstein RM and Webster FX. Spectrometric Identification of Organic Compounds. Published by library of congress cataloging publication, reprint 1998;76: 149.

Fujita M, Ito S, Ota A. Synthesis of calcium channel antagonistic activity of Benzothiazine. C.R.L. Santen Pharmaceutical Co., Ltd., J Med Chem 1989.

Yamamoto K, Fujita M, Tabashi, K. Synthesis and SAR of Benzothiazepine derivatives as novel calcium antagonists. Santen Pharmaceutical Co. Ltd., J Med Chem 1987.

Gualtieri F, Teodori E, Bellucci C. SAR studies in the field of calcium channel antagonist effect of Verapamil like compounds. Santen Pharmaceutical Co. Ltd., J Med Chem 1985.

Fossheim R, Svarteng K, Mosted A.Crystal Structure and Pharmacological Activity of Calcium Channel Antagonist Verapamil like compound. Norway and School of Pharmacy USA, J Med Chem 1981.

Luis MM, Aguilar A. Effect of Gnaphalium conoideum HBK on Guinea pig airway smooth muscle: role of L-type Calcium Channels. J Bio and Biomed Sci 2004.

Pavia DL, Lampman GM, Kriz GS, Vyvyan JR. Infrared Spectroscopy. Spectroscopy. Cengage Learning India 2007: pp 26-92.

Godfraind T, Miller R, Wibo M. Calcium Antagonism and Calcium entry Blockade. Pharmacol Rev 1986;38: 321

Gilani AH, Bashir S, Janbaz KH, Shah AJ. Presence of Cholinergic and Calciun Channel Blocking Activities Explains the traditional use of Hibiscus Rosasinensis in Constipation and Diarrhoea. J of Ethnopharmaco 2005;102: 289-294.

Kulkarni SK. Hand Book of Experimental Pharmacology. 1999; 3: Vallabh Prakashan, pp 13.

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Published

2016-01-31

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Section

Research Articles

How to Cite

1.
Synthesis, Characterization and Pharmacological Evaluation of Thiosalicylamide Derivative as a Class of Calcium Channel Blocker. Int J of Pharm Chem [Internet]. 2016 Jan. 31 [cited 2025 Jun. 15];6(1):01-22. Available from: https://ssjournals.co.in/index.php/ijpc/article/view/2874