scholarly journals BIOLOGICAL POTENTIAL OF BENZOXAZOLE DERIVATIVES: AN UPDATED REVIEW

2020 ◽  
pp. 28-41
Author(s):  
UDDIN KAMAL ◽  
NAIM MOHD JAVED ◽  
KUMAR ARUN
Keyword(s):  
Antimicrobial Activity ◽  
Literature Search ◽  
Therapeutic Potential ◽  
Anthelmintic Activity ◽  
Pharmacological Activities ◽  
Drug Molecules ◽  
Biological Potential ◽  
Derivatives Of ◽  
Heterocyclic Moiety

Objective: Heterocycles exhibited an extensive role in the medicinal chemistry for the development of pharmaceutically active molecules. A heterocyclic scaffold is responsible for the therapeutic potential of majority of synthesized drug molecules. Therapeutic changes in the drug molecules related to the slight changes in the heterocyclic moiety. Benzoxazole and its derivatives showed potent and significant pharmacological activities. The main objective of our study is to impart updated information about synthesized benzoxazole derivatives and their biological potential against numerous diseases. Methods: A literature search was directed on the databases, namely, in MDPI, Science direct, PubMed, Springer, Taylor, and Francis by searching different keywords “Benzoxazole,” antimicrobial activity, anticancer activity, antitubercular, anti-inflammatory, analgesic, and anthelmintic activity. Conclusion: This review may radiate the path of researchers that are working to synthesized novel benzoxazole derivatives in the prospects of effectiveness and safety. Nonetheless, further in vivo and clinical studies are warranted on the potential derivatives of benzoxazole.

scholarly journals Pharmacological Advances of Chloroquine and Hydroxychloroquine: From Antimalarials to Investigative Therapies in COVID-19

2020 ◽  
Vol 15 (9) ◽  
pp. 1934578X2095364
Author(s):  
Yang Song ◽  
Elise Fields
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Adverse Effects ◽  
Viral Infection ◽  
Therapeutic Potential ◽  
Pharmacological Activities ◽  
Pharmaceutical Applications ◽  
Natural Alkaloid ◽  
Derivatives Of ◽  
Existing Chemicals

During the coronavirus disease 2019 (COVID-19) pandemic, numerous existing chemicals have been screened for antiviral potential against the emerging coronavirus severe acute respiratory syndrome coronavirus 2. Chloroquine and hydroxychloroquine, after exhibiting potent in vitro efficacy, have gained tremendous attention. Both therapeutics are derivatives of natural alkaloid quinine and were first synthesized to treat malaria. Thereafter, the pharmaceutical applications of the agents have expanded to many new areas. In this article, the medicinal history and pharmacological activities of chloroquine and hydroxychloroquine are summarized. Antimalarial, anti-inflammatory, antitumor, antiviral properties, and therapeutic potential in the emerging viral infection COVID-19 are discussed. Pharmacokinetics, adverse effects, and toxicities are reviewed.

Chyavanprash: Choice of Drug for immunity boosting and health supplements during COVID -19 pandemic

2020 ◽  
Vol 11 (SPL1) ◽  
pp. 1346-1350
Author(s):  
Bharat Rathi ◽  
Renu Rathi ◽  
Vinod Ade ◽  
Akshay Pargaonkar
Keyword(s):  
Therapeutic Potential ◽  
Age Groups ◽  
Pharmacological Activities ◽  
Common People ◽  
The World ◽  
The Common ◽  
Made In ◽  
Health Supplements

Chyavanprash a known Ayurvedic formulation formulated by sage Chyavan to impart youth, charm, strength & prolonged life. It is very much valued for possessing numerous health benefits with respect to the preventive, curative and promotive aspects of health. Chyavanprash can be consumed throughout the year. Several scientific evidences support its wholesome and safe healthy tonic status that is favorable for all age groups and genders alike. In modern days, it has gained mammoth popularity throughout the world. CP is prepared with Amalaki (Emblica officinalis) as a prime drug with other nutrient rich herbs help to preserve stamina, strength and vitality. Various pre clinical (in vivo & in vitro), Experimental, Analytical and clinical studies conducted on CP and its individual components revealed its various pharmacological activities most of which are suggestive of immunity enhancer and health supplements. Hence an attempt is made in the present paper to find out and explore the scientific evidences based on therapeutic potential of CP with respect to immunity and health supplements and make evidences available to the common people to combat the COVID-19 menace effectively.

A Review of Saurauia roxburghii Wall. (Actinidiacaea) as a Traditional Medicinal Plant, Its Phytochemical Study and Therapeutic Potential

2020 ◽  
Vol 20 (19) ◽  
pp. 2036-2051
Author(s):  
Afsana Nahrin ◽  
Md. Junaid ◽  
Syeda Samira Afrose ◽  
Muhammad Shaiful Alam ◽  
S.M. Zahid Hosen ◽  
...  
Keyword(s):  
Ursolic Acid ◽  
Therapeutic Potential ◽  
Wide Spectrum ◽  
Relevant Information ◽  
In Vitro Tests ◽  
Pharmacological Activities ◽  
Phytochemical Study ◽  
Corosolic Acid

Saurauia roxburghii Wall. is an interesting plant, found growing chiefly along the eastern and south-eastern countries of Asia. The various ethnic groups of these regions use the plant as a medication for relieving a wide spectrum of diseases and conditions, including indigestion, boils, fever, gout, piles, eczema, asthma, ulcers, bronchitis, epilepsy, and hepatitis B. This review aims to appraise the vernacular information, botanical characterization, geographical distribution, traditional uses, phytochemistry, and pharmacological activities of S. roxburghii as well as to conduct a critical analysis on the findings. To understand the therapeutic potential and provide an overall idea about the ethnomedicinal practices, phytochemistry, and pharmacological activities of S. roxburghii, relevant information was collected via a library and electronic search of online journals, books, and reputed databases. Phytochemical examination revealed the presence of alkaloids, glycosides, O-glycosides, flavonoids, carbohydrates, saponins, steroids, reducing sugars, tannins, phlobatannins, and triterpenoids. The sterols were identified as Stigmasterol and beta-Sitosterol. The triterpenes were found to be Ursolic acid, Corosolic acid, Maslinic acid, 24-Hydroxy corosolic acid, 3b,7b,24-trihydroxy-urs-12-en-28-oic acid, Oleanolic acid, beta-Amyrin, cis-3-O-p-Hydroxycinnamoyl ursolic acid, trans-3-O-p- Hydroxycinnamoyl ursolic acid, and 7,24-dihydroxyursolic acid. Several in-vivo and in-vitro tests revealed anti-bacterial, anti-cancer, anti-diabetic, anti-oxidant, and anti-viral activities of the plant leaves. Detailed analysis of the information collected on S. roxburghii suggested some promising leads for future drug development. However, many scientific gaps were found in the study of this and further extensive investigation is needed to fully understand the mechanism of action of the active constituents and exploit its therapeutic promises.

New Derivatives of Bacteriopurpurin with Thiolated Au (I) Complexes: Dual Darkand Light Activated Antitumor Potency

2020 ◽  
Vol 20 (1) ◽  
pp. 49-58
Author(s):  
Mikhail A. Grin ◽  
Sergei I. Tikhonov ◽  
Albina S. Petrova ◽  
Victor A. Pogorilyy ◽  
Аlexey N. Noev ◽  
...  
Keyword(s):  
Cell Death ◽  
Antitumor Agents ◽  
Therapeutic Potential ◽  
Human Tumor ◽  
Water Soluble ◽  
Light Activation ◽  
Massive Cell Death ◽  
P53 Inactivation ◽  
Derivatives Of

Background:: Conventional antitumor Photosensitizers (PS) are normally low toxic in the dark whereas light activation triggers massive cell death (photodynamic therapy, PDT). Objective:: To expand the therapeutic potential of PS to dual potency cytocidal agents, taking advantage of the use of bacteriopurpurin for a deeper tissue penetration of light, and suitability of the tetrapyrrolic macrocycle for chemical modifications at its periphery. Methods:: Conjugation of a pro-oxidant thiolate Au (I) moiety to the bacteriopurpurin core and evaluation of cytotoxicity in cell culture and in vivo. Results:: New water-soluble derivatives showed micromolar cytotoxicity for cultured human tumor cell lines in the dark, including the subline with an altered drug response due to p53 inactivation. Cellular PDT with the selected conjugate, thiolate Au (I)-dipropoxybacteriopurpurinimide (compound 6) with two triphenylphosphine Au fragments, triggered rapid (within minutes) cell death. Damage to the plasma membrane (necrosis) was a hallmark of cell death by compound 6 both in the dark and upon light activation. Furthermore, one single i.v. injection of compound 6 caused retardation of transplanted syngeneic tumors at the tolerable dose. Illumination of tumors that accumulated compound 6 significantly synergized with the effect of 6 in the dark. Conclusion:: Complexes of virtually non-toxic, photoactivatable bacteriopurpurin with the gold-containing organic moiety are considered the dual potency antitumor agents, tentatively applicable for intractable tumors.

scholarly journals Antimicrobial Activity of Oleanolic and Ursolic Acids: An Update

2015 ◽  
Vol 2015 ◽  
pp. 1-14 ◽  
Author(s):  
Jéssica A. Jesus ◽  
João Henrique G. Lago ◽  
Márcia D. Laurenti ◽  
Eduardo S. Yamamoto ◽  
Luiz Felipe D. Passero
Keyword(s):  
Antimicrobial Activity ◽  
Animal Health ◽  
Mechanisms Of Action ◽  
Human Pathogens ◽  
Future Perspectives ◽  
Pharmacological Activities ◽  
Long Period ◽  
Wide Range ◽  
Potential Use

Triterpenoids are the most representative group of phytochemicals, as they comprise more than 20,000 recognized molecules. These compounds are biosynthesized in plants via squalene cyclization, a C30hydrocarbon that is considered to be the precursor of all steroids. Due to their low hydrophilicity, triterpenes were considered to be inactive for a long period of time; however, evidence regarding their wide range of pharmacological activities is emerging, and elegant studies have highlighted these activities. Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids. These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now. Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, viain vivostudies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

Can antioxidant nutraceuticals benefit the menopause?

2002 ◽  
Vol 8 (3) ◽  
pp. 98-101
Author(s):  
Erick Valencia ◽  
Angela Marin ◽  
Gil Hardy
Keyword(s):  
Breast Cancer ◽  
Chronic Diseases ◽  
Prognostic Value ◽  
Literature Search ◽  
Therapeutic Potential ◽  
Nutritional Supplements ◽  
Ageing Population ◽  
Physiological Changes ◽  
Menopausal Women

The antioxidants glutathione, selenium and vitamins C and E meet the criteria for nutraceuticals and their in vivo concentrations can undoubtedly influence and improve many disease processes. In an attempt to quantify and correlate their individual roles as nutritional supplements with their therapeutic potential to improve symptoms and lifestyle during the menopause, we conducted a literature search covering the 15 years up to 2001. Few publications were found dealing specifically with menopausal women. Approximately 90% reported research with vitamins and/or selenium and only one paper investigated a possible correlation between glutathione and breast cancer. This relatively low level of research interest in nutritional or antioxidant aspects of the menopause may just reflect a preoccupation with the more general chronic diseases of an ageing population, without necessarily acknowledging the important physiological changes that occur in women. The little encouraging data in the literature should stimulate more research into the prognostic value, mechanisms and efficacy of nutraceutical supplementation that specifically relate to menopausal women.

scholarly journals Imperata cylindrica: A Review of Phytochemistry, Pharmacology, and Industrial Applications

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1454
Author(s):  
Young-Kyung Jung ◽  
Dongyun Shin
Keyword(s):  
Medicinal Plant ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Industrial Applications ◽  
Imperata Cylindrica ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Pharmacological Studies

Imperata cylindrica is a medicinal plant native to southwestern Asia and the tropical and subtropical zones. To date, 72 chemical constituents have been isolated and identified from I. cylindrica Among these compounds, saponins, flavonoids, phenols, and glycosides are the major constituents. Investigations of pharmacological activities of I. cylindrica revealed that this edible medicinal herb exhibits a wide range of therapeutic potential including immunomodulatory, antibacterial, antitumor, anti-inflammatory, and liver protection activities both in vivo and in vitro. The purpose of this review is to provide an overview of I. cylindrica studies until 2019. This article also intends to review advances in the botanical, phytochemical, and pharmacological studies and industrial applications of I. cylindrica, which will provide a useful bibliography for further investigations and applications of I. cylindrica in medicines and foods.

scholarly journals Synthesis and therapeutic potential of imidazole containing compounds

BMC Chemistry ◽  
2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Ankit Siwach ◽  
Prabhakar Kumar Verma
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Biological Properties ◽  
New Drugs ◽  
Hydrogen Atoms ◽  
Tautomeric Forms ◽  
Synthetic Routes ◽  
Derivatives Of ◽  
Heterocyclic Moiety ◽  
Antihistaminic Agent

Abstract Imidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen. The imidazole name was reported by Arthur Rudolf Hantzsch (1857–1935) in 1887. 1, 3-diazole is an amphoteric in nature i.e. it shows both acidic and basic properties. It is a white or colorless solid that is highly soluble in water and other polar solvents. Due to the presence of a positive charge on either of two nitrogen atom, it shows two equivalent tautomeric forms. Imidazole was first named glyoxaline because the first synthesis has been made by glyoxal and ammonia. It is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. The derivatives of 1, 3-diazole show different biological activities such as antibacterial, antimycobacterial, anti-inflammatory, antitumor, antidiabetic, anti-allergic, antipyretic, antiviral, antioxidant, anti-amoebic, antihelmintic, antifungal and ulcerogenic activities, etc. as reported in the literature. There are different examples of commercially available drugs in the market which contains 1, 3-diazole ring such as clemizole (antihistaminic agent), etonitazene (analgesic), enviroxime (antiviral), astemizole (antihistaminic agent), omeprazole, pantoprazole (antiulcer), thiabendazole (antihelmintic), nocodazole (antinematodal), metronidazole, nitroso-imidazole (bactericidal), megazol (trypanocidal), azathioprine (anti rheumatoid arthritis), dacarbazine (Hodgkin's disease), tinidazole, ornidazole (antiprotozoal and antibacterial), etc. This present review summarized some pharmacological activities and various kinds of synthetic routes for imidazole and their derived products.

scholarly journals Antimicrobial Activity from Species Plectranthus amboinicus (Lour.) Spreng, a Review

2020 ◽  
pp. 1-14
Author(s):  
Juliane Maria dos Santos Silva ◽  
Jackson Roberto Guedes da Silva Almeida ◽  
Cristiane dos Santos Cerqueira Alves ◽  
Daniel Amando Nery ◽  
Livia Maria Oliveira Damasceno ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Therapeutic Potential ◽  
In Vivo Studies ◽  
Synergistic Activity ◽  
Popular Medicine ◽  
Plectranthus Amboinicus

Introduction: Nowadays, several bacteria have acquired resistance to available antimicrobial agents making necessary the search for new therapeutic alternatives. Plectranthus amboinicus L. is a succulent and aromatic herb, popularly known as thick leaf mint, used in popular medicine for the treatment of colds, digestive diseases, asthma, headache and to fight pathogenic bacteria activity. In view the antimicrobial activity of P. amboinicus this study had as aim to review publications involving researches about antimicrobial activity of this species. Materials and Methods: For this, PubMed, Scopus, Science Direct and Scielo databases were consulted in November 2020 using the keywords Plectranthus amboinicus and antimicrobial activity. In vitro and/or in vivo studies on the antimicrobial activity of the species in the last 10 years were considered. Results: The main microorganisms evaluated were: Klebsiella pneumoniae, Mycobacterium tuberculosis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and some Candida species. The essential oils had carvacrol, germacrene D, thymol and camphor as main constituents. Most studies evaluated the antimicrobial activity using broth dilution and agar diffusion methods. In most studies essential oil, extracts and/or isolated substances showed significant antimicrobial activity. Synergistic activity was also observed through association with antibiotics. Conclusion: P. amboinicus has therapeutic potential for antimicrobial treatments and can be an alternative to the treatment of resistant microorganisms and that further in vivo and clinical studies with the species are still needed.

Antimicrobial activities of various thiazine based heterocyclic compounds: A mini-review

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran ◽  
Abida
Keyword(s):  
Antimicrobial Activity ◽  
Drug Resistance ◽  
Heterocyclic Compounds ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Vital Role ◽  
Pharmacological Activities ◽  
Natural Sources ◽  
Anti Inflammatory ◽  
Heterocyclic Moiety

: Heterocyclic compounds play a vital role in the development of novel compounds due to their diverse pharmacological activities. Thiazine is a six-membered heterocyclic moiety. Various thiazine derivatives were synthesized or isolated from natural sources like plants and animals. Thiazine derivatives have varieties of pharmacological activities such as antimicrobial, antibacterial, antifungal, antiviral, anti-inflammatory, anticoagulant, anticancer, antihypertensive, and other useful biological as well as chemical applications. In the therapy of antimicrobial infections, new antimicrobial agents are needed because current antimicrobials have developed drug resistance. So, we discussed some thiazine derivatives which exhibited antimicrobial activity.

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