An Updated and Focused Review on Heterocyclic Inhibitors for SARS-CoV and SARS-CoV-2 3CLpro.

BACKGROUND: SARS-CoV and SARS-CoV-2 are extremely infective and frequently cause severe respiratory issues (acute respiratory syndrome). These emerging viruses represent huge challenges to worldwide health. Reliable and systematic examination of SARS-CoV and COVID-19 will assist in identifying infectious persons accurately. Based on the biological, chemical, and genetic link of SARS CoV-2 towards SARS-CoV, the recurrence of different anti-SARS-CoV natural drug molecules may be beneficial in the advancement of anti COVID-19 herbal drug molecules. Here, we reviewed published literature on SAR, and molecular docking study of previously synthesized derivatives, which targeted SARS-CoV along with future prospects on SARS-CoV-2 have been reviewed. This study would assist researchers in developing newer/novel potential molecules that would target SAR-CoV-2. OBJECTIVES: The review highlights the inhibition potential of heterocyclic inhibitors for SARS-CoV and SARS-CoV-2. The structure-activity relationship of potential compounds has been discussed. EVIDENCE ACQUISITION: We carried out a thorough literature assessment employing electronic databases for scientific articles highlighting potential heterocyclic inhibitors for SARS-CoV and SARS-CoV-2, published from 2010 to 2021. We recovered 415 articles, but only 220 were involved and conversed in this manuscript. The article apprehended appropriate research considering three areas: 1) SAR activity, 2) Molecular docking, and 3) Biological activity and future prospects on SARS-CoV-2. METHODS: The potential compounds with good inhibition are discussed, and their inhibition is expressed in terms of IC50. RESULTS: Heterocyclic scaffolds reflected an extensive range of therapeutic activity and may act as an initiating idea for designing and discovering potential inhibitors for SARS-CoV and SARS-CoV-2 treatment. CONCLUSION: The points highlighted here may prove to be a vital tool for medicinal chemists working/investigating more potent and efficacious scaffolds in treating SARS-CoV and SARS-CoV-2.

Discovery, Development, and Patent Trends on Molnupiravir: A Prospective Oral Treatment for COVID-19.

The COVID-19 pandemic needs no introduction at present. Only a few treatments are available for this disease, including remdesivir and favipiravir. Accordingly, the pharmaceutical industry is striving to develop new treatments for COVID-19. Molnupiravir, an orally active RdRp inhibitor, is in a phase 3 clinical trial against COVID-19. The objective of this review article is to enlighten the researchers working on COVID-19 about the discovery, recent developments, and patents related to molnupiravir. Molnupiravir was originally developed for the treatment of influenza at Emory University, USA. However, this drug has also demonstrated activity against a variety of viruses, including SARS-CoV-2. Now it is being jointly developed by Emory University, Ridgeback Biotherapeutics, and Merck to treat COVID-19. The published clinical data indicate a good safety profile, tolerability, and oral bioavailability of molnupiravir in humans. The patient-compliant oral dosage form of molnupiravir may hit the market in the first or second quarter of 2022. The patent data of molnupiravir revealed its granted compound patent and process-related patent applications. We also anticipate patent filing related to oral dosage forms, inhalers, and a combination of molnupiravir with marketed drugs like remdesivir, favipiravir, and baricitinib. The current pandemic demands a patient compliant, safe, tolerable, and orally effective COVID-19 treatment. The authors believe that molnupiravir meets these requirements and is a breakthrough COVID-19 treatment.

Trends in the development of remdesivir based inventions against COVID-19 and other disorders: A patent review.

The development of remdesivir has been a breakthrough for COVID-19 treatment. It has been approved in about 50 countries, including Saudi Arabia, since 2020. The generic structure of remdesivir was first disclosed in 2009. This patent review summarizes the remdesivir based inventions to treat/prevent COVID-19 and other disorders from 2009 to May 16, 2021, emphasizing the patents related to medical and pharmaceutical sciences. The primary patents/patent applications of remdesivir are related to its compositions, new combinations with other therapeutic agents, delivery systems, and new indications. The inventive combinations have displayed synergistic effects against COVID-19, whereas the delivery systems/compositions have improved patient compliance. The inventions related to new indications of remdesivir to treat Ebola, hepatitis, idiopathic pulmonary fibrosis, diabetic nephropathy, and cardiovascular complications enhance its therapeutic area. Many new innovative combinations and delivery systems of remdesivir are anticipated to provide better treatment for COVID-19.

Awareness of COVID-19 among the General Population of the Northern Border Region of Saudi Arabia

The pandemic Coronavirus Disease-19 (COVID-19) is an international apprehension, and there exists no effective treatment for it. Therefore, educating people about the necessary information regarding COVID-19 has become an essential tool to fight against COVID-19. The purpose of this research was to evaluate the awareness of COVID-19 among the general people of the Northern Border Region of Saudi Arabia (NBRSA). A self-administered questionnaire containing basic questions was designed and shared with the people after taking their consent. A total of 249 people participated in this study. The data was collected and analyzed. This study has been revealed that the general public of the NBRSA has a passable knowledge of the specific information about the COVID-19. However, the public is not satisfactorily aware of the complications associated with COVID-19. Accordingly, COVID-19 related education programs should be conducted regularly to increase the awareness of the general public of the NBRSA for COVID-19.