Book Volume 10
Preface
Page: ii-ii (1)
Author: Ashok Kumar Jha and Ravi S. Singh
DOI: 10.2174/9789815165043123100002
Isoxazole Derivatives as Potential Pharmacophore for New Drug Development
Page: 1-49 (49)
Author: Biswa Mohan Sahoo*, Bera Venkata Varaha Ravi Kumar, Krishna Chandra Panda, Bimal Krishna Banik*, Abhishek Tiwari, Varsha Tiwari, Sunil Singh and Manish Kumar
DOI: 10.2174/9789815165043123100004
PDF Price: $15
Abstract
Isoxazoles are five-membered aromatic heterocyclic compounds in which
oxygen and nitrogen atoms are present at positions 1 and 2 of the ring system.
Isoxazole derivatives play a vital role due to their diverse biological activities, such as
antimicrobial, antifungal, anti-viral, anti-tubercular, anti-epileptic, anti-diabetic,
anticancer, anthelmintic, antioxidant, antipsychotic, antimalarial, analgesic, anti-inflammatory, etc. Isoxazole scaffold is present in various drug molecules, such as
leflunomide (antirheumatic), valdecoxib (non-steroidal anti-inflammatory drug), and
zonisamide (anti-convulsant). Similarly, isoxazole derivatives such as isocarboxazid
act as monoamine oxidase inhibitors. It is used to treat symptoms of depression that
may include anxiety, panic, or phobias. Whereas the isoxazole derivatives, including
sulfamethoxazole, sulfisoxazole, and oxacillin, are used clinically for the treatment of
bacterial infections. Isoxazole pharmacophore is also present in β-lactamase resistant
antibiotics such as cloxacillin, dicloxacillin, and flucloxacillin. Cycloserine is a
naturally occurring antibiotic that possesses isoxazole moiety with anti-tubercular,
activity. This study focuses on the therapeutic potentials of isoxazole derivatives in
new drug development.
Contemporary Trends in Drug Repurposing: Identifying New Targets for Existing Drugs
Page: 50-80 (31)
Author: Srikant Bhagat*, ,Asim Kumar and Gaurav Joshi
DOI: 10.2174/9789815165043123100005
PDF Price: $15
Abstract
Drug repurposing or drug repositioning has emerged as an efficient, very
popular and alternative technique in modern drug discovery to identify old drugs for
new targets cost-effectively and dynamically. This concept gets a tremendous boost,
especially in the century's most challenging healthcare concern of the Covid-19
pandemic across the globe. In this approach, scientists seek new indications and
clinical use of the drugs at minimum risk, which have previously already been
pharmacologically established and approved. The methods developed for drug
repositioning include computational approaches and biological methodologies, and
with the fast technological advancement, various new drug-target- diseases are
discovered, and thereby immense information is now available in the different
databases, such as DrugBank, OMIM, ChemBank, KEGG, Pubmed, Genecard, and
many more. The information available on all the above public domain databases has
been utilized successfully in many drug repositioning projects. The present chapter
discusses the concept of drug repurposing and its impact on academia, industries and,
of course, their social implications. Besides this, the chapter will also cover details on
tools and techniques to identify drugs for repositioning and their application in
identifying drugs for various diseases and disorders. The current work will also foresee
the recent market analysis and updates on the cost of drug discovery and development
by drug repurposing, its comparison with traditional drug discovery approaches,
challenges involved with drug repurposing, and future perspectives.
Pharmaceutical Potential of Pyrimidines as Antiviral Agents
Page: 81-147 (67)
Author: Dina Nath Singh* and Nisha Verma
DOI: 10.2174/9789815165043123100006
PDF Price: $15
Abstract
Antiviral drugs are a class of medicines particularly used for the treatment of
viral infections. Drugs that combat viral infections are called antiviral drugs. Viruses
are among the major pathogenic agents that cause a number of serious diseases in
humans, animals and plants. Viruses cause many diseases in humans, from self-resolving diseases to acute fatal diseases. The strategies for the development of
antiviral drugs are generally focused on two different approaches, i.e., targeting the
viruses themselves or the host cell factors. Antiviral drugs that directly target viruses
include the inhibitors of virus attachment, inhibitors of virus entry, uncoating
inhibitors, polymerase inhibitors, protease inhibitors, nucleotide reverse transcriptase,
inhibitors of nucleoside and the inhibitors of integrase. The inhibitors of protease
(ritonavir, atazanavir and darunavir), viral DNA polymerase (acyclovir, tenofovir,
valganciclovir and valacyclovir) and integrase (raltegravir) are listed among the top
200 drugs by sales during the2010. Still, there are no effective antiviral drugs available
for many viral infections. There is a couple of drugs for herpes viruses, many for
influenza and some new antiviral drugs for treating hepatitis C infection and HIV. This
chapter gives an overview of the pyrimidines and hetero annulated pyrimidines that
have been reported to be active against viral infections; identification of novel
pyrimidine leads may be used in the designing of new potent, selective and less toxic
novel therapeutic agents having promising antiviral activity. An effort has been made
to compile all the possible information regarding antiviral pyrimidines and bring them
together to make easy availability of the existing literature on the subject. The objective
of this chapter is to provide the structural and antiviral activity information as well as
methods being used for the screening of the antiviral activity and antiviral potential
IC50/ED50/CC50 values of the reported active pyrimidines are briefly discussed.
Drugs and Phytochemicals Targeting Cancer
Page: 148-178 (31)
Author: Garima Tripathi, Anil Kumar Singh* and Abhijeet Kumar*
DOI: 10.2174/9789815165043123100007
PDF Price: $15
Abstract
Cancer which is basically uncontrolled cell division and, thereby, the
formation of tumors, has been a prominent cause of death across the world. More than
10 million people have lost their lives due to different types of cancer such as breast,
lung, prostate, gastrointestinal, etc. Several pathways, including metabolic, signalling,
etc., get altered to support uncontrolled cell division and their growth in case of cancer.
Despite an increasing understanding of this disease over the period of time, still,
specific causes could not be held responsible for the occurrence. Therefore, various
different strategies mainly focused on preventing and killing cancerous cells have been
explored. This chapter will primarily focus on the different drugs, including different
types of chemotherapeutic agents such as DNA-alkylating agents like nitrogen mustard,
cyclophosphamide, drug-peptide, drug-steroid conjugates, antimetabolites, antibiotics,
etc. In addition to that, phytochemicals, which have also been investigated for their
anti-cancerous activities and are under clinical trial, have also been discussed.
Harnessing the Neurological Properties of Indian Brain Health Booster Brahmi
Page: 179-204 (26)
Author: Neerja Tiwari, Manju Singh, Namita Gupta, Kishan Singh and Kapil Dev*
DOI: 10.2174/9789815165043123100008
PDF Price: $15
Abstract
Brahmi (Bacopa monnieri Linn.) is a well-known therapeutic herb used in a
broad spectrum of conventional medicines to alleviate various ailments, prominently
those involving intellect, anxiety and mental health. In Ayurveda, it is classified as
Medhya rasayanas (meaning intellect rejuvenator) and claimed to be a cognitive
nutrient and memory enhancer. Although the plant possesses a plethora of compounds,
its neurological activity is mainly attributed to its major phytochemical constituents,
i.e., bacoside saponins. Majorly isolated compounds are dammarane triterpenoids
glycone and aglycones. There are several reports published with neurological activities
on Bacopa monnieri to validate traditional claims through scientific findings. Some
therapeutic formulations containing standardized extracts of Bacopa monnieri have
also been developed for the betterment of mental health. Besides, being
neuroprotective, the plant is reported to possess anti-inflammatory, analgesic, and
antipyretic properties and systemic disorders like cardiovascular, hepatic,
gastrointestinal, myocardial ischemia, respiratory problems, opioid-related
nephrotoxicity and hepatotoxicity. The present chapter described the phytochemical
profiling, extraction and isolation, neurological properties, as well as toxicological and
clinical studies of the plant.
Carcinogenicity of Hexavalent Chromium and Its Effects
Page: 205-213 (9)
Author: Sachin Verma, Pallavi Kumari, Shailesh Kumar and Ashok Kumar Jha*
DOI: 10.2174/9789815165043123100009
PDF Price: $15
Abstract
Hexavalent chromium has been a potential threat to human beings due to its
toxicity and carcinogenesis. The pathway of entry of hexavalent chromium in an
aqueous medium is both anthropogenic and natural through ores of chromium.
Prolonged exposure to hexavalent chromium may cause DNA mismatch and gene
mutation, resulting in cancer. Cr(VI)- induced malignant cell and its study has become
very important towards the possible mechanism of Cr(VI) binding. When a cell of the
human lungs adsorbs hexavalent chromium due to prolonged ingestion of Cr(VI)
contaminated water or inhalation, oxidative DNA damage is caused in the specific
gene. This causes mutations in adenine and guanine bases of DNA in cases of lung
cancer.
Medicinal Plants: A Future of Modern Medical System
Page: 214-232 (19)
Author: Aakansha Singh and Anjani Kumar*
DOI: 10.2174/9789815165043123100010
PDF Price: $15
Abstract
Humans, since their evolution, have always been in close contact with
mother nature. Early life has been dependent solely on environmental resources for
their livelihood. The trial-and-error approach in utilizing different resources came up
with incorporating plants as a whole or their parts for food and survival. Gradually, the
knowledge of medicinal plants was gained by our ancestors, and there started the
Indian medical history of Ayurveda. In the current scenario, a huge number of
medicinal herbs are being consumed in day-to-day life, which imparts tremendous
benefits to human health. Our interest in gaining knowledge of medicinal components
present in these herbs has led to many important discoveries in the area of drug
development. Nowadays, numerous plants derived compounds are being used in
modern medicines. In view of utilizing these natural resources efficiently, we need to
understand their components in a better way. This chapter is towards gaining a deeper
knowledge about medicinal plants, their role in different diseases, and insights into
drug discovery.
Shikonin, a Naphthaquinone of Commercial Importance: its Biosynthesis and Prospect for Use as Drugs
Page: 233-248 (16)
Author: Ravi S. Singh* and Sanjay Kumar
DOI: 10.2174/9789815165043123100011
PDF Price: $15
Abstract
Shikonin is a red naphthaquinone pigment present in the roots of plants of
the Boraginaceae family. This pigment is an as active ingredient in several
pharmaceutical and cosmetics preparations, and as a dye for fabrics and food items. It
shows many bioactivities such as stimulation of peroxidase, protection against UV-radiation, inhibition of microsomal monooxygenase and induction and secretion of
nerve growth factor. In this book chapter, we have provided detailed information on its
biosynthesis and prospects for pharmaceutical use.
Fast Foods: Chemical Composition and Implications for Health
Page: 249-261 (13)
Author: Ruchi Kumari and Ravi S. Singh*
DOI: 10.2174/9789815165043123100012
PDF Price: $15
Abstract
With changing the scenarios of living style, professional work culture, and
daily hectic routine, liberal and global thoughts are impacting our dietary patterns and
normal food consumption. So the preference for foods is changing, and foods that can
be ready in a shorter time, like “fast foods”, are gaining popularity among the masses,
especially young generations. The fast food business has become one of the fastest-growing industries across the globe. This growing trend of fast food consumption has
also brought several health-associated issues, like obesity and heart-related problems.
Therefore, health-conscious people do like to know the chemical ingredients embedded
in fast foods as well as their packaging and storage. For this purpose, the chemistry
relating to quality aspects of fast foods, including nutritional, physiological, sensory,
flavor, microbiological and packaging, is very important for healthy consumption of
fast food for a healthy life. In this book chapter, we have made efforts to bring updated
information related to fast food, its chemical composition and implications for human
health.
Implications of DNA-acting Agents as Anticarcinogenic Potential in Breast Cancer Therapeutics
Page: 262-280 (19)
Author: Lovely Sinha* and Ujjwal Kumar
DOI: 10.2174/9789815165043123100013
PDF Price: $15
Abstract
Breast cancer is the most prevalent neoplasm diagnosed in women
worldwide. There are many factors responsible for breast cancer susceptibility.
Mutation in tumor suppressor genes BRCA1 and BRCA2 predispose women to the early
onset of breast cancer. The BRCA genes are involved in multiple cellular processes in
response to DNA damage, including checkpoint activation, gene transcription, and
DNA repair. Several DNA-acting agents act as effective anticancer used for treating
cancer disease. Certain groups of chemicals are known to affect specific phases of cell
division, such as, Cyclophosphamide is the most potent and successful anticancer agent
that acts by alkylating the N-7position of guanine to cause crosslinking of DNA’s
double helix, resulting in DNA breaks that interfere with the DNA replication and
RNA transcription. This chapter deals with the classification of DNA-acting agents
according to their modes of action.
Aloe Vera-A Medicinal Plant as Potential Therapeutic Agents for Liver Cancer
Page: 281-289 (9)
Author: Lovely Sinha*, Ghanshyam Kumar Satyapal and Shailendra Kumar
DOI: 10.2174/9789815165043123100014
PDF Price: $15
Abstract
Liver cancer is the sixth most commonly diagnosed cancer and the fourth
leading cause of cancer death worldwide. Research over the last two decades has
revealed that medicinal plants have been used for the treatment of various neoplastic
diseases. Aloe vera is a ubiquitously naturally occurring and drought-resisting herbal
medicinal plant. Some reports suggest that Aloe vera possesses wound and burn
healing activities and anti-inflammatory as well as immunomodulatory effects. There
are no direct studies available on the role of the Aloe vera extract and its active
ingredient like aloe-emodin that modulates antiaging and anticancer activities,
particularly on immune cells as well as liver cancer cells. Aloe vera has many bioactive
compounds and pharmacological properties that may show an important role in liver
cancer prevention and treatment through the enhancement of regeneration, antiaging
activity, antioxidant activity, anticancer activity and modulation of genetic pathways.
Here, we discuss the study of the anticancer effect and modulation of expression of
various genes in response to Aloe vera in liver cancer.
Subject Index
Page: 290-294 (5)
Author: Ashok Kumar Jha and Ravi S. Singh
DOI: 10.2174/9789815165043123100015
Introduction
Frontiers in Medicinal Chemistry is a book series devoted to reviews on research topics relevant to medicinal chemistry and allied disciplines. Frontiers in Medicinal Chemistry covers developments in rational drug design, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, chemoinformatics, and structure-activity relationships. This book series is essential for any medicinal chemist who wishes to be updated on the latest and the most important advances in the field. This is the tenth volume of the series. The extensive volume brings 11 reviews on a variety of topics including anti-cancer drug therapeutics, food chemistry, toxicology and drug development strategies. The list of topics in this volume includes: Isoxazole derivatives as potential pharmacophore for new drug development Contemporary trends in drug repurposing: identifying new targets for existing drugs Pharmaceutical potential of pyrimidines as antiviral agents Drugs and phytochemicals targeting cancer Harnessing the neurological properties of indian brain health booster brahmi Carcinogenicity of hexavalent chromium and its effects Medicinal plants: a future of modern medical system Shikonin, a naphthaquinone of commercial importance: its biosynthesis and prospect for use as drugs Fast foods: chemical composition and implications for health Implications of DNA-acting agents as anticarcinogenic potential in breast cancer therapeutics Aloe vera - a medicinal plant as potential therapeutic agents for liver cancer