I found the field of Pharmacology & Pharmacy very interesting. Saw the article The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators published in 2019. Quality Control of Benzoic anhydride, Reprint Addresses Zanda, M; Greig, IR (corresponding author), Univ Aberdeen, Kosterlitz Ctr Therapeut, Aberdeen AB25 2ZD, Scotland.; Zanda, M (corresponding author), CNR, ICRM, Via Mancinelli 7, I-20131 Milan, Italy.; Zanda, M (corresponding author), Loughborough Univ, Ctr Sensing & Imaging Sci, Sir David Davies Bldg, Loughborough LE11 3TU, Leics, England.. The CAS is 93-97-0. Through research, I have a further understanding and discovery of Benzoic anhydride
The first generation of CB1 positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs include the nitro group, it is generally not regarded as being drug-like, and this is particularly true for aliphatic nitro groups. There are very few case studies where an appropriate bioisostere replaced a nitro group that had a direct role in binding. This may be indicative of the difficulty of replicating its binding interactions. Herein, we report the design and synthesis of ligands targeting the allosteric binding site on the CB, cannabinoid receptor, in which a CF3 group successfully replaced the aliphatic NO2. In general, the CF3-bearing compounds were more potent than their NO2 equivalents and also showed improved in vitro metabolic stability. The CF3 analogue (1) with the best balance of properties was selected for further pharmacological evaluation. Pilot in vivo studies showed that (+/-)-1 has similar activity to (+/-)-ZCZ011, with both showing promising efficacy in a mouse model of neuropathic pain.
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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com