scholarly journals Natural products as inspiration for the development of bacterial antibiofilm agents

2020 ◽  
Vol 37 (11) ◽  
pp. 1454-1477 ◽  
Author(s):  
Roberta J. Melander ◽  
Akash K. Basak ◽  
Christian Melander
Keyword(s):  
Natural Products ◽  
Medicinal Chemistry ◽  
Antibiofilm Agents ◽  
Derivatives Of ◽  
Structure Confirmation

Synthetic and medicinal chemistry are important tools in the development of more potent, more accessible, or more pharmacologically favorable derivatives of anti-biofilm natural products, in addition to facilitating structure confirmation and understanding of mechanistic pathways.

Amino-derivatives of the sesquiterpene lactone class of natural products as prodrugs

MedChemComm ◽  
2013 ◽  
Vol 4 (1) ◽  
pp. 27-33 ◽  
Author(s):  
James R. Woods ◽  
Huaping Mo ◽  
Andrew A. Bieberich ◽  
Tanja Alavanja ◽  
David A. Colby
Keyword(s):  
Natural Products ◽  
Sesquiterpene Lactone ◽  
Medicinal Chemistry ◽  
Sesquiterpene Lactones ◽  
Clinical Translation ◽  
Amino Derivatives ◽  
Derivatives Of

The medicinal chemistry of amino-derivatives of the sesquiterpene lactones is described, beginning with synthetic development, moving into pharmacological applications, and finishing with clinical translation.

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

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.

Recent Advances on Small Molecule Medicinal Chemistry to Treat Human Diseases-Part III

2021 ◽  
Vol 21 (17) ◽  
pp. 1517-1518
Author(s):  
Dharmendra Kumar Yadav
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Small Molecule ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Review Article ◽  
Human Diseases ◽  
Bioactive Metabolite ◽  
Metabolite Production ◽  
Life Threatening

The discovery and utilization of novel metabolites from natural sources are gaining momentum in the present era. The drug discovery programs have witnessed a remarkable shift from conventional medicines to exploiting natural products and their “value addition”, for treating lifethreatening diseases. The global outbreak of life-threatening diseases namely Ebola, SARS,including infections of the bloodstream (bacteremia), heart valves (endocarditis), lungs (pneumonia), and brain (meningitis) and AIDS calls for a more targeted approach to effectively combat the emerging diseases. In the present scenario, natural products and their extracts are being explored extensively for the treatment of various life threatening diseases. In this thematic issue, several review articles contributed by the scientist and researchers in the different areas of medicinal chemistry, synthetic chemistry, new emerging multi-drug targets were collected. This issue begins with a review article on the “Chemistry and Pharmacology of Natural Catechins from Camellia sinensis as anti-MRSA agents” by Gaur et al. and focuses on the spread of MRSA strains is of great concern because of limited treatment options for staphylococcal infections, since these strains are resistant to the entire class of β-lactam antibiotics. In addition, MRSA exhibits resistance to other classes of antimicrobial agents such as fluoroquinolones, cephalosporins, aminoglycosides, macrolide and even glycopeptides (vancomycin and teicoplanine), leading to the emergence of resistant strains such as glycopeptide intermediate (GISA) and resistant strain (GRSA) of S. aureus. In this review, chemical constituents responsible for the anti-MRSA activity of tea are explored [1]. The next article of this issue is a review article on the “Recent Advancements in the Synthesis and Chemistry of Benzofused Nitrogen- and Oxygen-based Bioactive Heterocycles” by Sharma et al. which focuses on medicinal importance of these bioactive benzo-fused heterocycles; special attention has been given to their synthesis as well as medicinal/pharmaceutical properties in detail [2]. “Trends in pharmaceutical design of Endophytes as anti-infective,” by Tiwari et al., is the third article in this issue. The review focused on the meta-analysis of bioactive metabolite production from endophytes, extensively discussing the bioprospection of natural products for pharmaceutical applications. In light of the emerging importance of endophytes as antiinfective agents, an exploration of the pharmaceutical design of novel chemical entities and analogues has enabled efficient and cost-effective drug discovery programs. However, bottlenecks in endophytic biology and research requires a better understanding of endophytic dynamics and mechanism of bioactive metabolite production towards a sustainable drug discovery program [3]. The last article of this issue is also research article on “Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents” by Yadav et al. The article reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity an target involved and structural features responsible for the better activity, so the reader can directly find detail for designing new anticancer agents. [4]. Finally I would like to thank all authors who contributed to this issue, titled “Recent advances on small molecule medicinal chemistry to treat human diseases”.

Semisynthetic triazoles as an approach in the discovery of Novel Lead Compounds

2021 ◽  
Vol 25 ◽  
Author(s):  
Pedro Alves Bezerra Morais ◽  
Carla Santana Francisco ◽  
Heberth de Paula ◽  
Rayssa Ribeiro ◽  
Mariana Alves Eloy ◽  
...  
Keyword(s):  
Natural Products ◽  
Medicinal Chemistry ◽  
Chemical Space ◽  
Biological Activities ◽  
Post Translational Modification ◽  
Cellular Processes ◽  
Modern Drug ◽  
New Chemical Entities ◽  
Almost All ◽  
The 19Th Century

: Historically, the medicinal chemistry is concerned with the approach of organic chemistry to new drug synthesis. Considering the fruitful collections of new molecular entities, the dedicated efforts for medicinal chemistry are rewarding. Planning and search of new and applicable pharmacologic therapies involve the altruistic nature of the scientists. Since the 19th century, notoriously the application of isolated and characterized plant-derived compounds in modern drug discovery and in various stages of clinical development highlight its viability and significance. Natural products influence a broad range of biological processes, covering transcription, translation, and post-translational modification and being effective modulators of almost all basic cellular processes. The research of new chemical entities through “click chemistry” continuously opens up a map for the remarkable exploration of chemical space in towards leading natural products optimization by structure-activity relationship. Finally, here in this review, we expect to gather a broad knowledge involving triazolic natural products derivatives, synthetic routes, structures, and their biological activities.

Construction of N-heterocycles via Pd-mediated C–H activation/annulation strategies

2022 ◽  
Author(s):  
Mengyu Qiu ◽  
Xuegang Fu ◽  
Peng Fu ◽  
Jianhui Huang
Keyword(s):  
Natural Products ◽  
Organic Synthesis ◽  
Material Science ◽  
Medicinal Chemistry ◽  
Drug Molecules

N-heterocycles can be found in natural products and drug molecules, which are indispensable components in the area of organic synthesis, medicinal chemistry and material science. The construction of these N-containing...

Novel and less explored chemotypes of natural origin for the inhibition of Hsp90

MedChemComm ◽  
2016 ◽  
Vol 7 (11) ◽  
pp. 2063-2075 ◽  
Author(s):  
Federica Pellati ◽  
Giulio Rastelli
Keyword(s):  
Natural Products ◽  
Medicinal Chemistry ◽  
Natural Origin ◽  
Hsp90 Function

This review focuses on novel classes of natural products whose structures have not yet been thoroughly explored for medicinal chemistry purposes. These novel chemotypes may be useful starting points to develop compounds that alter Hsp90 functionvianovel mechanisms.

scholarly journals Natural Products in Medicinal Chemistry

2009 ◽  
Vol 17 (6) ◽  
pp. 2120 ◽  
Author(s):  
David Newman ◽  
Gordon Cragg
Keyword(s):  
Natural Products ◽  
Medicinal Chemistry
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