scholarly journals Benzophenone: a ubiquitous scaffold in medicinal chemistry

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1803-1817 ◽  
Author(s):  
Khemchand Surana ◽  
Bharatkumar Chaudhary ◽  
Monika Diwaker ◽  
Satyasheel Sharma
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Bioactive Compounds ◽  
Medicinal Chemistry ◽  
Naturally Occurring

Diaryl ketones are an important scaffold in drug discovery due to their prevalence in naturally occurring bioactive compounds. This review discusses molecules containing the benzophenone moiety that have potent biological activity.

Chemical and Functional Diversity of Natural Products from Plant Associated Endophytic Fungi

2009 ◽  
Vol 4 (11) ◽  
pp. 1934578X0900401 ◽  
Author(s):  
Vijay C. Verma ◽  
Ravindra N. Kharwar ◽  
Gary A. Strobel
Keyword(s):  
Natural Products ◽  
Biological Activity ◽  
Functional Diversity ◽  
Bioactive Compounds ◽  
Endophytic Fungi ◽  
Host Plants ◽  
Fungal Endophytes ◽  
Sources Identification ◽  
Naturally Occurring

This review describes examples of naturally occurring bioactive compounds obtained from fungal endophytes from various host plants. The main topics addressed are sources, identification, biological activity, biosynthesis, and ecological and chemosystematic significance of those bioactive compounds whose sources were well defined.

scholarly journals Steroids in Medicinal Chemistry: Literature Review

2021 ◽  
pp. 69-78
Author(s):  
Samy M. Ibrahim ◽  
Esraa H. Elshafiey ◽  
Esraa K. Al batreek ◽  
Esraa R. Abdulrahim ◽  
Esraa R. Azazy ◽  
...  
Keyword(s):  
Biological Activity ◽  
Literature Review ◽  
Organic Compounds ◽  
Medicinal Chemistry ◽  
Clinical Implications ◽  
Biological Functions ◽  
Naturally Occurring

Background: Steroids are naturally occurring organic compounds with a great variety of different biological functions. They are subdivided into progesterone, mineralocorticoids, glucocorticoids, androgens, and estrogens, depending on their function. Aim: In this literature review, we are introducing the most updated information about steroids in terms of their history, functions, types either according to their occurrence or biological activity, different pathways of synthesis, and uses. Methods: reported methods are mentioned in detail. Results and Discussion: Steroids are the mainstay of therapy for a variety of disorders and knowledge of the clinical implications of steroids is critical.

scholarly journals More Than Resveratrol: New Insights into Stilbene-Based Compounds

Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1111
Author(s):  
Paulina Pecyna ◽  
Joanna Wargula ◽  
Marek Murias ◽  
Malgorzata Kucinska
Keyword(s):  
Biological Activity ◽  
Drug Development ◽  
Medicinal Chemistry ◽  
Molecular Level ◽  
Molecular Targets ◽  
Disease Pathogenesis ◽  
Development Path ◽  
Naturally Occurring ◽  
Starting Point ◽  
Sophisticated Equipment

The concept of a scaffold concerns many aspects at different steps on the drug development path. In medicinal chemistry, the choice of relevant “drug-likeness” scaffold is a starting point for the design of the structure dedicated to specific molecular targets. For many years, the chemical uniqueness of the stilbene structure has inspired scientists from different fields such as chemistry, biology, pharmacy, and medicine. In this review, we present the outstanding potential of the stilbene-based derivatives. Naturally occurring stilbenes, together with powerful synthetic chemistry possibilities, may offer an excellent approach for discovering new structures and identifying their therapeutic targets. With the development of scientific tools, sophisticated equipment, and a better understanding of the disease pathogenesis at the molecular level, the stilbene scaffold has moved innovation in science. This paper mainly focuses on the stilbene-based compounds beyond resveratrol, which are particularly attractive due to their biological activity. Given the “fresh outlook” about different stilbene-based compounds starting from stilbenoids with particular regard to isorhapontigenin and methoxy- and hydroxyl- analogues, the update about the combretastatins, and the very often overlooked and underestimated benzanilide analogues, we present a new story about this remarkable structure.

The Quinazoline-Chalcone and Quinazolinone-Chalcone Hybrids: A Promising Combination for Biological Activity.

2020 ◽  
Vol 20 ◽  
Author(s):  
Eduardo Bustos Mass ◽  
Gilmar Vieira Duarte ◽  
Dennis Russowsky
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Pharmaceutical Research ◽  
Antimicrobial Activities ◽  
Molecular Hybridization ◽  
Hybrid Compounds ◽  
Synthetic Methodologies ◽  
Number Of Publications

: Quinazoline and/or chalcones derivatives are important targets in several areas of chemical sciences, mainly, in the medicinal chemistry and pharmaceutical research. The purpose of this review is to systematize the information available in the literature, including patents, regarding the benefits exerted by the combination of these two pharmacophores into single molecules. These hybrid compounds can exhibit different biological activities, causing a synergistic or a new effect, compared to the individuals. The variability of biological activities includes anticancer, anti-Alzheimer, antiviral and antimicrobial activities, among others. Additionally, synthetic methodologies to prepare the different molecular architectures were discussed based on their similarities. The increasing number of publications indicates the importance of molecular hybridization on the field of drug discovery.

Fungal Bioactive Compounds in Pharmaceutical Research and Development

2019 ◽  
Vol 15 (2) ◽  
pp. 211-231 ◽  
Author(s):  
Sanjai Saxena ◽  
Manmohan Chhibber ◽  
Inder Pal Singh
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Drug Development ◽  
Natural Product ◽  
Bioactive Compounds ◽  
Medicinal Chemistry ◽  
Bioactive Compound ◽  
New Drugs ◽  
Ecological Groups ◽  
Pharmaceutical Industries

Background:Exploration of antibiotics from microorganisms became widespread in the academia and the industry with the serendipitous discovery of Penicillin from Penicillium notatum by Sir Alexander Fleming. This embarked the golden era of antibiotics which lasted for over 60 years. However, the traditional phenotypic screening was replaced with more rational and smarter methods of exploration of bioactive compounds from fungi and microorganisms. Fungi have been responsible for providing a variety of bioactive compounds with diverse activities which have been developed into blockbuster drugs such as Cyclosporine, Caspofungin, Lovastatin and Fingolimod etc. It has been reported that ca. 40% of the 1453 New Chemical Entities (NCE’s) approved by USFDA are natural products, natural product inspired or mimics many of which have their origins from fungi. Hence fungal compounds are playing a very important role in drug discovery and development in the pharmaceutical industry.Methods:We undertook structured searches of bibliographic databases of peer-reviewed research literature which pertained to natural products, medicinal chemistry of natural products and drug discovery from fungi. With the strategic improvement in screening and identification methods, fungi are still a potential resource for novel chemistries. Thus the searches also comprised of bioactive agents from fungi isolated or derived from special ecological groups and lineages. To find different molecules derived or isolated from fungi under clinical studies, clinical trial data from the NIH as well as from pharmaceutical companies were also explored. This comprised of data wherein the pharmaceutical industries have acquired or licensed a fungal bioactive compound for clinical study or a trial.Results:Natural product chemistry and medicinal chemistry continue to play an important role in converting a bioactive compound into therapeutic moieties or pharmacophores for new drug development.Conclusion:Thus one can say fungal bioactive compounds are alive and well for development into new drugs as novel ecological groups of fungi as well as novel chemistries are being uncovered. This review further emphasizes the collaboration of fungal biologists with chemists, pharmacologists and biochemists towards the development of newer drugs for taking them into the drug development pipeline.

scholarly journals Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry

RSC Advances ◽  
2020 ◽  
Vol 10 (24) ◽  
pp. 14170-14197 ◽  
Author(s):  
Maged Henary ◽  
Carl Kananda ◽  
Laura Rotolo ◽  
Brian Savino ◽  
Eric A. Owens ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Medicinal Chemistry ◽  
Research Interest ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Naturally Occurring

Nitrogen containing heterocycles are of immense research interest because they are often found as naturally occurring bioactive compounds.

A Revised Modular Approach to D8-THC and Derivatives Through Late-Stage Suzuki-Miyaura Cross-Coupling Reactions

2019 ◽  
Author(s):  
Victor Bloemendal ◽  
Floris P. J. T. Rutjes ◽  
Thomas J. Boltje ◽  
Daan Sondag ◽  
Hidde Elferink ◽  
...  
Keyword(s):  
Biological Activity ◽  
Late Stage ◽  
Medicinal Chemistry ◽  
Cross Coupling ◽  
Modular Approach ◽  
Coupling Reactions ◽  
One Pot ◽  
Biologically Relevant ◽  
Cross Coupling Reactions ◽  
Chemistry Research

<p>In this manuscript we describe a modular pathway to synthesize biologically relevant (–)-<i>trans</i>-Δ<sup>8</sup>-THC derivatives, which can be used to modulate the pharmacologically important CB<sub>1</sub> and CB<sub>2</sub> receptors. This pathway involves a one-pot Friedel-Crafts alkylation/cyclization protocol, followed by Suzuki-Miyaura cross-coupling reactions and gives rise to a series of new Δ<sup>8</sup>-THC derivatives. In addition, we demonstrate using extensive NMR evidence that similar halide-substituted Friedel-Crafts alkylation/cyclization products in previous articles were wrongly assigned as the para-isomers, which also has consequence for the assignment of the subsequent cross-coupled products and interpretation of their biological activity. </p> <p>Considering the importance of the availability of THC derivatives in medicinal chemistry research and the fact that previously synthesized compounds were wrongly assigned, we feel this research is describing a straightforward pathway into new cannabinoids.</p>

Naphthoquinone Derivatives Isolated from Plants: Recent Advances in Biological Activity

2020 ◽  
Vol 20 (19) ◽  
pp. 2019-2035
Author(s):  
Esmaeil Sheikh Ahmadi ◽  
Amir Tajbakhsh ◽  
Milad Iranshahy ◽  
Javad Asili ◽  
Nadine Kretschmer ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Biological Activity ◽  
Small Molecules ◽  
Anticancer Activity ◽  
Clinical Significance ◽  
Phase Ii ◽  
Biological Activities ◽  
Phase Ii Clinical Trials ◽  
Naturally Occurring ◽  
The Subject

Naturally occurring naphthoquinones (NQs) comprising highly reactive small molecules are the subject of increasing attention due to their promising biological activities such as antioxidant, antimicrobial, apoptosis-inducing activities, and especially anticancer activity. Lapachol, lapachone, and napabucasin belong to the NQs and are in phase II clinical trials for the treatment of many cancers. This review aims to provide a comprehensive and updated overview on the biological activities of several new NQs isolated from different species of plants reported from January 2013 to January 2020, their potential therapeutic applications and their clinical significance.

Synthesis and Biological Activity of Embelin and its Derivatives: An Overview

2020 ◽  
Vol 20 (5) ◽  
pp. 396-407 ◽  
Author(s):  
Zhaojun Sheng ◽  
Siyuan Ge ◽  
Min Gao ◽  
Rongchao Jian ◽  
Xiaole Chen ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Effects ◽  
New Drugs ◽  
Hydroxyl Groups ◽  
Carbonyl Groups ◽  
Cellular Mechanisms ◽  
Embelia Ribes ◽  
Naturally Occurring ◽  
Ic50 Value ◽  
Apoptosis Protein

Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.) of the Myrsinaceae family, and contains two carbonyl groups, a methine group and two hydroxyl groups. With embelin as the lead compound, more than one hundred derivatives have been reported. Embelin is well known for its ability to antagonize the X-linked inhibitor of apoptosis protein (XIAP) with an IC50 value of 4.1 μM. The potential of embelin and its derivatives in the treatment of various cancers has been extensively studied. In addition, these compounds display a variety of other biological effects: antimicrobial, antioxidant, analgesic, anti-inflammatory, anxiolytic and antifertility activity. This paper reviews the recent progress in the synthesis and biological activity of embelin and its derivatives. Their cellular mechanisms of action and prospects in the research and development of new drugs are also discussed.

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