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 Biochemistry, Safety, Pharmacological Activities, and Clinical Applications of Turmeric: A Mechanistic Review

2020 ◽  
Vol 2020 ◽  
pp. 1-14 ◽  
Author(s):  
Rabia Shabir Ahmad ◽  
Muhammad Bilal Hussain ◽  
Muhammad Tauseef Sultan ◽  
Muhammad Sajid Arshad ◽  
Marwa Waheed ◽  
...  
Keyword(s):  
Clinical Research ◽  
Biological Activities ◽  
Curcuma Longa ◽  
Clinical Applications ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range ◽  
Different Types ◽  
Safety And Toxicity ◽  
Anti Inflammatory

Turmeric (Curcuma longa L.) is a popular natural drug, traditionally used for the treatment of a wide range of diseases. Its root, as its most popular part used for medicinal purposes, contains different types of phytochemicals and minerals. This review summarizes what is currently known on biochemistry, safety, pharmacological activities (mechanistically), and clinical applications of turmeric. In short, curcumin is considered as the fundamental constituent in ground turmeric rhizome. Turmeric possesses several biological activities including anti-inflammatory, antioxidant, anticancer, antimutagenic, antimicrobial, antiobesity, hypolipidemic, cardioprotective, and neuroprotective effects. These reported pharmacologic activities make turmeric an important option for further clinical research. Also, there is a discussion on its safety and toxicity.

scholarly journals An Updated Review on Synthesis and Biological Activities of Thiosemicarbazide Analogs

2021 ◽  
Vol 33 (9) ◽  
pp. 1957-1975
Author(s):  
Akhalesh Kumar ◽  
Rakhi Mishra ◽  
Avijit Mazumder ◽  
Rupa Mazumder ◽  
Arun Kumar
Keyword(s):  
Drug Discovery ◽  
Review Paper ◽  
Biological Activities ◽  
Reaction Scheme ◽  
Review Article ◽  
Pharmacological Activities ◽  
Thiosemicarbazide Derivative ◽  
Synthetic Methodologies ◽  
Thiosemicarbazide Derivatives

This review paper focuses on the different synthetic methodologies that researchers have adopted to synthesize various thiosemicarbazide derivatives with different biological activities of synthesized compounds in the last 20 years. Most of the investigations available in the literature are directed to the biological activities of thiosemicarbazide derivatives with less discussion on its synthetic schemes. This review article presents various reaction scheme, which has been adopted for thiosemicarbazide derivative synthesis along with the reported pharmacological activities of synthesized analogs. The available literature in the article aims to encourage more studies on the synthesis of thiosemicarbazide derivatives, which will help for drug discovery having thiosemicarbazide nucleus.

scholarly journals A review on Indole and Benzothiazole derivatives its importance

2019 ◽  
Vol 9 (1-s) ◽  
pp. 505-509 ◽  
Author(s):  
Shaheen Sulthana ◽  
P. Pandian
Keyword(s):  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Biological Activities ◽  
New Product ◽  
Review Article ◽  
Literature Survey ◽  
Pharmacological Activities ◽  
Benzothiazole Derivatives ◽  
Wide Range ◽  
Anti Inflammatory

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range of biological and pharmacological activities such as antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer. This review article literature survey summarizes the synthesis and pharmacological activities of Indole, Benzothiazole and its derivatives. Keywords: Indole, Benzothiazole, antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer

scholarly journals Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives.

2017 ◽  
Vol 10 (7) ◽  
pp. 38 ◽  
Author(s):  
Sunny Jalhan
Keyword(s):  
Biological Activities ◽  
Biochemical Properties ◽  
Review Article ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Methylene Groups ◽  
Anti Oxidant ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological, therapeutic and biochemical properties depend upon their pattern of substitution. Coumarins exhibit a wide range of pharmacological activities, which includes anti-diabetic, anti-viral, anti-microbial, anticancer, anti-oxidant, anti-parasitic, anti-helminthic, anti-proliferative, anti-convulsant, anti-inflammatory and antihypertensive activities. 1,3,4-Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. It is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogens (-N=). There are three known isomers: 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5- oxadiazole. Oxadiazole moiety shows antimicrobial, anticancer and anti-inflammatory activity and suitably substituted 1,3,4-oxadiazole having biological activities like antimicrobial, anticancer and other biological activities.

scholarly journals Bunium persicum: A Review of Ethnopharmacology, Phytochemistry, and Biological Activities

2020 ◽  
Author(s):  
Zahra Majidi ◽  
Fatemeh Bina ◽  
Niloofar Kahkeshani ◽  
Roja Rahimi
Keyword(s):  
Biological Activities ◽  
Chemical Constituents ◽  
Antimicrobial Activities ◽  
Modern Medicine ◽  
Pharmacological Activities ◽  
Bunium Persicum ◽  
Comprehensive Information ◽  
Wide Range ◽  
Coa Reductase ◽  
Biological And Pharmacological Activities

Bunium persicum (Boiss) B. Fedtsh (Apiaceae, Persian name: Zireh Kermani) has been used to treat various diseases in traditional and folkloric medicine including gastrointestinal, respiratory, nasopharyngeal, cardiac, ocular, neurological, rheumatological and urinary tract diseases. Its essential oil contains different monoterpenes, sesquiterpenes and phenyl propenes. Other chemical constituents identified in B. persicum are phenolic compounds, fatty acids, carboxylic acids, and carbohydrates. Wide range of biological and pharmacological activities including antioxidant, analgesic, anti-inflammatory, acetylcholinesterase inhibitory, anticonvulsant, HMG-CoA reductase inhibitory, anti-pancreatic lipase, anticancer, antidiabetic, antihistamine, antidiarrheal, antispasmodic, antihematoxic, antityrosinase and antimicrobial activities have been reported from this plant in modern medicine. This article summarizes comprehensive information attributing traditional uses, phytochemistry, and pharmacological activities of Zireh Kermani.

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.

scholarly journals A REVIEW ON THERAPEUTIC POTENTIAL OF HETEROCYCLIC PYRIMIDINE DERIVATIVES AS POTENT ANTIVIRAL AGENTS

2020 ◽  
pp. 30-34
Author(s):  
SAGMA EG ◽  
BASKAR LAKSHMANAN
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Antiviral Agents ◽  
Viral Disease ◽  
Review Article ◽  
Pharmacological Activities ◽  
Therapeutic Uses ◽  
Wide Range ◽  
Derivatives Of ◽  
Anti Hiv

Pyrimidine nucleus exhibited remarkable pharmacological activities. The review of an article indicates that the compounds having pyrimidine nucleus have a wide range of therapeutic uses that include antiviral, anti-inflammatory, antibacterial, anticancer, antiviral, anti-HIV, antihypertensive, sedatives and hypnotics, anticonvulsant, and antihistaminic. This review article is intended to describe the antiviral activity of a compound containing the pyrimidine nucleus. The chemistry of pyrimidine is a thriving field for the study of their pharmacological uses. Numerous methods for the synthesis of pyrimidine as also their diverse reactions offer enormous scope in the field of medicinal chemistry. The review article aims to reveal the work reported on the antiviral synthetic pyrimidine compound and the chemistry and biological activities of pyrimidine during the past few decades. During this review article, we are mainly focusing the viral activities in different derivatives of pyrimidine nucleus. Therefore, we are going to discuss some important issues such as the good ideas to resist our increasing viral disease and the importance of a pyrimidine nucleus in the viral drugs. Hence, these are the main things we are going to discuss in this article.

1,8-naphthyridine derivatives: an updated review on recent advancements of their myriad biological activities

2021 ◽  
Author(s):  
Shivani Mithula ◽  
Adinarayana Nandikolla ◽  
Sankaranarayanan Murugesan ◽  
Venkata GCS Kondapalli
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
The Past ◽  
Anti Hiv ◽  
Past Half ◽  
Half Decade

Among all nitrogen-containing heterocycles, the 1,8-naphthyridine scaffold has recently gained an immense amount of curiosity from numerous researchers across fields of medicinal chemistry and drug discovery. This new attention can be ascribed to its versatility of synthesis, its reactiveness and the variety of biological activities it has exhibited. Over the past half-decade, numerous diverse biological evaluations have been conducted on 1,8-naphthyridine and its derivatives in a quest to unravel novel pharmacological facets to this scaffold. Its potency to treat neurodegenerative and immunomodulatory disorders, along with its anti-HIV, antidepressant and antioxidant properties, has enticed researchers to look beyond its broad-spectrum activities, providing further scope for exploration. This review is a consolidated update of previous works on 1,8-naphthyridines and their analogs, focusing on the past 5 years.

scholarly journals Advances in Studies on the Pharmacological Activities of Fucoxanthin

Marine Drugs ◽  
2020 ◽  
Vol 18 (12) ◽  
pp. 634
Author(s):  
Han Xiao ◽  
Jiarui Zhao ◽  
Chang Fang ◽  
Qi Cao ◽  
Maochen Xing ◽  
...  
Keyword(s):  
Biological Activities ◽  
Intestinal Flora ◽  
Small Molecular Weight ◽  
Pharmacological Activities ◽  
Beneficial Effects ◽  
Wide Range ◽  
Cell Components ◽  
Underlying Mechanisms ◽  
Organ Fibrosis ◽  
Active Can

Fucoxanthin is a natural carotenoid derived mostly from many species of marine brown algae. It is characterized by small molecular weight, is chemically active, can be easily oxidized, and has diverse biological activities, thus protecting cell components from ROS. Fucoxanthin inhibits the proliferation of a variety of cancer cells, promotes weight loss, acts as an antioxidant and anti-inflammatory agent, interacts with the intestinal flora to protect intestinal health, prevents organ fibrosis, and exerts a multitude of other beneficial effects. Thus, fucoxanthin has a wide range of applications and broad prospects. This review focuses primarily on the latest progress in research on its pharmacological activity and underlying mechanisms.

scholarly journals Molecular Targets Involved in the Neuroprotection Mediated by Terpenoids

Planta Medica ◽  
2019 ◽  
Vol 85 (17) ◽  
pp. 1304-1315 ◽  
Author(s):  
Laura González-Cofrade ◽  
Beatriz de las Heras ◽  
Luis Apaza Ticona ◽  
Olga M. Palomino
Keyword(s):  
Therapeutic Potential ◽  
Cell Damage ◽  
Biological Activities ◽  
Neuronal Cell ◽  
Molecular Targets ◽  
Research Activity ◽  
Neuroprotective Effects ◽  
Therapeutic Value ◽  
Wide Range ◽  
Drug Leads

AbstractNatural products and their derivatives represent the most consistently successful source of drug leads. Terpenoids, a structurally diverse group, are secondary metabolites widely distributed in nature, endowed with a wide range of biological activities such as antibacterial, anti-inflammatory, antitumoral, or neuroprotective effects, which consolidate their therapeutic value. During the last decades, and taking into consideration the prevalence of aging-related diseases, research activity into the neuroprotective effects of these types of compounds has increased enormously. Several signaling pathways involved in neuroprotection are targets of their mechanism of action and mediate their pleiotropic protective activity in neuronal cell damage. In the present review, molecular basis of the neuroprotection exerted by terpenoids is presented, focusing on preclinical evidence of the therapeutic potential of diterpenoids and triterpenoids on neurodegenerative disorders. By acting on diverse mechanisms simultaneously, terpenoids have been emphasized as promising multitarget agents.

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