Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities

2022 ◽  
pp. 114085
Author(s):  
Xiaoying Jiang ◽  
Kaiyu Wu ◽  
Renren Bai ◽  
Pengfei Zhang ◽  
Yi Zhang
Keyword(s):  
Pharmacological Activities ◽  
Privileged Structures

scholarly journals A Review of the Pharmacological Activities and Recent Synthetic Advances of γ-Butyrolactones

2021 ◽  
Vol 22 (5) ◽  
pp. 2769
Author(s):  
Joonseong Hur ◽  
Jaebong Jang ◽  
Jaehoon Sim
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Small Molecules ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Pharmacological Activities ◽  
New Developments ◽  
The Past ◽  
Privileged Structures ◽  
Significant Attention

γ-Butyrolactone, a five-membered lactone moiety, is one of the privileged structures of diverse natural products and biologically active small molecules. Because of their broad spectrum of biological and pharmacological activities, synthetic methods for γ-butyrolactones have received significant attention from synthetic and medicinal chemists for decades. Recently, new developments and improvements in traditional methods have been reported by considering synthetic efficiency, feasibility, and green chemistry. In this review, the pharmacological activities of natural and synthetic γ-butyrolactones are described, including their structures and bioassay methods. Mainly, we summarize recent advances, occurring during the past decade, in the construction of γ-butyrolactone classified based on the bond formation in γ-butyrolactone between (i) C5-O1 bond, (ii) C4-C5 and C2-O1 bonds, (iii) C3-C4 and C2-O1 bonds, (iv) C3-C4 and C5-O1 bonds, (v) C2-C3 and C2-O1 bonds, (vi) C3-C4 bond, and (vii) C2-O1 bond. In addition, the application to the total synthesis of natural products bearing γ-butyrolactone scaffolds is described.

Multicomponent Catalytic Synthesis of 1,5-Benzodiazepines: An Update

2020 ◽  
Vol 17 (4) ◽  
pp. 465-484 ◽  
Author(s):  
Rajesh K. Singh ◽  
Sadhna Sharda ◽  
Shikha Sharma ◽  
Sahil Kumar ◽  
Deo Nandan Prasad
Keyword(s):  
Lewis Acids ◽  
Supported Catalysts ◽  
Pharmacological Activities ◽  
One Pot ◽  
Reaction Condition ◽  
Current Review ◽  
Main Motive ◽  
Privileged Structures ◽  
Green Chemical Synthesis ◽  
The One

1,5-Benzodiazepines are considered some of the most vital classes of heterocyclic compounds due to their amazing biological and varied pharmacological activities. They are regarded as privileged structures and therefore have been striking synthetic targets for organic and medicinal chemists over the last decade. This results in the exploration of various silica supported catalysts, Lewis acids, organoacids, magnetic nanoparticles and other miscellaneous catalysts that have been investigated till date for an efficient and green synthesis of 1,5-benzodiazepine and its derivatives. The current review article primarily covers the one-pot green chemical synthesis of 1,5- benzodiazepines using various novel catalysts. The main motive of this review is the assessment of the literature on various catalysts along with their yield, reaction condition, and mechanism of action. In the end, the entire catalysts are structured systematically into various Lewis acids, Bronsted organoacids, supported catalysts, nanocatalysts, and miscellaneous catalysts and are presented in the form of tables for quick ‘at a glance’ study of catalysts, their reaction condition, time taken, etc.

The effect of different extraction methods on chemical composition profile and pharmacological activities of essential oils and hydrosols

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
F Ghavidel ◽  
MM Zarshenas ◽  
A Sakhteman ◽  
A Gholami ◽  
Y Ghasemi ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oils ◽  
Extraction Methods ◽  
Composition Profile ◽  
Pharmacological Activities

FRACTIONATION AND ANALYSIS OF MONKEY PITUITARY GLANDS FOR POSTERIOR LOBE HORMONES

1962 ◽  
Vol 40 (2) ◽  
pp. 283-289 ◽  
Author(s):  
Darrell N. Ward ◽  
Earl F. Walborg ◽  
Harry S. Lipscomb ◽  
Roger Guillemin
Keyword(s):  
Amino Acid ◽  
Current Distribution ◽  
Arginine Vasopressin ◽  
Specific Activity ◽  
Small Scale ◽  
Posterior Lobe ◽  
Pharmacological Activities ◽  
Pituitary Glands ◽  
Counter Current ◽  
Counter Current Distribution

ABSTRACT Fractionation of monkey pituitary glands gave an oxytocin fraction in low yield which showed a counter-current distribution coefficient equivalent to that obtained with oxytocin from other species. Fractionation and chromatography of monkey vasopressin on carboxymethyl cellulose gave arginine-vasopressin of 60% purity, based on amino acid analysis and specific activity. Counter-current distribution on a small scale gave arginine-vasopressin of 89% purity. Reports by others that monkey pituitary glands contain arginine-vasopressin, based on pharmacological activities, are substantiated by the chemical data presented here.

Antipyretic Activity of the Root Extracts of Xylocarpus

2019 ◽  
Vol 9 (3) ◽  
pp. 35-38
Author(s):  
Ganesh Kumar Y ◽  
Pranitha D ◽  
Phaneendra D ◽  
Madhava Reddy Ch
Keyword(s):  
Mechanisms Of Action ◽  
Prostaglandin Synthesis ◽  
The Body ◽  
Human Race ◽  
Pharmacological Activities ◽  
Standard Drug ◽  
Root Extracts ◽  
Antipyretic Activity ◽  
Inhibition Of Prostaglandin Synthesis ◽  
Elevated Body Temperature

Various types of conditions exist in the body that causes fever and pain. Drugs that are used to treat fever are called antipyretics, and those are usually prescribed to treat elevated body temperature. But those drugs result in many other side effects like ulcers, perforations, bleedings and obstructions, which make their use questionable and limiting. Medicinal plants are used in the treatment of diseases from the starting of the human race and the process; they had been subjected to rigorous investigations and tests to establish a scientific proof and validation of the various pharmacological activities and their respective mechanisms of action in treating the herbs. Considering the anti-inflammatory properties of the plant, Xylocarpus mekongesis was investigated for its antipyretic activity in yeast method and 3doses out of which 00mg/kg body weight showed a better activity compared to the standard drug and other extracts too. The mechanism of action was similar to the paracetamol action that is inhibition of prostaglandin synthesis.

A REVIEW ON RECENT ADVANCES IN CHEMISTRY, SYNTHESIS AND BIOLOGICAL APPLICATIONS OF ISATIN DERIVATIVES

2018 ◽  
pp. 16-22
Author(s):  
Shukla PK ◽  
Singh MP ◽  
Patel R
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Biological Applications ◽  
Plant Origin ◽  
Recent Past ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Biological Aspects ◽  
Isatin Derivatives

Indole and its derivatives have engaged a unique place in the chemistry of nitrogen heterocyclic compounds. The recognition of the plant growthhormone, heteroauxin, the significant amino acids, tryptamine & tryptophan and anti-inflammatory drug, indomethacine are the imperativederivatives of indole which have added stimulus to this review work. Isatin (1H-indole-2,3-dione), an indole derivative of plant origin. Althoughit is a naturally occurring compound, but was synthesized by Erdmann and Laurent in 1840 before it was found in nature. Isatin is a versatileprecursor for many biologically active molecules and its diversified nature makes it a versatile substrate for further modifications. It is concernedin many pharmacological activities like anti-malarial, antiviral, anti-allergic, antimicrobial etc; isatin and its derivatives have been also found todemonstrate promising outcomes against various cancer cell lines. This review provides a brief overview on the recent advances and futureperspectives on chemistry and biological aspects of isatin and its derivatives reported in the recent past.

Privileged Structures in the Design of Potential Drug Candidates for Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4323-4354 ◽  
Author(s):  
Ana Cristina Lima Leite ◽  
José Wanderlan Pontes Espíndola ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
Gevanio Bezerra de Oliveira Filho
Keyword(s):  
Biologically Active ◽  
Neglected Diseases ◽  
Financial Return ◽  
Drug Candidates ◽  
Lead Compounds ◽  
Wide Range ◽  
Methods Of Synthesis ◽  
Current Therapies ◽  
Resistant Strains ◽  
Privileged Structures

Background: Privileged motifs are recurring in a wide range of biologically active compounds that reach different pharmaceutical targets and pathways and could represent a suitable start point to access potential candidates in the neglected diseases field. The current therapies to treat these diseases are based in drugs that lack of the desired effectiveness, affordable methods of synthesis and allow a way to emergence of resistant strains. Due the lack of financial return, only few pharmaceutical companies have been investing in research for new therapeutics for neglected diseases (ND). Methods: Based on the literature search from 2002 to 2016, we discuss how six privileged motifs, focusing phthalimide, isatin, indole, thiosemicarbazone, thiazole, and thiazolidinone are particularly recurrent in compounds active against some of neglected diseases. Results: It was observed that attention was paid particularly for Chagas disease, malaria, tuberculosis, schistosomiasis, leishmaniasis, dengue, African sleeping sickness (Human African Trypanosomiasis - HAT) and toxoplasmosis. It was possible to verify that, among the ND, antitrypanosomal and antiplasmodial activities were between the most searched. Besides, thiosemicarbazone moiety seems to be the most versatile and frequently explored scaffold. As well, phthalimide, isatin, thiazole, and thiazolidone nucleus have been also explored in the ND field. Conclusion: Some described compounds, appear to be promising drug candidates, while others could represent a valuable inspiration in the research for new lead compounds.

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.

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