Synthesizing a CuIIcomplex of tinidazole to tune the generation of the nitro radical anion in order to strike a balance between efficacy and toxic side effects

2017 ◽  
Vol 41 (12) ◽  
pp. 4879-4886 ◽  
Author(s):  
Ramesh Chandra Santra ◽  
Durba Ganguly ◽  
Subrata Jana ◽  
Neha Banyal ◽  
Jyotsna Singh ◽  
...  

Synthesis, characterization, enzyme assay, DNA binding and antimicrobial activity of a monomeric complex of CuIIwith tinidazole: significance of the controlled formation of the nitro radical anion.

RSC Advances ◽  
2020 ◽  
Vol 10 (39) ◽  
pp. 23286-23296
Author(s):  
Promita Nandy ◽  
Soumen Singha ◽  
Neha Banyal ◽  
Sanjay Kumar ◽  
Kasturi Mukhopadhyay ◽  
...  

A monomeric complex of ZnII with ornidazole [Zn(Onz)2Cl2] decreases formation of the nitro-radical anion (R–NO2˙−), and this is realized by recording it in an enzyme assay using xanthine oxidase, which is a model nitro-reductase.


INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 5-19
Author(s):  
A Mohammad ◽  

Tuberculosis (TB) is one of most prevailing diseases, responsible for the morbidity and mortality of a large number of populations worldwide. Traditionally, it has relied on a limited number of drugs such as isoniazid, rifampicin, ethambutol, streptomycin, ethionamide and pyrazinamide. However, many of these drugs have different disadvantages such as prolonged duration of treatment, host toxicity and ineffectiveness against resistant strains. This has motivated the search of newer drug molecules, capable of rapid mycobactericidal action with shortened duration of therapy, reduced toxicity and enhanced activity against multidrug resistant strains. These observations have been guiding for the currently used and newly developed anti-tubercular agents that possess potent antimicrobial activity and their side effects, activity against multi drug resistant Mycobacterium, and also in patients co-infected with HIV/AIDS.


ACS Omega ◽  
2020 ◽  
Vol 5 (40) ◽  
pp. 25668-25676
Author(s):  
Promita Nandy ◽  
Alivia Mukherjee ◽  
Chiranjit Pradhan ◽  
Saurabh Das

2020 ◽  
Vol 11 ◽  
Author(s):  
Wilian C. Rosa ◽  
Inaiá O. Rocha ◽  
Melissa B. Rodrigues ◽  
Helena S. Coelho ◽  
Laura B. Denardi ◽  
...  

2020 ◽  
Vol 117 (51) ◽  
pp. 32423-32432
Author(s):  
Mary E. O’Sullivan ◽  
Yohan Song ◽  
Robert Greenhouse ◽  
Randy Lin ◽  
Adela Perez ◽  
...  

Gentamicin is a potent broad-spectrum aminoglycoside antibiotic whose use is hampered by ototoxic side-effects. Hospital gentamicin is a mixture of five gentamicin C-subtypes and several impurities of various ranges of nonexact concentrations. We developed a purification strategy enabling assaying of individual C-subtypes and impurities for ototoxicity and antimicrobial activity. We found that C-subtypes displayed broad and potent in vitro antimicrobial activities comparable to the hospital gentamicin mixture. In contrast, they showed different degrees of ototoxicity in cochlear explants, with gentamicin C2b being the least and gentamicin C2 the most ototoxic. Structure–activity relationships identified sites in the C4′-C6′ region on ring I that reduced ototoxicity while preserving antimicrobial activity, thus identifying targets for future drug design and mechanisms for hair cell toxicity. Structure–activity relationship data suggested and electrophysiological data showed that the C-subtypes both bind and permeate the hair cell mechanotransducer channel, with the stronger the binding the less ototoxic the compound. Finally, both individual and reformulated mixtures of C-subtypes demonstrated decreased ototoxicity while maintaining antimicrobial activity, thereby serving as a proof-of-concept of drug reformulation to minimizing ototoxicity of gentamicin in patients.


1994 ◽  
Vol 6 (5-6) ◽  
pp. 509-513 ◽  
Author(s):  
Luis J. Nuñez-Vergara ◽  
C. Matus ◽  
A. F. Alvarez-Lueje ◽  
B. K. Cassels ◽  
J. A. Squella

2016 ◽  
Vol 2 (3) ◽  
pp. 83-91 ◽  
Author(s):  
Laila H. Abdel-Rahman ◽  
Ahmed M. Abu-Dief ◽  
Rafat M. El-Khatib ◽  
Shimaa Mahdy Abdel-Fatah ◽  
Amin Abdou Seleem

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