scholarly journals A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold

2020 ◽  
Vol 8 (1) ◽  
pp. 23-29
Author(s):  
Ritchu Babbar ◽  
Swikriti ◽  
Sandeep Arora
Keyword(s):  
Therapeutic Potential ◽  
Therapeutic Agents ◽  
Pharmacological Activities ◽  
Therapeutic Drugs ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds ◽  
Therapeutic Compounds ◽  
Derivatives Of ◽  
Cns Stimulant

Background: Benzimidazole is a category of heterocyclic aromatic compounds formed from the fusion of six membered benzene with five membered imidazolering. The moiety possesses diverse biological and clinical applications. A number of studies have shown that a varied substituent around the benzimidazole nucleus results in pharmacologically active compounds of therapeutic interest. Purpose: Owing to its number of pharmacological properties, this moiety is of choice of interest in designing and synthesis of new therapeutic compounds. The existence of the benzimidazole core in numerous groups of biological agents like antimicrobial, antiviral, antiparasitic, antihypertensive, anticancer, CNS stimulant as well as depressants has made important scaffold for development of many newer therapeutic agents. There is utmost need to understand the synthesis and associated role of benzimidazole derived compounds in different diseases. Therefore, in the present review, we attempt to discuss various derivatives of benzimidazole nucleus with different pharmacological activities. Conclusion: Benzimidazoles have played a great role in discovery of drug and development. Huge attempt has been made towards benzimidazole heterocyclic-based organic compounds with great excellence that resulted in drugs with enormous biological activity. Therapeutic drugs containing benzimidazole nucleus are used in building drugs that serve to be an active area of research. This article becomes a source that will lead to discovery of new opportunities for all researchers interested in benzimidazole-based heterocyclic medicinal chemistry.

scholarly journals A review on phytochemical and ethnopharmacological studies of Ajuga Bracteosa Wall. Ex Benth.

2019 ◽  
Vol 9 (2) ◽  
pp. 489-492
Author(s):  
Tabasum Ali ◽  
Zahida Shah ◽  
Rabiah Bashir
Keyword(s):  
Therapeutic Potential ◽  
Iridoid Glycosides ◽  
Herbal Medicines ◽  
Review Article ◽  
Pharmacological Activities ◽  
Cardiotonic Activity ◽  
Traditional System ◽  
The Family ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds

Herbal medicines as the major remedy in traditional system of medicine have been used in medical practices since antiquity. The plants of genus Ajuga are evergreen, clump-forming rhizomatous perennial or annual herbaceous flowering species, with Ajuga being one of the 266 genera of the family Lamiaceae. There are at least 301 species of the genus Ajuga with many variations. Ajugabracteosa Wall. ex Benth (A. bracteosa) is an important medicinal plant of Himalaya regions. Medicinal potential is due to presence of of various pharmacologically active compounds such as neo-clerodane diterpenoids, flavonol glycosides, iridoid glycosides, ergosterol-5,8- endoperoxide and phytoecdysones. The aim of this review article was to gather information about A. bracteosa which is currently scattered in form of various publications. This review article tried to attract the attention from people for therapeutic potential of A. bracteosa. The present review comprises upto date information of,traditional uses, botanical aspects, active ingredients and pharmacological activities such as antitumor, antimicrobial, antimalarial, anti-inflammatory, cardiotonic activity, antiarthritic activity, antioxidant activity . A large variety of compounds have so far been isolated from Ajuga bracteosa. Keywords:  Ajuga bracteosa, Herbal medicines, pharmacological activities.

scholarly journals Synthesis, physico-chemical properties of derivatives 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-4-amine

2018 ◽  
pp. 50-54
Author(s):  
A. A. Safonov
Keyword(s):  
Chemical Properties ◽  
High Reactivity ◽  
Pharmacological Activities ◽  
High Biological Activity ◽  
Physico Chemical ◽  
Low Toxicity ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds ◽  
New Compounds ◽  
Derivatives Of

Recently, the search for new compounds with high biological activity, which can be the basis for potential drugs, becomes topical for world scientists. A heterocyclic compound cause particular interest in this area as highly pharmacologically active compounds. Scientists extends interest due to the low toxicity and high reactivity 1,2,4-triazole of the system. It is proved that the combination of triazole nucleus with other heterocyclic systems, especially in the fifth position, causes increased biological effect, and, sometimes, the appearance of new pharmacological activities. The aim of the work was the synthesis of 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines and their derivatives, study of their physico-chemical properties. A series of new derivatives of the compounds 4-amino-5-R-1,2,4-triazole-3-thione (3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines and N-R-idene)-3-(nonylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines) was synthesizes. The structure of compounds is set with modern physico-chemical methods of analysis (elemental analysis, 1H-NMR spectroscopy). Individuality is proved by HPLC-MS.

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.

scholarly journals Development of A Continuous Fluorescence-Based Assay for N-Terminal Acetyltransferase D

2021 ◽  
Vol 22 (2) ◽  
pp. 594
Author(s):  
Yi-Hsun Ho ◽  
Lan Chen ◽  
Rong Huang
Keyword(s):  
Lung Cancer ◽  
Cancer Progression ◽  
High Throughput Screening ◽  
Coenzyme A ◽  
Therapeutic Potential ◽  
Biological Functions ◽  
Histone H4 ◽  
Fluorescent Signal ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds

N-terminal acetylation catalyzed by N-terminal acetyltransferases (NATs) has various biological functions in protein regulation. N-terminal acetyltransferase D (NatD) is one of the most specific NAT with only histone H4 and H2A proteins as the known substrates. Dysregulation of NatD has been implicated in colorectal and lung cancer progression, implying its therapeutic potential in cancers. However, there is no reported inhibitor for NatD yet. To facilitate the discovery of small-molecule NatD inhibitors, we report the development of a fluorescence-based acetyltransferase assay in 384-well high-throughput screening (HTS) format through monitoring the formation of coenzyme A. The fluorescent signal is generated from the adduct in the reaction between coenzyme A and fluorescent probe ThioGlo4. The assay exhibited a Z′-factor of 0.77 and a coefficient of variation of 6%, indicating it is a robust assay for HTS. A pilot screen of 1280 pharmacologically active compounds and subsequent validation identified two hits, confirming the application of this fluorescence assay in HTS.

ChemInform Abstract: SEARCH FOR PHARMACOLOGICALLY ACTIVE COMPOUNDS IN A SERIES OF AMINOMETHYL DERIVATIVES OF 5-HYDROXYBENZOFURAN

1979 ◽  
Vol 10 (29) ◽  
Author(s):  
A. N. GRINEV ◽  
N. V. ARKHANGEL'SKAYA ◽  
G. YA. URETSKAYA ◽  
A. A. STOLYARCHUK ◽  
P. A. GALENKO-YAROSHEVSKII
Keyword(s):  
Active Compounds ◽  
Aminomethyl Derivatives ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds ◽  
Derivatives Of

V. Therapeutic potential of nitric oxide donors and inhibitors

1999 ◽  
Vol 276 (6) ◽  
pp. G1313-G1316 ◽  
Author(s):  
Marcelo N. Muscará ◽  
John L. Wallace
Keyword(s):  
Nitric Oxide ◽  
Therapeutic Potential ◽  
Tissue Injury ◽  
Mucosal Injury ◽  
Therapeutic Agents ◽  
Gastrointestinal Physiology ◽  
Inflammatory Drugs ◽  
Nitric Oxide Releasing ◽  
Oxide Synthase

Nitric oxide is a crucial mediator of gastrointestinal mucosal defense, but, paradoxically, it also contributes to mucosal injury in several situations. Inhibitors of nitric oxide synthesis and compounds that release nitric oxide have been useful pharmacological tools for evaluating the role of nitric oxide in gastrointestinal physiology and pathophysiology. Newer inhibitors with selectivity for one of the isoforms of nitric oxide synthase are even more powerful tools and may have utility as therapeutic agents. Also, agents that can scavenge nitric oxide or peroxynitrite are promising as drugs to prevent nitric oxide-associated tissue injury. Compounds that release nitric oxide in small amounts over a prolonged period of time may also be very useful for prevention of gastrointestinal injury associated with shock and with the use of drugs that have ulcerogenic effects. Indeed, the coupling of a nitric oxide-releasing moiety to nonsteroidal anti-inflammatory drugs has proven to be a valid means of substantially reducing the gastrointestinal toxicity of these drugs without decreasing their efficacy.

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.

A High-Throughput Assay for Modulators of NNT Activity in Permeabilized Yeast Cells

2011 ◽  
Vol 16 (7) ◽  
pp. 734-743
Author(s):  
Nicholas A. Meadows ◽  
Barbara Saxty ◽  
Mary S. Albury ◽  
Catherine A. Kettleborough ◽  
Frances M. Ashcroft ◽  
...  
Keyword(s):  
Insulin Secretion ◽  
Mammalian Cells ◽  
Yeast Cells ◽  
Glucose Tolerance Tests ◽  
Novel Target ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds ◽  
High Throughput Assay ◽  
First Time

Nicotinamide nucleotide transhydrogenase (NNT) mutant mice show glucose intolerance with impaired insulin secretion during glucose tolerance tests. Uncoupling of the β cell mitochondrial metabolism due to such mutations makes NNT a novel target for therapeutics in the treatment of pathologies such as type 2 diabetes. The authors propose that increasing NNT activity would help reduce deleterious buildup of reactive oxygen species in the inner mitochondrial matrix. They have expressed human Nnt cDNA for the first time in Saccharomyces cerevisiae, and transhydrogenase activity in mitochondria isolated from these cells is six times greater than is seen in wild-type mitochondria. The same mitochondria have partially uncoupled respiration, and the cells have slower growth rates compared to cells that do not express NNT. The authors have used NNT’s role as a redox-driven proton pump to develop a robust fluorimetric assay in permeabilized yeast. Screening in parallel a library of known pharmacologically active compounds (National Institute of Neurological Disorders and Stroke collection) against NNT ± cells, they demonstrate a robust and reproducible assay suitable for expansion into larger and more diverse compound sets. The identification of NNT activators may help in the elucidation of the role of NNT in mammalian cells and assessing its potential as a therapeutic target for insulin secretion disorders.

scholarly journals Development of a continuous fluorescence-based assay for N-terminal acetyltransferase D

2020 ◽  
Author(s):  
Yi-Hsun Ho ◽  
Lan Chen ◽  
Rong Huang
Keyword(s):  
Lung Cancer ◽  
Cancer Progression ◽  
High Throughput Screening ◽  
Coenzyme A ◽  
Therapeutic Potential ◽  
Biological Functions ◽  
Histone H4 ◽  
Fluorescent Signal ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds

AbstractN-terminal acetylation catalyzed by N-terminal acetyltransferases (NATs) has various biological functions in protein regulation. N-terminal acetyltransferase D (NatD) is one of the most specific NAT with only histone H4 and H2A proteins as the known substrates. Dysregulation of NatD has been implicated in colorectal and lung cancer progression, implying its therapeutic potential in cancers. However, there is no reported inhibitor for NatD yet. To facilitate the discovery of small-molecule NatD inhibitors, we report the development of a fluorescence-based acetyltransferase assay in 384-well high-throughput screening (HTS) format through monitoring the formation of coenzyme A. The fluorescent signal is generated from the adduct in the reaction between coenzyme A and fluorescent probe ThioGlo4. The assay exhibited a Z’-factor of 0.77 and a coefficient of variation of 6%, indicating it is a robust assay for HTS. A pilot screen of 1280 pharmacologically active compounds and subsequent validation identified two hits, confirming the application of this fluorescence assay in HTS.

scholarly journals Ursolic Acid-Based Derivatives as Potential Anti-Cancer Agents: An Update

2020 ◽  
Vol 21 (16) ◽  
pp. 5920 ◽  
Author(s):  
Vuyolwethu Khwaza ◽  
Opeoluwa O. Oyedeji ◽  
Blessing A. Aderibigbe
Keyword(s):  
Ursolic Acid ◽  
Clinical Medicine ◽  
Biological Activities ◽  
Therapeutic Effects ◽  
Pharmacological Activities ◽  
Pentacyclic Triterpenoid ◽  
Anti Cancer ◽  
Pharmacologically Active ◽  
Derivatives Of ◽  
Cell Signaling Pathways

Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.

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