Synthesis, Characterization, and Antihypertensive Evaluation of Some Novel 2,2,8,8-Tetramethyl-2,3,7,8-tetrahydro-4,6-diamino-3,7-dihydroxy-6,7-epoxy-benzo-[1,2-b:5,4-b′]dipyran Derivatives
Table 1
Antihypertensive activity of the benzodipyran derivatives 7a–e and 8a–c.
Comp. code
Parameter
Baseline
With adrenaline
With test alone
With test + adrenaline
Inference
7a
SBP
101.2 (±0.693)
147.8 (±1.308)
140.6 (±1.121)
141.4 (±2.040)
Minimal activity
DBP
57.9 (±0.769)
79.2 (±0.861)
83.2 (±1.240)
73.9 (±1.167)
MABP
77.5 (±0.480)
143.9 (±1.202)
107.2 (±1.387)
109.3 (±0.894)
HR
196.5 (±3.201)
291.9 (±3.158)
248.1 (±3.118)
260.2 (±3.201)
7b
SBP
106.4 (±0.482)
160.6 (±1.198)
124.6 (±1.389)
126.0 (±1.406)
Antihypertensive
DBP
47.8 (±0.927)
75.1 (±3.054)
53.0 (±0.107)
59.3 (±1.541)
MABP
72.97 (±0.890)
122.1 (±1.883)
83.44 (±0.488)
109.2 (±0.931)
HR
299.9 (±3.106)
326.0 (±5.431)
321.0 (±0.557)
302.4 (±3.658)
7c
SBP
105.7 (±1.203)
148.2 (±1.055)
127.1 (±1.031)
132.4 (±2.049)
Antihypertensive
DBP
63.1 (±1.202)
86.5 (±1.218)
62.1 (±3.983)
84.2 (±1.160)
MABP
68.1 (±0.399)
109.1 (±0.963)
119.8 (±1.991)
101.3 (±0.896)
HR
278.8 (±2.697)
302.1 (±2.616)
298.7 (±2.065)
296.4 (±3.120)
7d
SBP
120.8 (±1.061)
162.7 (±1.211)
143.6 (±0.892)
121.7 (±0.231)
Antihypertensive
DBP
64.2 (±0.381)
86.8 (±0.665)
84.6 (±0.820)
71.1 (±1.858)
MABP
98.2 (±0.485)
120.7 (±1.390)
111.7 (±1.057)
99.2 (±1.524)
HR
209.5 (±1.161)
267.2 (±1.108)
248.9 (±2.868)
266.8 (±2.830)
7e
SBP
108.9 (±0.519)
135.4 (±1.328)
160.8 (±0.940)
167.0 (±3.027)
Moderately active
DBP
61.0 (±1.291)
87.1 (±1.966)
68.2 (±1.332)
91.3 (±1.857)
MABP
88.9 (±1.135)
102.1 (±1.503)
106.2 (±1.887)
119.3 (±0.197)
HR
232.2 (±2.097)
241.0 (±3.088)
209.2 (±3.210)
216.1 (±2.118)
8a
SBP
128.8 (±3.62)
182.7 (±2.63)
168.8 (±0.85)
198.0 (±3.43)
Minimal activity
DBP
70.89 (±2.33)
108.4 (±2.02)
134.3 (±0.95)
143.1 (±3.93)
MABP
103.7 (±3.28)
139.3 (±1.532)
149.9 (±1.152)
163.9 (±0.852)
HR
286.4 (±5.128)
304.6 (±3.210)
338.6 (±3.308)
341.9 (±1.409)
8b
SBP
106.8 (±2.367)
178.6 (±1.349)
179.3 (±2.101)
189.3 (±0.239)
No activity
DBP
84.0 (±2.105)
126.2 (±0.968)
128.7 (±1.151)
148.6 (±1.059)
MABP
112.9 (±2.250)
146.7 (±2.152)
182.3 (±1.788)
195.6 (±1.272)
HR
306.3 (±3.977)
331.8 (±3.300)
34.6 (±2.312)
361.8 (±2.008)
8c
SBP
89.82 (±1.363)
121.1 (±2.015)
143.3 (±1.38)
147.5 (±1.843)
Minimal activity
DBP
67.1 (±0.379)
89.5 (±0.895)
102.8 (±3.516)
123.3 (±2.331)
MABP
88.0 (±3.837)
135.5 (±1.293)
142.8 (±2.870)
150.2 (±0.922)
HR
269.8 (±3.897)
302.1 (±4.430)
348.5 (±3.772)
356.9 (±1.573)
SBP: systolic blood pressure, DBP: diastolic blood pressure, MABP: mean arterial blood pressure, and HR: heart rate. Values are expressed in mean ± S.E.M. Number of readings: 03.