An article The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators WOS:000469304500015 published article about INDOLES; CATALYST; DISCOVERY; ROUTE; MILD; PAIN in [Tseng, Chih-Chung; Zanato, Chiara; Massarenti, Chiara; Dall’Angelo, Sergio; Zanda, Matteo; Greig, Iain R.] Univ Aberdeen, Kosterlitz Ctr Therapeut, Aberdeen AB25 2ZD, Scotland; [Baillie, Gemma; Ross, Ruth A.] Univ Toronto, Dept Pharmacol & Toxicol, Toronto, ON M5S 1A8, Canada; [Donvito, Giulia; Mustafa, Mohammed A.; Juola, Sophie E.; Lichtman, Aron H.] Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA; [Lichtman, Aron H.] Virginia Commonwealth Univ, Dept Med Chem, Richmond, VA 23298 USA; [Zanda, Matteo] CNR, ICRM, Via Mancinelli 7, I-20131 Milan, Italy; [Harrison, William T. A.] Univ Aberdeen, Dept Chem, Aberdeen AB24 3UE, Scotland; [Zanda, Matteo] Loughborough Univ, Ctr Sensing & Imaging Sci, Sir David Davies Bldg, Loughborough LE11 3TU, Leics, England in 2019, Cited 37. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. COA of Formula: C14H10O3
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