scholarly journals Synthetic Transformations and Medicinal Significance of 1,2,3-Thiadiazoles Derivatives: An Update

2021 ◽  
Vol 11 (12) ◽  
pp. 5742
Author(s):  
Ali Irfan ◽  
Sami Ullah ◽  
Ayesha Anum ◽  
Nazish Jabeen ◽  
Ameer Fawad Zahoor ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Review Article ◽  
Present Review ◽  
Hybrid Structures ◽  
Activity Relationship ◽  
Pharmacological Activities ◽  
Structure Activity ◽  
Synthetic Transformations

The 1,2,3-thiadiazole moiety occupies a significant and prominent position among privileged heterocyclic templates in the field of medicine, pharmacology and pharmaceutics due to its broad spectrum of biological activities. The 1,2,3-thiadiazole hybrid structures showed myriad biomedical activities such as antifungal, antiviral, insecticidal, antiamoebic, anticancer and plant activators, etc. In the present review, various synthetic transformations and approaches are highlighted to furnish 1,2,3-thiadiazole scaffolds along with different pharmaceutical and pharmacological activities by virtue of the presence of the 1,2,3-thiadiazole framework on the basis of structure–activity relationship (SAR). The discussion in this review article will attract the attention of synthetic and medicinal researchers to explore 1,2,3-thiadiazole structural motifs for future therapeutic agents.

Steroidal pyrazolines as a promising scaffold in drug discovery

2020 ◽  
Vol 12 (10) ◽  
pp. 949-959
Author(s):  
Ranju Bansal ◽  
Ranjit Singh
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Review Article ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

scholarly journals Recent Advances in the Semisynthesis, Modifications and Biological Activities of Ocotillol-Type Triterpenoids

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5562
Author(s):  
Yucheng Cao ◽  
Kaiyi Wang ◽  
Si Xu ◽  
Lingtan Kong ◽  
Yi Bi ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Pharmacological Activities ◽  
Structure Activity ◽  
Recent Advances ◽  
The World ◽  
Anti Inflammatory ◽  
Active Substances

Ginseng is one of the most widely consumed herbs in the world and plays an important role in counteracting fatigue and alleviating stress. The main active substances of ginseng are its ginsenosides. Ocotillol-type triterpenoid is a remarkably effective ginsenoside from Vietnamese ginseng that has received attention because of its potential antibacterial, anticancer and anti-inflammatory properties, among others. The semisynthesis, modification and biological activities of ocotillol-type compounds have been extensively studied in recent years. The aim of this review is to summarize semisynthesis, modification and pharmacological activities of ocotillol-type compounds. The structure–activity relationship studies of these compounds were reported. This summary should prove useful information for drug exploration of ocotillol-type derivatives.

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

scholarly journals Recent Updates on the Synthesis of Bioactive Quinoxaline-Containing Sulfonamides

2021 ◽  
Vol 11 (12) ◽  
pp. 5702
Author(s):  
Ali Irfan ◽  
Sajjad Ahmad ◽  
Saddam Hussain ◽  
Fozia Batool ◽  
Haseeba Riaz ◽  
...  
Keyword(s):  
Literature Review ◽  
Biomedical Applications ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmacological Activities ◽  
Lead Compounds ◽  
Structure Activity ◽  
Wide Range ◽  
Sulfonamide Group

Quinoxaline is a privileged pharmacophore that has broad-spectrum applications in the fields of medicine, pharmacology and pharmaceutics. Similarly, the sulfonamide moiety is of considerable interest in medicinal chemistry, as it exhibits a wide range of pharmacological activities. Therefore, the therapeutic potential and biomedical applications of quinoxalines have been enhanced by incorporation of the sulfonamide group into their chemical framework. The present review surveyed the literature on the preparation, biological activities and structure-activity relationship (SAR) of quinoxaline sulfonamide derivatives due to their broad range of biomedical activities, such as diuretic, antibacterial, antifungal, neuropharmacological, antileishmanial, anti-inflammatory, anti-tumor and anticancer action. The current biological diagnostic findings in this literature review suggest that quinoxaline-linked sulfonamide hybrids are capable of being established as lead compounds; modifications on quinoxaline sulfonamide derivatives may give rise to advanced therapeutic agents against a wide variety of diseases.

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 Flavonoids from the Genus Euphorbia: Isolation, Structure, Pharmacological Activities and Structure–Activity Relationships

2021 ◽  
Vol 14 (5) ◽  
pp. 428
Author(s):  
Douglas Kemboi Magozwi ◽  
Mmabatho Dinala ◽  
Nthabiseng Mokwana ◽  
Xavier Siwe-Noundou ◽  
Rui W. M. Krause ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Structure Activity Relationship ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Skeletal Structure ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity ◽  
Review Reports

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.

Carbohydrazide analogues: a review of synthesis and biological activities

2021 ◽  
Vol 21 ◽  
Author(s):  
Ebuka Leonard Onyeyilim ◽  
Mercy Amarachi Ezeokonkwo ◽  
David Izuchukwu Ugwu ◽  
Chiamaka Peace Uzoewulu ◽  
Florence Uchenna Eze ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Inorganic Chemistry ◽  
Schiff Bases ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Important Class ◽  
Synthetic Route ◽  
Structure Activity

: Carbohydrazides and their Schiff bases are important class of heterocycles that are not only employed in the area of organic chemistry, but also have tremendous applications in physical and inorganic chemistry. A series of potential bioactive compounds, containing carbohydrazide functionality and their hydrazone derivatives have been synthesized and screened for antibacterial, anticancer, antifungal and anti-inflammatory etc. This brief review discloses some synthetic route to so many reported carbohydrazides, their Schiff bases, their biological activities and their structure activity relationship.

Bioactivities of Natural Catalpol Derivatives

2019 ◽  
Vol 26 (33) ◽  
pp. 6149-6173 ◽  
Author(s):  
Liu-Qiang Zhang ◽  
Kai-Xian Chen ◽  
Yi-Ming Li
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Inhibitory Potency ◽  
Pharmacological Activities ◽  
Chemical Structures ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Extensive Coverage ◽  
Relationship Of

Catalpol, a famous molecule of iridoids, possesses extensive pharmacological activities. Our studies found that compounds with low-polarity substituents at the 6-O position of catalpol exhibited higher NF-κB inhibitory potency than catalpol. However, catalpol derivatives are not much focused. Here this review provides extensive coverage of naturally occurring catalpol derivatives discovered from 1888 until 2018. It covers their distribution, chemotaxonomic significance, chemical structures, and bioactivities from more than 200 peer-reviewed articles, and highlights the structure-activity relationship of catalpol derivatives.

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