Oxadiazole-An Important Bioactive Scaffold for Drug Discovery and Development Process Against HIV and Cancer- A Review

2019 ◽  
Vol 15 (3) ◽  
pp. 271-279 ◽  
Author(s):  
Davinder Kumar ◽  
Virender Kumar ◽  
Rakesh Marwaha ◽  
Gajendra Singh

Background: Acquired immunodeficiency syndrome (AIDS) and cancer treatment have been a major task for research scientists and pharmaceutical industry for the last many years. Seeking to the development, many promising chemical entities especially five-membered heterocyclic rings like oxadiazole have revealed good anticancer and anti HIV activities. The current review enlists some recently developed anti-HIV and anti-cancer oxadiazole moieties. Methods: on the basis of structural modification for the syntheses of new oxadiazole analogs, the new anti-HIV and anti-cancer agents have been summarized, which can improve treatment of AIDs and cancer. Results: The oxadiazole ring is more potent in comparison to some other heterocyclic rings (five and six membered) towards anti-HIV and anti-cancer activities. The important mechanisms involved for anti HIV and anticancer activity are mainly inhibition of enzymes like protease, HIV-integrase, telomerase, histone deacetylase, methionine amino peptidase, thymidylate synthase and focal adhesion kinase and inhibition of some growth factors. Conclusion: By reviving the past literature about 50 most potent oxadiazole derivatives, depending upon activity and structural modifications, have been selected as potent anti-HIV, and anti-cancer agents. Thus, oxadiazole seems to be a ‘privileged structure’ for further screening and syntheses of the new drug analogs against life threatening HIV and cancer like diseases.

2016 ◽  
Vol 88 (11) ◽  
pp. 4-11 ◽  
Author(s):  
V V Pokrovsky

In 2015, the infection caused by human immunodeficiency virus (HIV) (HIV infection) dominated among life-threatening infections in Russians: it was first diagnosed in 98,177 Russians and 15,530 citizens of the Russian Federation died from HIV/AIDS, amounting to 45% of all deaths from infectious diseases in Russia. By the mid-2016, there were a total of 1,062,476 identified HIV-positive Russians, of whom 225,992 people died. The estimated number of HIV-infected patients in Russia approximated to 1% of the population, the highest prevalence of HIV being found in the age group of 30—40 years. The most active and expensive measures against HIV/AIDS in Russia are to examine the population for anti-HIV antibodies (29 million screenings per year) and to use in HIV-positive people antiretroviral therapy that was free of charge to more than 200,000 patients, i.e. nearly 25% of the registered Russians living with the HIV-infected. However, treatment coverage and quality are far from the target indicators that the international experts consider needed to reduce HIV prevalence and mortality. A wider program on HIV/AIDS, which includes a number of preventive measures with proven efficiency, as well as a program of promising researches and developments should be introduced in Russia.


2021 ◽  
Vol 9 ◽  
pp. 232470962110146
Author(s):  
Roopam Jariwal ◽  
Nadia Raza ◽  
Janpreet Bhandohal ◽  
Everardo Cobos

Plasmablastic lymphoma (PBL) is a subtype of non-Hodgkin’s lymphoma that manifests in patients with the diagnosis of human immunodeficiency virus (HIV), more prominently in the head, neck, and oral mucosal region. The diagnosis of this rare lymphoma serves as a concomitant diagnosis of acquired immunodeficiency syndrome. The case is of a 33-year-old previously healthy male, with an unknown diagnosis of HIV with a painful right mandibular mass. He was subsequently diagnosed with PBL and HIV. This case of PBL illustrates the importance of linking a rare and potentially life-threatening diagnosis as a possible first manifestation of HIV.


2010 ◽  
Vol 50 (3) ◽  
pp. 154-155
Author(s):  
B L Meel

Traditional healers contribute significantly to the level of health-care systems in Africa. They could play an important role in the prevention and care of patients with human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS) in the community. The traditional healing system deals with psychosocial stress associated with HIV/AIDS as well as herbal medications. Sometimes, herbal medicine causes serious life-threatening complications. Two case reports are presented in this article. The first is a 48-year-old woman with HIV who was made to drink a large volume of a herbal decoction to stimulate vomiting in the belief that cleansing the bowel would rid the system of the disease. The second is a 25-year-old young man who had a herbal enema, which resulted in gangrene of the large bowel. The case histories, mechanism of action and causes of death are discussed.


2021 ◽  
Vol 14 (9) ◽  
pp. 893
Author(s):  
Maria da Conceição Avelino Dias Bianco ◽  
Debora Inacio Leite Firmino Marinho ◽  
Lucas Villas Boas Hoelz ◽  
Monica Macedo Bastos ◽  
Nubia Boechat

Acquired immunodeficiency syndrome (AIDS) is caused by human immunodeficiency virus (HIV) and remains a global health problem four decades after the report of its first case. Despite success in viral load suppression and the increase in patient survival due to combined antiretroviral therapy (cART), the development of new drugs has become imperative due to strains that have become resistant to antiretrovirals. In this context, there has been a continuous search for new anti-HIV agents based on several chemical scaffolds, including nitrogenated heterocyclic pyrrole rings, which have been included in several compounds with antiretroviral activity. Thus, this review aims to describe pyrrole-based compounds with anti-HIV activity as a new potential treatment against AIDS, covering the period between 2015 and 2020. Our research allowed us to conclude that pyrrole derivatives are still worth exploring, as they may provide highly active compounds targeting different steps of the HIV-1 replication cycle and act with an innovative mechanism.


1988 ◽  
Vol 34 (12) ◽  
pp. 2574-2576
Author(s):  
C M Huang ◽  
M Ruddel ◽  
R J Elin

Abstract We determined the enzyme activities of glucose-6-phosphate isomerase, alanine aminotransferase, aspartate aminotransferase, and lactate dehydrogenase in serum from 23 normal controls, 27 anti-HIV seropositive individuals confirmed by Western blot, and 53 patients with acquired immunodeficiency syndrome (AIDS). There is a significant difference for all four enzyme activities among controls, HIV seropositive individuals, and patients with AIDS, the enzyme activities showing a progressive increase as the disease progresses. Evidently these enzyme measurements may be adjunctive biochemical markers for progression of AIDS.


2009 ◽  
Vol 20 (8) ◽  
pp. 582-584 ◽  
Author(s):  
S Shushan ◽  
U Cinamon ◽  
D Levy ◽  
M Sokolov ◽  
Y Roth

With improved survival, more AIDS patients, especially heavy smokers and alcohol abusers, may be confronted with laryngeal squamous cell carcinoma. Since curative treatment may require aggressive combined therapy, these patients, often suffering from immunosupression and poor general condition, present unique therapeutic challenges. The objective of the study was to describe treatment dilemmas. This case report presents a detailed description of an AIDS patient with carcinoma of the larynx. A patient with T3N0M0 laryngeal carcinoma and AIDS underwent tracheotomy and biopsy, followed by severe neck and pulmonary infection. After convalescence, radiotherapy was administered, with no evidence of a disease during a 3.5-year follow-up. During his remaining life, the patient developed severe psychoaffective disorder, his immune state deteriorated until he demised from sepsis. In conclusion, patients with HIV infection, especially having a history of tobacco or alcohol abuse, should be carefully examined for head and neck carcinoma that is likely to be more aggressive. Following surgery, AIDS patients may have worse wound healing and a greater tendency to contract infections. Radiotherapy and especially chemotherapy may cause life-threatening complications. Although early detection may increase survival, curative treatment should involve many disciplines and extra caution.


2019 ◽  
Vol 7 ◽  
pp. 232470961988369
Author(s):  
Precious Macauley ◽  
Mohammad Abu-Hishmeh ◽  
Carissa Dumancas ◽  
Vijay Alexander-Rajan ◽  
Fernando Piedra-Chavez ◽  
...  

Hemophagocytic lymphohistiocytosis (HLH) is a rare and life-threatening condition characterized by widespread inflammation due to massive immune activation and cytokine release. It is of 2 types, primary or familial and secondary or acquired. Diagnosis is made by fulfilling 5 of 8 criteria as determined by the Histiocyte Society. Treatment includes etoposide, dexamethasone, with or without intrathecal methotrexate in the presence of neurologic involvement as well as treating the underlying cause in secondary HLH. We present a case of a 23-year-old female with congenital human immunodeficiency virus (HIV) infection who presents with nonspecific signs and symptoms of cough, fever, leukopenia, and anemia, and a high-serum parvovirus B19 DNA, later diagnosed with HLH and treated with etoposide and dexamethasone. She made clinical improvements and was successfully discharged to home after 26 days of admission.


2020 ◽  
Vol 66 (2) ◽  
pp. 34-43
Author(s):  
Mohamed Amin El-Ansari ◽  
Lamyaa Fawzy Ibrahim ◽  
Mohamed Sharaf

Summary Acquired immunodeficiency syndrome (AIDS) is an immunosuppressive disease caused by human immunodeficiency virus (HIV). The urgent need for searching novel anti-HIV/AIDS medicines is a global concern. So far, a lot of medicinal and aromatic plants (MAPs) have been analyzed to select those that could assist in the prevention and/or amelioration of the disease. Among biologically active compounds present in these plants, one of the most promising group are phenolics. The purpose of this article was to report anti-HIV activity of selected phenolic compounds of plant origin.


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