1- and 2-substituted naphthalenes: A new class of potential hypotensive agents

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 11, 2004, Pages 2797-2800

  Tandon, Vishnu K ^a   Singh, Kunwar A ^a   Goswamy, Gajendra K ^a  

^a UNIVERSITY OF LUCKNOW   (India)

Author keywords

[No Author keywords available]

Indexed keywords

2 (N 4 PHENYL N 1 PIPERAZINO)METHYLOXYNAPHTHALENE; ANTIHYPERTENSIVE AGENT; BUTYRIC ACID DERIVATIVE; NAPHTHALENE DERIVATIVE; PROPRANOLOL; UNCLASSIFIED DRUG;

ANTIHYPERTENSIVE ACTIVITY; ARTICLE; CAT; CHEMICAL REACTION; CONTROLLED STUDY; DRUG EFFECT; DRUG STRUCTURE; DRUG SYNTHESIS; MANNICH REACTION; NONHUMAN; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTIHYPERTENSIVE AGENTS; BLOOD PRESSURE; CATS; DOSE-RESPONSE RELATIONSHIP, DRUG; NAPHTHALENES; STRUCTURE-ACTIVITY RELATIONSHIP;

FELIS CATUS;

EID: 2342597889     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.03.080     Document Type: Article

References (19)

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12. The hypotensive activity was carried out in the pharmacology division of Central Drug Research Institute, Lucknow, India Pharmacology: Cats (2.5-4.0 kg) were anaesthetized with pentobarbitone sodium (35.0 mg/kg ip) and their blood pressure (BP) was recorded from a carotidartery. The arterial vase was cannulated with a polyethylene catheter, filled with sodium citrate (5%) as anticoagulant and connected to a Hg-manometer. The trachea was intubated and respiration was recorded through a Marey's tambour. BP and respiration were recorded on a kymograph. The left femoral vein was cannulated with a polyethylene tube for injection of drugs and test compound. Contractions of the nictitating membrane due to electrical stimulation of preganglionic sympathetic nerve (50 Hz, 1 ms, 5-10 V for 5-101 s) were recorded through a system of pulleys and frontal wending lever on the kymograp. Responses of intravenous adrenaline (2-4 μg), acetylcholine (1-2 μg), histamine (1-2 μg) and isoprenaline (0.1 μg) on the BP were recorded before and after the administration of 1 and 5 mg/kg iv dose of the test compound. SE was calculated on the basis of three to four experiments carried out for each of the compounds reported in Table 1
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16. 2O (318): C 79.24, H 6.91, N 8.80. Found C 79.20, H 7.0, N 8.84
17. 3 (404): C 74.25, H 6.93, N 6.93. Found C 74.02, H 6.86, N 7.01
18. Proposed structure of 5.
19. 4, filtered and the filtrate concentrated to distill off solvent ether. Compound 1a-f were obtained as solids in 75-90% yields. The analytical data of 1a-f were identical to those obtained by general procedure reported for synthesis of 1 in Ref. 15