Interaction of manganese(II) with the hybrid molecule (E)-4-(2-(pyridin-2-ylmethylene)hydrazinyl)quinazoline: Structure and biological profile

Polyhedron ◽  
2021 ◽  
Vol 195 ◽  
pp. 114986
Author(s):  
Chrisoula Kakoulidou ◽  
Antonios G. Hatzidimitriou ◽  
Konstantina C. Fylaktakidou ◽  
George Psomas
Keyword(s):  
Hybrid Molecule ◽  
Biological Profile

Synthesis and Biological Activity of Quaternary Quinolinium Salts: A Review

2020 ◽  
Vol 23 (21) ◽  
pp. 2271-2294 ◽  
Author(s):  
Divya Utreja ◽  
Shivali Sharma ◽  
Akhil Goyal ◽  
Komalpreet Kaur ◽  
Sonia Kaushal
Keyword(s):  
Tyrosine Kinases ◽  
Biological Activities ◽  
Polymeric Materials ◽  
Tubulin Polymerization ◽  
Quinoline Derivatives ◽  
Heterocyclic Chemistry ◽  
Biological Profile ◽  
Drug Candidates ◽  
Anti Hiv ◽  
Quinolinium Salts

Heterocyclic chemistry is the only branch of chemistry that has applications in varied areas such as dyes, photosensitizers, coordination compounds, polymeric materials, biological, and many other fields. Quinoline and its derivatives have always engrossed both synthetic chemists and biologists because of their diverse chemical and pharmacological properties as these ring systems can be easily found in various natural products, especially in alkaloids. Among alkaloids, quinoline derivatives i.e. quinolinium salts have attracted much attention nowadays owing to their diverse biological profile such as antimicrobial, antitumor, antifungal, hypotensive, anti-HIV, analgesics and anti-inflammatory, etc. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization, topoisomerase, and DNA repair. These observations have been guiding scientists for the expansion of new quinoline derivatives with improved and varied biological activities. Quinolinium salts have immense possibilities and scope to investigate these compounds as potential drug candidates. Therefore, we shall present a concise compilation of this work to aid in present knowledge and to help researchers explore an interesting quinoline class having medicinal potential.

Inorganic Gold and Polymeric Poly(Lactide-co-glycolide) Nanoparticles as Novel Strategies to Ameliorate the Biological Properties of Antimicrobial Peptides

2020 ◽  
Vol 21 (4) ◽  
pp. 429-438 ◽  
Author(s):  
Bruno Casciaro ◽  
Francesca Ghirga ◽  
Deborah Quaglio ◽  
Maria Luisa Mangoni
Keyword(s):  
Antimicrobial Peptides ◽  
Biological Properties ◽  
Biological Profile ◽  
Innovative Strategy ◽  
Different Types ◽  
New Antibiotics ◽  
Interesting Class ◽  
Alternative Antimicrobials ◽  
Nanoparticulate Systems ◽  
Infective Activity

Cationic antimicrobial peptides (AMPs) are an interesting class of gene-encoded molecules endowed with a broad-spectrum of anti-infective activity and immunomodulatory properties. They represent promising candidates for the development of new antibiotics, mainly due to their membraneperturbing mechanism of action that very rarely induces microbial resistance. However, bringing AMPs into the clinical field is hampered by some intrinsic limitations, encompassing low peptide bioavailability at the target site and high peptide susceptibility to proteolytic degradation. In this regard, nanotechnologies represent an innovative strategy to circumvent these issues. According to the literature, a large variety of nanoparticulate systems have been employed for drug-delivery, bioimaging, biosensors or nanoantibiotics. The possibility of conjugating different types of molecules, including AMPs, to these systems, allows the production of nanoformulations able to enhance the biological profile of the compound while reducing its cytotoxicity and prolonging its residence time. In this minireview, inorganic gold nanoparticles (NPs) and biodegradable polymeric NPs made of poly(lactide-coglycolide) are described with particular emphasis on examples of the conjugation of AMPs to them, to highlight the great potential of such nanoformulations as alternative antimicrobials.

Therapeutic Journey of 5-Pyrazolones as a Versatile Scaffold: A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Ravinder Sharma ◽  
Pooja A. Chawla ◽  
Viney Chawla ◽  
Rajeev Verma ◽  
Nandita Nawal ◽  
...  
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Protease Inhibitor ◽  
Medicinal Chemistry ◽  
Membered Ring ◽  
Present Review ◽  
Biological Profile ◽  
3C Protease ◽  
Structure Activity ◽  
Derivatives Of ◽  
Heterocyclic Moiety

Abstract: A sizeable proportion of currently marketed drugs come from heterocycles. The heterocyclic moiety 5-pyrazolone is well known five membered ring containing nitrogen. Derivatives of this wonder nucleus have exhibited activities as diverse as antimicrobial, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antidiabetic, antihyperlipidemic, antiviral, antitubercular, antioxidant, anticancer and antiviral including action against severe acute respiratory syndrome (SARS) or 3C protease inhibitor. A number of drugs based on this motif have already made it to the market. Standard texts and literature on medicinal chemistry cite different approaches for the synthesis of 5-pyrazolones. The present review provides an insight view to 5-pyrazolone synthesis, their biological profile and structure activity relationship studies.

scholarly journals FRI0052 INFLUENCE OF RHEUMATOID ARTHRITIS ON THE CLINICAL AND BIOLOGICAL PROFILE OF TYPE-2 DIABETES MELLITUS

2020 ◽  
Vol 79 (Suppl 1) ◽  
pp. 601.2-602
Author(s):  
J. Avouac ◽  
M. Elhai ◽  
M. Forien ◽  
J. Sellam ◽  
F. Eymard ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Insulin Resistance ◽  
Type 2 Diabetes ◽  
Insulin Requirement ◽  
Multivariate Logistic Regression ◽  
Biological Profile ◽  
Research Support ◽  
Insulin Resistant ◽  
Research Grant

Background:Type-2 diabetes and rheumatoid arthritis (RA) are two chronic diseases characterized by tissue inflammation and insulin resistance. To date, no data have evaluated the influence of RA-induced joint and systemic inflammation on the course of type-2 diabetes.Objectives:To study the impact of RA on type-2 diabetesMethods:Observational, multicenter, cross-sectional usual-care study, including 7 rheumatology centers. This study included over a 24-month period consecutive patients with type-2 diabetes and RA, fulfilling the 2010 ACR / EULAR criteria, and diabetic controls with osteoarthritis (OA). The following data were collected: demographics, disease activity and severity indices, current treatment for RA and diabetes, history and complications of diabetes. A systematic blood test was performed, assessing inflammatory (CRP levels) and metabolic (fasting glycemia and insulin levels, HbA1c) parameters. The HOMA2%B (insulin secretion) and HOMA2%S (tissue insulin sensitivity) indices (HOMA calculator, © Diabetes Trials Unit, University of Oxford) were used to assess insulin resistance. Ra and OA patients were compared using parametric tests after adjusting for age and BMI. A multivariate logistic regression was performed ti identify factors independently associated with insulin resistance.Results:We included 122 RA patients (74% women, mean age 64+/-11 years, mean disease duration 15+/-11 11 years, 75% with positive ACPA antibodies and 64% with erosive disease) and 54 controls with OA. 64% of RA patients were treated with oral corticosteroids <10 mg/day, 65% received methotrexate and 53% received targeted biological therapies.The characteristics of type-2 diabetes in the 54 OA patients corresponded to severe insulin-resistant diabetes: age> 65 years, high BMI> 30 kg/m2, mean HbA1c 7.3%+/-11 1.3%, 30% of insulin requirement, high frequency of other cardiovascular risk factors, macroangiopathy found in almost half of patients and biological criteria of insulin resistance (elevation of HOMA2%B and decrease of HOMA2%S).RA patients with type-2 diabetes had a younger age (64+/-11 years vs. 68+/-12 years, p=0.031) and lower BMI (27.7+/-11 5.5 vs. 31.5+/-11 6.3, p<0.001). These patients also had severe diabetes (HbA1c 7.0%+/-11 1.2%, 29% of insulin requirement, 43% of macroangiopathy) with an insulin resistance profile identical to OA controls. After adjusting for age and BMI, RA patients had a significantly increased insulin secretion compared to OA patients (HOMA2%B: 83.1+/-11 65.2 vs. 49.3+/-11 25.7, p=0.023) as well as a significant reduction of insulin sensitivity (HOMA2%S: 61.1+/-11 31.6 vs. 92.9+/-11 68.1, p=0.016). This insulin resistance was associated with the inflammatory activity of RA, with a negative correlation between the HOMA2%S and the DAS28 (r=-0.28, p=0.027). The multivariate logistic regression confirmed the independent association between the HOMA2%S index and DAS28 (OR: 3.93, 95% CI 1.02-15.06), as well as high blood pressure (OR: 1.29, 95% CI 0.33-1.99 CI).Conclusion:RA patients with type-2 diabetes displayed severe, poorly controlled diabetes, highlighting the burden of comorbidities associated with RA. The clinical-biological profile of diabetic RA patients was severe insulin-resistant diabetes, with a biological profile of insulin resistance linked to the inflammatory activity of the disease. These findings may have therapeutic implications, with the potential targeting of insulin resistance through the treatment of joint and systemic inflammation.Acknowledgments:Société Française de Rhumatologie (research grant)Bristol Myers Squibb (research grant)Disclosure of Interests:Jérôme Avouac Grant/research support from: Pfizer, Bristol Myers Squibb, Consultant of: Sanofi, Bristol Myers Squibb, Abbvie, Boerhinger, Nordic Pharma, Speakers bureau: Sanofi, Bristol Myers Squibb Abbvie, MSD, Pfizer, Nordic Pharma, Muriel ELHAI: None declared, Marine Forien: None declared, Jérémie SELLAM: None declared, Florent Eymard Consultant of: Regenlab, Anna Moltó Grant/research support from: Pfizer, UCB, Consultant of: Abbvie, BMS, MSD, Novartis, Pfizer, UCB, Laure Gossec Grant/research support from: Lilly, Mylan, Pfizer, Sandoz, Consultant of: AbbVie, Amgen, Biogen, Celgene, Janssen, Lilly, Novartis, Pfizer, Sandoz, Sanofi-Aventis, UCB, Frédéric Banal: None declared, Joel Daminano: None declared, Philippe Dieudé: None declared, Yannick Allanore Shareholder of: Sanofi, Roche, Consultant of: Actelion, Bayer, BMS, Boehringer Ingelheim, Inventiva, Sanofi

Trinuclear and tetranuclear iron(III) complexes with fenamates: Structure and biological profile

2021 ◽  
pp. 111410
Author(s):  
Filitsa Dimiza ◽  
Antonios G. Hatzidimitriou ◽  
Yiannis Sanakis ◽  
Athanasios N. Papadopoulos ◽  
George Psomas
Keyword(s):  
Biological Profile

scholarly journals Unicystic Mural Ameloblastoma: An Unusual Case Report

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
V. Nagalaxmi ◽  
Mithare Sangmesh ◽  
Kotya Naik Maloth ◽  
Srikanth Kodangal ◽  
Vani Chappidi ◽  
...  
Keyword(s):  
Unusual Case ◽  
Biological Profile ◽  
Unicystic Ameloblastoma ◽  
Tumor Group ◽  
Jaw Cyst ◽  
Dentigerous Cysts ◽  
Odontogenic Neoplasm ◽  
Cyst Cavity ◽  
Unusual Case Report

Ameloblastoma is a benign odontogenic neoplasm which frequently affects the mandible. The term ameloblastoma includes several clinicoradiological and histological types. Apart from the most commonly encountered clinicopathologic models, there are few variants, whose biological profile is unknown or not elicited. Among these types, unicystic ameloblastoma is the least encountered variant of the ameloblastoma. Unicystic ameloblastoma refers to those cystic lesions that show clinical, radiographic, or gross features of a jaw cyst but on histologic examination show a typical ameloblastomatous epithelium lining the cyst cavity, with or without luminal and/or mural tumor proliferation. Unicystic ameloblastoma is a less encountered variant of the ameloblastoma and is believed to be less aggressive. As this tumor shows considerable similarities with dentigerous cysts, both clinically and radiographically, the biologic behaviour of this tumor group was reviewed. Moreover, recurrence of unicystic ameloblastoma may be long delayed, and a long-term postoperative followup is essential for proper management of these patients. Here we are presenting a case of unicystic ameloblastoma in an 18-year-old female patient.

Vanillin-coumarin hybrid molecule as an efficient fluorescent probe for trace level determination of Hg(II) and its application in cell imaging

Talanta ◽  
2011 ◽  
Vol 85 (3) ◽  
pp. 1658-1664 ◽  
Author(s):  
Subarna Guha ◽  
Sisir Lohar ◽  
Ipsit Hauli ◽  
Subhra K. Mukhopadhyay ◽  
Debasis Das
Keyword(s):  
Fluorescent Probe ◽  
Cell Imaging ◽  
Hybrid Molecule ◽  
Trace Level ◽  
Trace Level Determination

Constructing a hybrid molecule with low capacity of IgE binding from Chenopodium album pollen allergens

2012 ◽  
Vol 144 (1-2) ◽  
pp. 67-77 ◽  
Author(s):  
Hamid Reza Nouri ◽  
Abdolreza Varasteh ◽  
Fatemeh Vahedi ◽  
Jamshidkhan Chamani ◽  
Danial Afsharzadeh ◽  
...  
Keyword(s):  
Chenopodium Album ◽  
Hybrid Molecule ◽  
Pollen Allergens ◽  
Ige Binding
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