Results 1 to 10 of about 15,048 (225)

Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview

open access: yesPharmaceuticals, 2022
Nitroimidazole represents one of the most essential and unique scaffolds in drug discovery since its discovery in the 1950s. It was K. Maeda in Japan who reported in 1953 the first nitroimidazole as a natural product from Nocardia mesenterica with ...
Rohit Singh   +2 more
exaly   +5 more sources

Design, Synthesis and Anticancer Evaluation of Nitroimidazole Radiosensitisers

open access: yesMolecules, 2023
The role of hypoxic tumour cells in resistance to radiotherapy, and in suppression of immune response, continues to endorse tumour hypoxia as a bona fide, yet largely untapped, drug target.
Lydia P. Liew   +6 more
doaj   +2 more sources

Structure-enabled enhancement of potency in a metronidazole–benznidazole hybrid: design, synthesis, and evaluation of antitrypanosomal activity of a benzylamide-linked 5-nitroimidazole [PDF]

open access: yesFrontiers in Pharmacology
Benznidazole (1) remains the primary antiparasitic drug used clinically for Chagas disease, underscoring the need to discover novel treatments targeting Trypanosoma cruzi (T. cruzi) infection.
Afonso Santine M. M. Velez   +8 more
doaj   +2 more sources

Prevalence of Nitroimidazole-Refractory Giardiasis Acquired in Different World Regions, Sweden, 2008–2020 [PDF]

open access: yesEmerging Infectious Diseases
Treatment-refractory giardiasis is an emerging clinical problem. Of 4,285 giardiasis cases identified during 2008–2020 in Stockholm, Sweden, 102 (2.4%) were nitroimidazole refractory. Among cases acquired in India, the percentage was high (64/545 [12%])
Karin A. Ydsten   +3 more
doaj   +2 more sources

Influence of 2-Nitroimidazoles in the Response of FaDu Cells to Ionizing Radiation and Hypoxia/Reoxygenation Stress

open access: yesAntioxidants, 2023
Cellular adaptations to hypoxia promote resistance to ionizing radiation (IR). This presents a challenge for treatment of head and neck cancer (HNC) that relies heavily on radiotherapy.
Faisal Bin Rashed   +5 more
doaj   +1 more source

2-(Nitroaryl)-5-Substituted-1,3,4-Thiadiazole Derivatives with Antiprotozoal Activities: In Vitro and In Vivo Study

open access: yesMolecules, 2022
Nitro-containing compounds are a well-known class of anti-infective agents, especially in the field of anti-parasitic drug discovery. HAT or sleeping sickness is a neglected tropical disease caused by a protozoan parasite, Trypanosoma brucei.
Alireza Mousavi   +5 more
doaj   +1 more source

Niclosamide Is Active In Vitro against Mycetoma Pathogens

open access: yesMolecules, 2021
Redox-active drugs are the mainstay of parasite chemotherapy. To assess their repurposing potential for eumycetoma, we have tested a set of nitroheterocycles and peroxides in vitro against two isolates of Madurella mycetomatis, the main causative agent ...
Abdelhalim B. Mahmoud   +5 more
doaj   +1 more source

Fexinidazole for Human African Trypanosomiasis, the Fruit of a Successful Public-Private Partnership

open access: yesDiseases, 2022
After 100 years of chemotherapy with impractical and toxic drugs, an oral cure for human African trypanosomiasis (HAT) is available: Fexinidazole. In this case, we review the history of drug discovery for HAT with special emphasis on the discovery, pre ...
Sonja Bernhard   +3 more
doaj   +1 more source

Chemosensitization by lipophilic nitroimidazoles [PDF]

open access: yesBritish Journal of Cancer, 1983
We have carried out experiments to determine the response of tumours and normal tissues in the C3H mouse to the combination of lipophilic nitroimidazoles and CCNU, cyclophosphamide or melphalan. The nitroimidazoles studied were Ro 07-1902 (1902) and benznidazole (Ro 07-1051, BENZO). Maximum enhancement of CCNU response in the KHT sarcoma by 2.5 mmol kg-
P R, Twentyman, P, Workman
openaire   +2 more sources

The Role of Nitroreductases in Resistance to Nitroimidazoles [PDF]

open access: yesBiology, 2021
Antimicrobial resistance is a major challenge facing modern medicine, with an estimated 700,000 people dying annually and a global cost in excess of $100 trillion. This has led to an increased need to develop new, effective treatments. This review focuses on nitroimidazoles, which have seen a resurgence in interest due to their broad spectrum of ...
Carol Thomas, Christopher D. Gwenin
openaire   +3 more sources

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