Khan, Irfan published the artcileA versatile pre and post Ugi modification for the synthesis of natural product inspired fused peptide-carboline scaffolds as potential anti-leishmanial agents, Name: 4-Methoxyphenylacetic acid, the main research area is natural product synthesis peptide carboline peptidomimetic anti leishmanial agent; leishmanicidal structure activity amastigote promastigote cytotoxicity mol docking pharmacokinetic; amine amino acid isocyanide aldehyde Ugi reaction antiamastigote activity; drug design toxicity carcinogenicity.
A series of novel β-carboline-peptide/tetrahydro-β-carbolines-peptide has been synthesized via natural product inspired mol. hybridization approach. All the hybrids were examined for their anti-leishmanial potential. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote and intracellular amastigotes (IC50 ranging from 2.43 to 7.61μM) than the control, miltefosine (IC50 = 8.2μM), with less cytotoxicity in comparison to the standard drugs (sodium stibogluconate, and miltefosine). Compound (I) was also able to inhibit Leishmania donovani TR (LdTR). A mol. modeling study based on docking and subsequent binding free energy evaluation was carry out in the active site of LdTR to understand their possible binding site. Our results show that prepared β-carboline-peptide/tetrahydro-β-carbolines-peptide represent a new structural lead for anti-leishmanial chemotherapy.
ChemistrySelect published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Name: 4-Methoxyphenylacetic acid.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem