Development of Novel Phthalazinone-Triazole Hybrids as Potential Antidiabetic Agents Targeting GLUT4 Translocation in Skeletal Muscle.

A series of 38 phthalazinone-triazole compounds were synthesized using Click chemistry to identify potential antidiabetic agents. These compounds were systematically tested for their ability to promote glucose transporter type 4 (GLUT4) translocation in skeletal muscle cells. Among the 38 derivatives, 11 compounds (i.

Design, synthesis and evaluation of novel carboline-triazole hybrids as promising antimalarial agents.

A series of twenty-four carboline-triazole derivatives were synthesized using a molecular hybridization approach and evaluated for their antimalarial activity against Plasmodium parasites. Ten compounds exhibited strong in vitro antimalarial activity against both chloroquine-sensitive Pf3D7 and chloroquine-resistant PfK1 strains, with IC values ranging from 0.21 to 0.

Design, synthesis, and biological evaluation of quinazolinone-dihydropyrimidinone as a potential anti-diabetic agent via GLUT4 translocation stimulation.

A library of 30 novel quinazolinone-dihydropyrimidinone derivatives was synthesized employing a diversity-oriented approach for the identification of potential anti-diabetic therapeutic lead. In vitro evaluation revealed that seven compounds (5d, 5e, 5i, 5j, 5l, 5m and 5s) significantly enhanced the rate of GLUT4 translocation to the cell surface in L6-GLUT4myc myotubes. Out of these, compound, 5m exhibited promising potency to stimulate GLUT4 translocation in skeletal muscle cells via activating AMPK-dependent pathway, but independent to PI-3-K/AKT signaling.

Antitubercular evaluation of dihydropyridine-triazole conjugates: design, synthesis, screening, SAR and ADME predictions.

This study investigates the potential of click chemistry for the development of novel anti-tuberculosis agents. A targeted library of 1,4-dihydropyridine-1,2,3-triazole conjugates was synthesized and evaluated for their activity against HRa using the resazurin microtiter assay (REMA). Among the synthesized derivatives, compounds J10, J11, J14, J22 and J23 demonstrated significant antimycobacterial activity.

Antileishmanial evaluation of triazole-butenolide conjugates: design, synthesis, screening, SAR and ADME predictions.

In the quest to discover novel scaffolds with leishmanicidal effects, a series of 23 compounds containing the most promising 1,2,3-triazole and highly potent butenolide in one framework were synthesized. The synthesized conjugates were screened against parasite; five of them showed moderate antileishmanial activity against promastigotes (IC 30.6 to 35.

Synthesis of tetracyclic 4H-benzo[5,6]chromeno[3,4-d]oxazoles via palladium-catalyzed intramolecular direct heteroarylation.

We report a palladium-catalyzed intramolecular direct heteroarylation of oxazole tethered β-naphthols to access corresponding tetracyclic 4H-benzo[5,6]chromeno[3,4-d]oxazoles. Various functional groups are well tolerated and furnished the desired products in good to excellent yields under the present reaction conditions. The scale-up reaction and synthetic utility of the resulting molecules have been demonstrated.

Synthesis of 2-methoxy-3-(thiophen-2-ylmethyl)quinoline containing amino carbinols as antitubercular agents.

We have designed and synthesized 2-methoxy-3-(thiophen-2-ylmethyl)quinoline containing amino carbinols as possible anti-tubercular agents to combat the disease. These molecules were synthesized by tethering amino ether linkage with hydroxyl group to diarylquinoline skeleton; hydroxyl and amine chains were engrafted on diaryl ring. They were evaluated against strain (HR) of Mycobacterium tuberculosis and most of compounds showed in vitro antitubercular activity.

Tandem Cu-catalyzed ketenimine formation and intramolecular nucleophile capture: Synthesis of 1,2-dihydro-2-iminoquinolines from 1-(o-acetamidophenyl)propargyl alcohols.

The copper-catalyzed ketenimine formation reaction of 1-(o-acetamidophenyl)propargyl alcohols with various sulfonyl azides is found to undergo a concomitant intramolecular nucleophile attack to generate 1,2-dihydro-2-iminoquinolines after aromatization (via elimination of acetyl and hydroxy groups) and tautomerization. The reaction produces 4-substituted and 3,4-unsubstituted title compounds in moderate to good yields under mild reaction conditions.