Pyrazole Containing Anti-HIV Agents: An Update

2022 ◽  
Vol 18 ◽  
Author(s):  
Sanjay Kumar ◽  
Shiv Gupta ◽  
Varsha Rani ◽  
Priyanka Sharma

Background: Pyrazole scaffolds have gained importance in drug discovery and development for various pharmacological activities like antiviral, antifungal, anticancer, antidepressant, anti-inflammatory, antibacterial, etc. Additionally, the pyrazole moiety has shown potent anti-HIV activity as a core heterocycle or substituted heterocycles derivatives (mono, di, tri, tetra, and fused pyrazole derivatives). To assist the development of further potential anti-HIV agents containing pyrazole nucleus, here we have summarized pyrazole containing anti-HIV compounds that have been reported by researchers all over the world for the last two decades. Objective: The present review concentrates on an assortment of pyrazole containing compounds, particularly for potential therapeutic activity against HIV. Methods: Google Scholar, Pubmed, and SciFinder were searched databases with ‘‘pyrazol’’ keywords. Further, the year of publication and keywords ‘‘Anti-HIV’’ filter was applied to obtain relevant reported literature for anti-HIV agents containing pyrazole as a core or substituted derivatives. Results: This review article has shown the comprehensive compilation of 220 compounds containing pyrazole nucleus and possessing anti-HIV activity by sorting approximately 40 research articles from 2001 to date. 1-(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-(1H-pyrazol-3-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (13), 3-(3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-fluoro-1H-pyrrolo[2,3-c]pyridin-7-yl)-1H-pyrazole-5-carboxamide (31), 3-(3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-fluoro-1H-pyrrolo[2,3-c]pyridin-7-yl)-1H-pyrazole-5-carboxamide (88), 3-cyanophenoxypyrazole derivative (130), and 4-(4-chlorophenyl)-5-(4-methyl-5-((4-nitrophenyl)diazenyl)thiazol-2-yl)-3-phenyl-5,6-dihydro-4H-pyrazolo[4,3-d]isoxazole (178) were the most potent mono-, di-, tri-, tetra-substituted, and fused pyrazole derivatives, respectively, which have shown potent anti-HIV activity among all the described derivatives as compared with standard anti-HIV drugs. Conclusion: This review article provides an overview of the potential therapeutic activity of pyrazole derivatives against HIV that will be helpful for designing pyrazole containing compounds for anti-HIV activity.

2016 ◽  
Author(s):  
Shao-Xing Dai ◽  
Huan Chen ◽  
Wen-Xing Li ◽  
Yi-Cheng Guo ◽  
Jia-Qian Liu ◽  
...  

AbstractDevelopment of new, effective and affordable drugs against HIV is urgently needed. In this study, we developed a world’s first web server called Anti-HIV-Predictor (http://bsb.kiz.ac.cn:70/hivpre) for predicting anti-HIV activity of given compounds. This server is rapid and accurate (accuracy >93% and AUC > 0.958). We applied the server to screen 1835 approved drugs for anti-HIV therapy. Totally 67 drugs were predicted to have anti-HIV activity, 25 of which are anti-HIV drugs. Then we experimentally evaluated 35 predicted new anti-HIV compounds by assays of syncytia formation, p24 quantification, cytotoxicity. Finally, we repurposed 7 approved drugs (cetrorelix, dalbavancin, daunorubicin, doxorubicin, epirubicin, idarubicin and valrubicin) as new anti-HIV agents. The original indication of these drugs is involved in a variety of diseases such as female infertility and cancer. Anti-HIV-Predictor and the 7 repurposed anti-HIV agents provided here demonstrate the efficacy of this strategy for discovery of new anti-HIV agents.


Author(s):  
Bhuwanendra Singh ◽  
Jitendra Gupta ◽  
Rohit Mohan ◽  
Reena Gupta ◽  
Kanchan Pal

The current review article is based on the facts to reveal the biological potentials of the genus ledum, and specie palustre. Although in the article all the species are well described with their distribution in all over the world and their pharmacological activities are also discussed. Rhododendron tomantosum is also known as Marsh Tea or northern Labrador tea, which is an evergreen shrub having the height of about 40 cm and the plant has about ten species in all over the world. Article has very informative aspect regarding Hypouricemic Significance of Ledum palustre (L. palustre), its chemical compounds extracted and analyzed by different spectroscopic and chromatographic techniques to report the active principles from the oil of the Rhododendron tomantosum fresh leaves. The main active compounds were found are given as (41.0–43.4%) ledol (23.3–26.7%) and ascaridole (15.1–4.5%). L. palustre has a very significant role in the gout and arthritis occurs due the presence of high amount of uric acid in the blood plasma. Various dosage forms are mentioned in the review article to explore the potentials of the drug. Hence according to literature if L. palustre is significantly capable to reduce the high level of the uric acid if give in the potency if 30 c (diluted 30 times)) and 1 M ((1000 dilutions) to the patients, and may be a good alternative to the allopurinol. So, this drug is frequently used in the homeopathic system of medicine to get the hypouricemic significance in the human beings.


Author(s):  
Qingtai Chen ◽  
Chongchong Wu ◽  
Jinjin Zhu ◽  
Enzhong Li ◽  
Zhi Xu

: Acquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus (HIV), is one of the leading causes of human deaths. The advent of different anti-HIV drugs over different disease progress has made AIDS/HIV from a deadly infection to chronic and manageable disease. However, the development of multidrug-resistant viruses, together with the severe side effects of anti-HIV agents, compromised their efficacy and limited the treatment options. Indoles, the most common frameworks in the bioactive molecules, represent attractive scaffolds for the design and development of novel drugs. Indole derivatives are potential inhibitors of HIV enzymes such as reverse transcriptase, integrase and protease, and some indole-based agents like Delavirdine have already been applied in clinics or under clinical evaluations for the treatment of AIDS/HIV, revealing that indole moiety is a useful template for the development of anti-HIV agents. This review focuses on the recent advancement of indole derivatives including indole alkaloids, hybrids, and dimers with anti-HIV potential, covering articles published between 2010 and 2020. The chemical structures, structure-activity relationship and mechanisms of action are also discussed.


2019 ◽  
Vol 18 (31) ◽  
pp. 2664-2680 ◽  
Author(s):  
Maninder Kaur ◽  
Ravindra K. Rawal ◽  
Goutam Rath ◽  
Amit K. Goyal

HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells. It has emerged as a potential target for developing anti-HIV agents. In the last two decades, a number of integrase inhibitors have been developed as potential anti-HIV therapeutics. Several integrase inhibitors have reached later stages of clinical trials including S-1360, L870,810, L870,812 and BMS-707035. Into the bargain, Raltegravir, Elvitegravir and Dolutegravir have been approved by FDA as anti-HIV agents. This review article summarizes the structural insights required for the inhibition of the HIV1 integrase in the context of clinically relevant HIV1 integrase inhibitors. Additionally, the structural features required for overcoming HIV resistance have been discussed. These insights will update the ongoing design of novel antiviral inhibitors.


2021 ◽  
Author(s):  
Duygu Koyuncu Irmak ◽  
Erdal Karaoz

In the pandemic of COVID-19, while living normals have been changing, there have been a huge effort globally to find out effective and safe treatment agents and vaccines. As of now, the advances show the progress in vaccine development, however the treatment of the COVID-19 is yet not fully specified. The drugs, i.e. antibiotics, antivirals, antimalarians, even anti-HIV agents which have been known already were taken out of the shelves and brought into use in different combinations. On the other hand, the cellular treatment, more specifically the mesenchymal stem cell therapy has been encouraged, resulting in various evidence published all over the world. This chapter aims to compile the published information, in means of methods, disease manifestations, results and limitations, about the stem cell treatment of the COVID-19 and to provide a source of harmonized reference for scientific society.


Author(s):  
Pragya Nigam ◽  
Bina Gidwani ◽  
Hemant Kumar Dhongde ◽  
Anshita Gupta ◽  
Chanchal Deep Kaur

The Cucurbitaceae family consists of about 735 species. The present study includes detailed aspects of species of Lagenaria siceraria(Mol.) Standley is a medicinal plant. The plant mainly contains carbohydrates, protein, fats and amino acids. The active constituent of Lagenaria is cucurbitacin, lagenin and various mineral matters. In most of the countries lagenaria has been used as antioxidant, cardiotonic, liver tonic, anti-inflammatory, diuretic, antihepatotoxic, antitumor, anti HIV, anti proliferative agent. Thus, lagenaria posses broad spectrum of pharmacological activities. Moreover, the entire plant and its parts like fruit, fruit pulp, seeds, epicarp etc. shows medicinally important properties. This review article focuses on the pharmacognostic, phytochemistry and pharmacological profile of Lagenaria.


2021 ◽  
Vol 10 (5) ◽  
pp. 338-344
Author(s):  
Manish Grover ◽  

Areca catechu belongs to the family Palmae and is commonly known by different names such as chikni supari, areca nut and betel nut. The fruit of this plant is called the areca nut, which carries significant medicinal properties. This plant is also mentioned in various ancient Sanskrit scriptures. The plant is mainly used for chewing and religious purposes of the Hindus of India. India is the largest consumer and producer of areca nut globally, which produces about 52% of the world production. Medicinally, the plant is used to treat leucoderma, diarrhea, anaemia, obesity, leprosy etc. In Ayurveda, the plant is astringent, diuretic, digestion-promoting, stimulant, wound healing and laxative agent. The plant is associated with various therapeutic and pharmacological potentials, including wound healing, antidepressant, antihelmintic, antihypertensive, antioxidant, antiallergic, antifungal and antimicrobial properties. However, this plant is considered as carcinogenic as it can cause mouth cancer. In this review article, attempts have been made to summarize the phytochemistry, folk uses and ayurvedic uses along with its pharmacological activities


Author(s):  
Monica Dinodia

Abstract: Nitrogen based heterocycles display an impressive repertoire of biological activities, including antioxidant, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, anti-viral, anti-HIV, anti-cancer, anti-helminthic, and other pharmacological activities. Numerous novel nitrogen-based heterocycles have been synthesized, which showed various physiological properties, and their application in medicinal chemistry is ever-growing. The present review will provide an in-depth view of N-heterocyclic compounds that showed biological activities in the last 5 years (2017-2021). This review article will be helpful for the structural design of effective and sustainable N-heterocyclic drugs against diseases with minimal side effects.


Author(s):  
Saabiya Farooqui ◽  
Tulika Tyagi

Nerium oleander is an important medicinal plant in Indian folk medicine. It is a potentially lethal plant in many cases and poisoning is reported in tropical and subtropical parts of the world as well as a number of suicidal cases are also prevalent in South Asian countries, especially in India and Sri Lanka. All parts of the plant are toxic and contain a variety of cardiac glycosides which includes neriin, oleandrin, cardenolides, gentiobiosyl and odoroside. This plant species also produce secondary metabolites such as alkaloids, flavonoids and steroids which have pharmacological applications. The important pharmacological activities are antibacterial, anthelmintic, anti-inflammatory, hepatoprotective, immunopotential, anti-pyretic, antioxidant, antifungal, anticancer and anti-HIV activity. This review describes the evidence-based information regarding pharmacological activity as well as phytochemicals of this plant.


Author(s):  
SAGMA EG ◽  
BASKAR LAKSHMANAN

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.


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