Novel Polyhydroquinoline-Hydrazide-Linked Schiff's Base Derivatives: Multistep Synthesis, Antimicrobial, and Calcium-Channel-Blocking Activities
Polyhydroquinoline (PHQ) are the unsymmetrical Hantzsch derivatives of 1,4-dihydropyridines with several biological applications. In this work, twenty-five (<b>3</b>-<b>27</b>) new Schiff's base derivatives of polyhydroquinoline hydrazide were synthesized in excellent to...
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MDPI AG,
2022-11-01T00:00:00Z.
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| 001 | doaj_aa836bb12c6f44b59a3a70f2db2f2c4e | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Zainab |e author |
| 700 | 1 | 0 | |a Haitao Yu |e author |
| 700 | 1 | 0 | |a Najeeb Ur Rehman |e author |
| 700 | 1 | 0 | |a Mumtaz Ali |e author |
| 700 | 1 | 0 | |a Aftab Alam |e author |
| 700 | 1 | 0 | |a Abdul Latif |e author |
| 700 | 1 | 0 | |a Nazish Shahab |e author |
| 700 | 1 | 0 | |a Irfan Amir Khan |e author |
| 700 | 1 | 0 | |a Abdul Jabbar Shah |e author |
| 700 | 1 | 0 | |a Momin Khan |e author |
| 700 | 1 | 0 | |a Ahmed Al-Ghafri |e author |
| 700 | 1 | 0 | |a Ahmed Al-Harrasi |e author |
| 700 | 1 | 0 | |a Manzoor Ahmad |e author |
| 245 | 0 | 0 | |a Novel Polyhydroquinoline-Hydrazide-Linked Schiff's Base Derivatives: Multistep Synthesis, Antimicrobial, and Calcium-Channel-Blocking Activities |
| 260 | |b MDPI AG, |c 2022-11-01T00:00:00Z. | ||
| 500 | |a 10.3390/antibiotics11111568 | ||
| 500 | |a 2079-6382 | ||
| 520 | |a Polyhydroquinoline (PHQ) are the unsymmetrical Hantzsch derivatives of 1,4-dihydropyridines with several biological applications. In this work, twenty-five (<b>3</b>-<b>27</b>) new Schiff's base derivatives of polyhydroquinoline hydrazide were synthesized in excellent to good yields by a multi-component reaction. The structures of the synthesized products (<b>1</b>-<b>27</b>) were deduced with the help of spectroscopic techniques, such as <sup>1</sup>H-, <sup>13</sup>C -NMR, and HR-ESI-MS. The synthesized products (<b>1</b>-<b>27</b>) were tested for their antibacterial and in vitro calcium -channel-blocking (CCB) potentials using the agar-well diffusion method, and isolated rat aortic ring preparations, respectively. Among the series, sixteen compounds were found to inhibit the growth of <i>Escherichia coli</i> and <i>Enterococcus faecalis</i>. Among them, compound <b>17</b> was observed to be the most potent one at a dose 2 µg/mL, with an 18 mm zone of inhibition against both bacteria when it was compared with the standard drug amoxicillin. Eight compounds showed CCB activity of variable potency; in particular, compound <b>27</b> was more potent, with an EC<sub>50</sub> value of 0.7 (0.3-1.1) µg/mL, indicating their CCB effect. | ||
| 546 | |a EN | ||
| 690 | |a polyhydroquinoline | ||
| 690 | |a Hantzsch derivatives | ||
| 690 | |a antibacterial | ||
| 690 | |a calcium-channel-blocking | ||
| 690 | |a spectroscopic data | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Antibiotics, Vol 11, Iss 11, p 1568 (2022) | |
| 787 | 0 | |n https://www.mdpi.com/2079-6382/11/11/1568 | |
| 787 | 0 | |n https://doaj.org/toc/2079-6382 | |
| 856 | 4 | 1 | |u https://doaj.org/article/aa836bb12c6f44b59a3a70f2db2f2c4e |z Connect to this object online. |