The structure-activity relationship of papaverine analogs, the inhibitors of adenosine cyclic 3', 5'-monophosphate (c-AMP) phosphodiesterase, is discussed. The enzyme inhibition activity of these compounds are found to be dominantly controlled by hydrophobicity and steric factors. A significant quantitative correlation has been obtained between the inhibition activity and the van der Waals volume.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Bioactive Sulfonamides Derived from Amino Acids: Their Synthesis and Pharmacological Activities.
Mini Rev Med Chem
January 2025
Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.
Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.
View Article and Find Full Text PDFDiscovery of Triketone-Indazolones as Novel 4-Hydroxyphenylpyruvate Dioxygenase Inhibiting-Based Herbicides.
J Agric Food Chem
January 2025
State Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, Central China Normal University, Wuhan 430079, PR China.
4-Hydroxyphenylpyruvate dioxygenase (HPPD) is a crucial herbicide target in current research, playing an important role in the comprehensive management of resistant weeds. However, the limited crop selectivity and less effectiveness against grass weeds of many existing HPPD inhibitors, limit their further application. To address these issues, a series of novel HPPD inhibitors with fused ring structures were designed and synthesized by introducing an electron-rich indazolone ring and combining it with the classical triketone pharmacophore structure.
View Article and Find Full Text PDFReview on antibacterial flavonoids from genus : Structure-activity relationship and mode of action.
Heliyon
January 2025
Department of Chemical Sciences, Faculty of Science and Technology, Universiti Kebangsaan Malaysia (UKM), 46300, Bangi, Selangor, Malaysia.
The Fabaceae family, particularly genus , is renowned for significant medicinal properties. These plants have been used as natural remedies to address various health issues and are rich in flavonoids. Therefore, this review aimed to provide a comprehensive overview of antibacterial activity, structure-activity relationship, especially against drug-resistance and mode of action for flavonoids isolated from .
View Article and Find Full Text PDFN-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents.
ACS Med Chem Lett
January 2025
Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Malaviya National Institute of Technology, Jawaharlal Nehru Marg, Jaipur 302017, India.
A series of novel N-arylsulfonylated C-homoaporphine alkaloids were synthesized under microwave irradiation and evaluated for their antiplatelet and antimicrobial activities. Among the series, compounds , , , , , , , , and demonstrated highly potent (∼3-fold) platelet aggregation inhibitory activity than acetylsalicylic acid (IC = 21.34 μg/mL).
View Article and Find Full Text PDFOptimizing Linezolid: Transforming It into a Selective MAO-B Inhibitor via a Toxicity-to-Activity Optimization Approach.
ACS Med Chem Lett
January 2025
Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra 425405, India.
Linezolid, a widely used oxazolidinone antibiotic, exhibits potent activity against resistant bacterial infections but is associated with serotonergic toxicity, primarily due to its inhibition of monoamine oxidase (MAO). MAOs, consisting of MAO-A and MAO-B isoforms, play crucial roles in neurotransmitter metabolism, with implications for neurodegenerative disorders like Parkinson's and Alzheimer's diseases. This study aims to optimize Linezolid's structure to transform it into a selective MAO-B inhibitor.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!