On September 21, 2021, Kshirsagar, Rajendra R.; Gadekar, Pradip K.; Khedkar, Vijay M.; Vijayakumar, Vijayaparthasarathi published an article.Electric Literature of 2010-06-2 The title of the article was Design, Synthesis, and the Effects of (E)-9-Oxooctadec-10-en-12-ynoic Acid Analogues to Promote Glucose Uptake. And the article contained the following:
(E)-9-Oxooctadec-10-en-12-ynoic acid is found to mediate its antidiabetic activity by increasing insulin-stimulated glucose uptake in L6 myotubes by activating the phosphoinositide 3-kinase (PI3K) pathway. A simultaneous study of site-specific modification followed by structure-activity relationship provides a tremendous scope for exploiting the bioactivity of the parent mol. Therefore, in the present study, we focused on site-specific modification of (E)-9-oxooctadec-10-en-12-ynoic acid (1) to generate multiple derivatives and extensive structure-activity relationship (SAR) studies. We have done structural base design and synthesized a series of amides from acid compound 1. Compound 1 consists of an acid functionality, which is known for its metabolism-related liabilities. The SAR has been generated using scaffolds of different antidiabetic drugs such as biguanides, sulfonylureas, thiazolidinediones/glitazones, peroxisome proliferator-activated receptors, K + ATP, α-glucosidase inhibitors, and others. Furthermore, the study demonstrates and explains the promising derivatives and importance of SAR of the compound (E)-9-oxooctadec-10-en-12-ynoic acid. In order to gain mechanistic insights, a mol. docking study was performed against PI3K, which could identify the binding modes and thermodn. interactions governing the binding affinity. According to our research,some compounds are the best compounds from the series having EC50 values of 15.47, 8.89, 7.00, 13.99, 8.70, 12.27, and 16.14μM, resp. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Electric Literature of 2010-06-2
The Article related to oxooctadecenynoic acid analog preparation antidiabetic activity, General Organic Chemistry: Synthetic Methods and other aspects.Electric Literature of 2010-06-2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica