Wang, Tao Kadow, John F. Meanwell, Nicholas A.
Published in
Medicinal Chemistry Research
The discovery and development of fostemsavir ( 2 ), the tromethamine salt of the phosphonooxymethyl prodrug of temsavir ( 1 ), encountered significant challenges at many points in the preclinical and clinical development program that, in many cases, stimulated the implementation of innovative solutions in order to enable further progression. In the...
Sun, Mingna Sun, Mingjiao Zhang, Jianye
Published in
Medicinal Chemistry Research
Osthole, also known as osthol, is a coumarin derivative found in several medicinal plants such as Cnidium monnieri and Angelica pubescens . It can be obtained via extraction and separation from plants or total synthesis. Plenty of experiments have suggested that osthole exhibited multiple biological activities covering antitumor, anti-inflammatory,...
Kousaxidis, Antonios Kovacikova, Lucia Nicolaou, Ioannis Stefek, Milan Geronikaki, Athina
Published in
Medicinal Chemistry Research
Sepsis is a life-threatening disease that affects millions of people worldwide. Microbial infections that lead to sepsis syndrome are associated with an increased production of inflammatory molecules. Aldose reductase has recently emerged as a molecular target that is involved in various inflammatory diseases, including sepsis. Herein, a series of ...
Madikizela, Balungile Eckhardt, Tamira Goddard, Richard Richter, Adrian Lins, Anika Lehmann, Christoph Imming, Peter Seidel, Rüdiger W.
Published in
Medicinal Chemistry Research
8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β- d -ribose-2′-epimerase (DprE1), an enzyme crucial for cell wall synthesis in the pathogen Mycobacterium tuberculosis . Synthesis, structural charact...
Serbian, Immo Prell, Erik Fischer, Claudia Deigner, Hans-Peter Csuk, René
Published in
Medicinal Chemistry Research
A convenient route has been developed for the synthesis of novel 6-amino-2,2-(or 3,3-difluoro)-2-(or 3),6-dideoxy-hexopyranoses. Biological screening showed these compounds as good inhibitors for several glycosidases. Especially n -propyl 6-amino-2,6-dideoxy-2,2-difluoro-β- d -glucopyranoside ( 8 ) was an excellent competitive inhibitor for the β-g...
Escalante, Diego E. Ferguson, David M.
Published in
Medicinal Chemistry Research
The type II transmembrane serine protease TMPRSS2 facilitates the entry of coronaviruses, such as SARS-CoV-2, into host cells by cleaving the S1/S2 interface of the viral spike protein. Based on structural data derived from X-ray crystallographic data of related trypsin-like proteases, a homology model of TMPRSS2 is described and validated using th...
Bakun, Paweł Czarczynska-Goslinska, Beata Goslinski, Tomasz Lijewski, Sebastian
Published in
Medicinal Chemistry Research
Azulene is an aromatic hydrocarbon that possesses a unique chemical structure and interesting biological properties. Azulene derivatives, including guaiazulene or chamazulene, occur in nature as components of many plants and mushrooms, such as Matricaria chamomilla , Artemisia absinthium , Achillea millefolium , and Lactarius indigo . Due to physic...
Spinozzi, Eleonora Baldassarri, Cecilia Acquaticci, Laura Del Bello, Fabio Grifantini, Mario Cappellacci, Loredana Riccardo, Petrelli
Published in
Medicinal Chemistry Research
The ocular drug discovery arena has undergone a significant improvement in the last few years culminating in the FDA approvals of 8 new drugs. However, despite a large number of drugs, generics, and combination products available, it remains an urgent need to find breakthrough strategies and therapies for tackling ocular diseases. Targeting the ade...
Alizadeh, Seyedeh Roya Hashemi, Seyedeh Mahdieh
Published in
Medicinal Chemistry Research
Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of this century, which concerns the medical community all over the world. Consequently, investigating small molecu...
Zhang, Gang Sheng, Li Hegde, Pooja Li, Yan Aldrich, Courtney C.
Published in
Medicinal Chemistry Research
8-Nitrobenzothiazinones (BTZs) exemplified by macozinone are a new class of antitubercular agents with exceptionally potent activity. The aryl nitro group has been considered indispensable for activity since this is bioactivated within mycobacteria by the flavoenzyme DprE1 to a reactive nitroso metabolite that covalently labels Cys387. However, the...
