In 2009,Katritzky, Alan R.; Tala, Srinivasa R.; Lu, Hong; Vakulenko, Anatoliy V.; Chen, Qi-Yin; Sivapackiam, Jothilingam; Pandya, Keyur; Jiang, Shibo; Debnath, Asim K. published 《Design, Synthesis, and Structure-Activity Relationship of a Novel Series of 2-Aryl 5-(4-Oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans as HIV-1 Entry Inhibitors》.Journal of Medicinal Chemistry published the findings.Product Details of 76006-33-2 The information in the text is summarized as follows:
We previously identified two small mols. targeting the HIV-1 gp41, N-(4-carboxy-3-hydroxy)phenyl-2,5-dimethylpyrrole (I) and N-(3-carboxy-4-chloro)phenylpyrrole (II), that inhibit HIV-1 infection at low micromolar levels. On the basis of mol. docking anal., we designed a series of 2-aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans, e.g. III. Compared with I and II, these compounds have bigger mol. size (437-515 Da) and could occupy more space in the deep hydrophobic pocket on the gp41 NHR trimer. Fifteen 2-aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans were synthesized by Suzuki-Miyaura cross-coupling followed by a Knoevenagel condensation and tested for their anti-HIV-1 activity and cytotoxicity on MT-2 cells. We found that all 15 compounds had improved anti-HIV-1 activity and 3 of them exhibited inhibitory activity against replication of HIV-1IIIB and 94UG103 at <100 nM range, more than 20-fold more potent than I and II, suggesting that these compounds can serve as leads for development of novel small mol. HIV fusion inhibitors. The experimental process involved the reaction of 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Product Details of 76006-33-2)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Product Details of 76006-33-2 Organobromine compounds have fallen under increased scrutiny for their environmental impact.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary