Novel silaproline (Sip)-incorporated close structural mimics of potent antidepressant peptide drug rapastinel (GLYX-13)
| Title | Novel silaproline (Sip)-incorporated close structural mimics of potent antidepressant peptide drug rapastinel (GLYX-13) |
| Publication Type | Journal Article |
| Year of Publication | 2017 |
| Authors | Madica, K, Nadimpally, KChaitanya, Sanjayan, GJ |
| Journal | Tetrahedron Letters |
| Volume | 58 |
| Issue | 16 |
| Pagination | 1568-1571 |
| Date Published | APR |
| Type of Article | Article |
| Abstract | Rapastinel (GLYX-13) is a C-amidated tetrapeptide drug under clinical development for adjunctive treatment of major depressive disorder (MDD). Rapastinel features two consecutive proline residues centered at the peptide sequence (Thr-Pro-Pro-Thr-NH2), which are detrimental to its biological activity. In this communication, we report the synthesis of very close structural analogues of rapastinel comprising silaproline (Sip) as proline surrogate. By virtue of its enhanced lipophilicity and metabolic stability, Sip introduction in the native rapastinel sequence is expected to improve its pharmacokinetic profiles. |
| DOI | 10.1016/j.tetlet.2017.03.015 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 2.125 |
Divison category:
Organic Chemistry
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