Recent Advances in Plasmepsin Medicinal Chemistry and Implications for Future Antimalarial Drug Discovery Efforts

2012 ◽  
Vol 12 (5) ◽  
pp. 445-455 ◽  
Author(s):  
Marvin J. Meyers ◽  
Daniel E. Goldberg
Keyword(s):  
Drug Discovery ◽  
Antimalarial Drug ◽  
Medicinal Chemistry ◽  
Recent Advances

Advances in antibiotic drug discovery: reducing the barriers for antibiotic development

2020 ◽  
Vol 12 (22) ◽  
pp. 2067-2087
Author(s):  
Kyle E Murphy ◽  
Grace F Sloan ◽  
Grace V Lawhern ◽  
Grace E Volk ◽  
Jacob T Shumate ◽  
...  
Keyword(s):  
Public Health ◽  
Multidrug Resistance ◽  
Drug Discovery ◽  
Natural Product ◽  
Medicinal Chemistry ◽  
Health Crisis ◽  
Antibiotic Development ◽  
Public Health Crisis ◽  
Recent Advances ◽  
Antibiotic Drug

Antibiotic drug discovery has been an essential field of research since the early 1900s, but the threat from infectious bacteria has only increased over the decades because of the emergence of widespread multidrug resistance. In this review, we discuss the recent advances in natural product, computational and medicinal chemistry that have reinvigorated the field of antibiotic drug discovery while giving perspective on how easily, both in cost and in expertise, these methods can be implemented by other researchers with the goal of increasing the number of scientists contributing to this public health crisis.

scholarly journals Recent advances in synthetic approaches for medicinal chemistry of C-nucleosides

2018 ◽  
Vol 14 ◽  
pp. 772-785 ◽  
Author(s):  
Kartik Temburnikar ◽  
Katherine L Seley-Radtke
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Nucleophilic Substitution ◽  
Medicinal Chemistry ◽  
Structural Diversity ◽  
Synthetic Analogues ◽  
Structural Modifications ◽  
Modular Synthesis ◽  
Recent Advances ◽  
Synthetic Approaches

C-nucleosides have intrigued biologists and medicinal chemists since their discovery in 1950's. In that regard, C-nucleosides and their synthetic analogues have resulted in promising leads in drug design. Concurrently, advances in chemical syntheses have contributed to structural diversity and drug discovery efforts. Convergent and modular approaches to synthesis have garnered much attention in this regard. Among them nucleophilic substitution at C1' has seen wide applications providing flexibility in synthesis, good yields, the ability to maneuver stereochemistry as well as to incorporate structural modifications. In this review, we describe recent reports on the modular synthesis of C-nucleosides with a focus on D-ribonolactone and sugar modifications that have resulted in potent lead molecules.

scholarly journals Antimalarial drug discovery targeting apical membrane antigen 1

MedChemComm ◽  
2017 ◽  
Vol 8 (1) ◽  
pp. 13-20 ◽  
Author(s):  
Shane M. Devine ◽  
Christopher A. MacRaild ◽  
Raymond S. Norton ◽  
Peter J. Scammells
Keyword(s):  
Drug Discovery ◽  
Antimalarial Drug ◽  
Malaria Parasite ◽  
Apical Membrane ◽  
Host Cells ◽  
Apical Membrane Antigen 1 ◽  
Essential Protein ◽  
Apical Membrane Antigen ◽  
Recent Advances

This review encompasses recent advances in drug discovery targeting apical membrane antigen 1, an essential protein involved in the invasion of host cells by the malaria parasite.

scholarly journals A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery

2020 ◽  
Vol 195 ◽  
pp. 112275 ◽  
Author(s):  
Thanigaimalai Pillaiyar ◽  
Sangeetha Meenakshisundaram ◽  
Manoj Manickam ◽  
Murugesan Sankaranarayanan
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Drug Repositioning ◽  
Recent Advances

scholarly journals Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization

Organics ◽  
2021 ◽  
Vol 2 (4) ◽  
pp. 337-347
Author(s):  
Carolina Durand ◽  
Michal Szostak
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Structural Diversity ◽  
Synthetic Methods ◽  
Nitrogen Heterocycle ◽  
Piperazine Ring ◽  
The Third ◽  
Recent Advances ◽  
Made In

Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diversity of piperazines is limited, with about 80% of piperazine-containing drugs containing substituents only at the nitrogen positions. Recently, major advances have been made in the C–H functionalization of the carbon atoms of the piperazine ring. Herein, we present an overview of the recent synthetic methods to afford functionalized piperazines with a focus on C–H functionalization.

Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present)

2020 ◽  
Vol 63 (9) ◽  
pp. 4445-4467 ◽  
Author(s):  
Peter Mubanga Cheuka ◽  
Godwin Dziwornu ◽  
John Okombo ◽  
Kelly Chibale
Keyword(s):  
Drug Discovery ◽  
Antimalarial Drug ◽  
Medicinal Chemistry ◽  
Target Validation

Sitagliptin: a potential drug for the treatment of SARS-CoV-2?

2020 ◽  
Author(s):  
Sanaa Bardaweel
Keyword(s):  
Clinical Trials ◽  
Drug Discovery ◽  
Antimalarial Drug ◽  
Drug Repurposing ◽  
Spike Protein ◽  
Diabetic Patients ◽  
Potential Drug ◽  
Chemokine Production ◽  
Drug Discovery And Development ◽  
Sequence Identity

Recently, an outbreak of fatal coronavirus, SARS-CoV-2, has emerged from China and is rapidly spreading worldwide. As the coronavirus pandemic rages, drug discovery and development become even more challenging. Drug repurposing of the antimalarial drug chloroquine and its hydroxylated form had demonstrated apparent effectiveness in the treatment of COVID-19 associated pneumonia in clinical trials. SARS-CoV-2 spike protein shares 31.9% sequence identity with the spike protein presents in the Middle East Respiratory Syndrome Corona Virus (MERS-CoV), which infects cells through the interaction of its spike protein with the DPP4 receptor found on macrophages. Sitagliptin, a DPP4 inhibitor, that is known for its antidiabetic, immunoregulatory, anti-inflammatory, and beneficial cardiometabolic effects has been shown to reverse macrophage responses in MERS-CoV infection and reduce CXCL10 chemokine production in AIDS patients. We suggest that Sitagliptin may be beneficial alternative for the treatment of COVID-19 disease especially in diabetic patients and patients with preexisting cardiovascular conditions who are already at higher risk of COVID-19 infection.

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