Synthesis and Modeling Studies of Furoxan Coupled Spiro-Isoquinolino Piperidine Derivatives as NO Releasing PDE 5 Inhibitors
| Autor: | Prafulla B. Choudhari, Zubaidha Pudukulathan, Manish S. Bhatia, Swami Prabhuling, Tapan Kumar Mohanta, Yasinalli Tamboli, Ahmed Al-Harrasi |
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| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
spiro-isoquinolino piperidine
Furoxan Medicine (miscellaneous) Phosphodiesterase Pharmacology Article General Biochemistry Genetics and Molecular Biology Intracellular messengers PDE 5 inhibitors Nitric oxide chemistry.chemical_compound lcsh:Biology (General) chemistry nitric oxide Piperidine Neurotransmitter lcsh:QH301-705.5 Cyclic guanosine monophosphate Intracellular furoxan |
| Zdroj: | Biomedicines Volume 8 Issue 5 Biomedicines, Vol 8, Iss 121, p 121 (2020) |
| ISSN: | 2227-9059 |
| DOI: | 10.3390/biomedicines8050121 |
| Popis: | Nitric oxide (NO) is considered to be one of the most important intracellular messengers that play an active role as neurotransmitter in regulation of various cardiovascular physiological and pathological processes. Nitric oxide (NO) is a major factor in penile erectile function. NO exerts a relaxing action on corpus cavernosum and penile arteries by activating smooth muscle soluble guanylate cyclase and increasing the intracellular concentration of cyclic guanosine monophosphate (cGMP). Phophodiesterase (PDE) inhibitors have potential therapeutic applications. NO hybridization has been found to improve and extend the pharmacological properties of the parental compound. The present study describes the synthesis of novel furoxan coupled spiro-isoquinolino-piperidine derivatives and their smooth muscle relaxant activity. The study reveals that, particularly 10d (1.50 ± 0.6) and 10g (1.65 ± 0.7) are moderate PDE 5 inhibitors as compared to Sidenafil (1.43 ± 0.5). The observed effect was explained by molecular modelling studies on phosphodiesterase. |
| Databáze: | OpenAIRE |
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