Khedkar, Nilesh Raghunath; Irlapatti, Nageswara Rao; Dadke, Disha; Kanoje, Vijay; Shaikh, Zubair; Karche, Vijay; Shinde, Vikas; Deshmukh, Gokul; Patil, Amit; Jachak, Santosh; Phukan, Samiron; Kizhakinagath, Praveenkumar Anidil; Gholve, Milind; Bhankhede, Trupti; Daler, Jagadeesh; Nemade, Harshal Narendra; Budhe, Sagar; Pareek, Himani; Yeshodharan, Rajesh; Gupta, Rajesh; Kalia, Anil; Pandey, Dilip; Wagh, Akshaya; Kumar, Swaroop; Patil, Vinod; Modi, Dipak; Sharma, Nidhi; Ahirrao, Prajakta; Mehta, Maneesh; Kumar, Hemant; Nigade, Prashant; Tamane, Kaustubh; Mallurwar, Sadanand; Kuldharan, Sandip; Pawar, Shashikant; Vishwase, Gururaj; Bokan, Sanjay; Singh, Minakshi; Naik, Kumar; Ingawale, Sachin; Shankar, Rajesh; Kamalakannan, Prabakaran; Venugopal, Spinvin; George, Shaji K.; Padiya, Kamlesh J.; Nemmani, Kumar V. S.; Gundu, Jaysagar; Bhonde, Mandar; Narasimham, Lakshmi; Sindkhedkar, Milind; Shah, Chirag; Sinha, Neelima; Sharma, Sharad; Bakhle, Dhananjay; Kamboj, Rajender Kumar; Palle, Venkata P. published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-N-(2′-methyl-3′-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1′-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization》.Safety of 3-Bromo-2-methylbenzoic acid The article contains the following contents:
The role of calcium release-activated calcium (CRAC) channels is well characterized and is of particular importance in T-cell function. CRAC channels are involved in the pathogenesis of several autoimmune diseases, making it an attractive therapeutic target for treating inflammatory diseases, like rheumatoid arthritis (RA). A systematic structure-activity relationship study with the goal of optimizing lipophilicity successfully yielded two lead compounds, 36 and 37. Both compounds showed decent potency and selectivity and a remarkable pharmacokinetic profile. Further characterization in in vivo RA models and subsequent histopathol. evaluation of tissues led to the identification of 36 as a clin. candidate. Compound 36 displayed an excellent safety profile and had a sufficient safety margin to qualify it for use in human testing. Oral administration of 36 in Phase 1 clin. study in healthy volunteers established favorable safety, tolerability, and good target engagement as measured by levels of IL-2 and TNF-α. In the part of experimental materials, we found many familiar compounds, such as 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Safety of 3-Bromo-2-methylbenzoic acid)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Safety of 3-Bromo-2-methylbenzoic acid The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary