Pharmacodynamic and pharmacokinetic profile of RBx 343E48F0: A novel, long acting muscarinic receptor antagonist

Gupta, Suman; Malhotra, Shivani; Sinha, Sandeep; Singh, Shashi Kant; Singh, Rakesh K.; Krishna, Siddarangaiah; Chhabra, Pooja; Chaira, Tridib; Kannayiram, Janaki; Sharma, Pradeep; Aeron, Shelly; Kaur, Jaskiran; Kumar, Naresh; Sattigeri, Jitendra A.; Shirumalla, Raj Kumar; Paliwal, Jyoti; Dastidar, Sunanda G.; Cliffe, Ian A.; Ray, Abhijit; Bhatnagar, Pradip K.

doi:10.1016/j.ejphar.2011.02.024

Cited by 5 publications

(2 citation statements)

References 23 publications

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“…Ranbaxy recently disclosed the pharmacodynamic profle of RBx 343E48FO (18; FiguRe 2), a novel imidazolium bromide quaternary salt incorporating a tiotropium, such as tertiary alcohol-substituted ester moiety [64]. The main characteristic of the compound is its 60-fold selectivity for the M 3 subtype (pK i = 9.6) over the M 2 receptor (pK i = 7.8) in radiolabeled binding studies.…”

Section: Future Science Groupmentioning

confidence: 99%

Inhaled Long-Acting Muscarinic Antagonists in Chronic Obstructive Pulmonary Disease

Busch-Petersen

Lainé

2011

Future Med. Chem.

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In 2002, the first long-acting muscarinic antagonist, tiotropium bromide (Spiriva(®)), was launched as a once-daily bronchodilating agent for the treatment of chronic obstructive pulmonary disease. Since then, there has been intense discovery research activity in this area and, currently, several alternative inhaled long-acting muscarinic antagonists are reported under clinical development by several pharmaceutical companies. This article will review the current inhaled development candidates, as well as literature reports of the most significant preclinical chemical series specifically designed as inhaled antimuscarinic agents.

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Section: Future Science Groupmentioning

confidence: 99%

Inhaled Long-Acting Muscarinic Antagonists in Chronic Obstructive Pulmonary Disease

Busch-Petersen

Lainé

2011

Future Med. Chem.

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“…Further optimization led to derivative 555 [391] . In a later work, RBx 343E48F0 derived from the same scaffold was characterized in a preclinical study as a bronchodilator [392] …”

Section: Biologically Active Derivatives Of Fluorinated Cycloalkyl Bu...mentioning

confidence: 99%

Fluorinated Cycloalkyl Building Blocks for Drug Discovery

et al. 2022

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The review covers various aspects of fluorinated cycloalkyl (C3−C7) building blocks for drug discovery, including their synthesis, key physicochemical properties, and biological and medicinal applications of their derivatives. The discussed synthetic methods include classical nucleophilic fluorinations of various substrates, the addition of fluorine and another heteroatom to double bonds, cycloadditions and other transformations of fluorine‐containing substrates, as well as some newer reactions like fluorination of non‐activated and remotely activated C−H bonds, decarboxylative and deborylative fluorinations, etc. The known data on the effect of introducing the fluorinated cycloalkyl groups on the compound's key in vitro parameters (such as acidity/basicity, lipophilicity, conformational behavior, and short contact capabilities) are surveyed. Finally, applications of fluorinated cycloalkyl building block derivatives in the design of biologically active compounds (including marketed drugs Maraviroc, Ivosidenib, and Sitafloxacin) are covered, with a focus on the fluorination impact.

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