Green synthesis of new naphthospiro chromanone scaffolds and their antimicrobial activity

An efficient synthesis of new naphthospiro chromanone scaffolds using ionic liquids as a green solvent under microwave irradiation is presented. The reaction was also studied under conventional elevated temperature conditions. The structures of newly synthesized compounds have been elucidated by means of IR, ¹H NMR, ¹³C NMR, and mass spectrometry data. All compounds were screened for their antimicrobial activity.     

Design,Synthesis, and Biological Activity of New Bis-1,2,3-triazole Derivatives Bearing Thiophene-Chalcone Moiety

Russian Journal of General Chemistry - A series of novel 1,4-substituted bis-aralkyl and aryl 1,2,3-triazoles bearing thiophene chalcones are synthesized via the Claisen condensation of bis...     

Iodine mediated synthesis of some new imidazo[1,2-a]pyridine derivatives and evaluation of their antimicrobial activity

Herein, we reported a series of new 2-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)imidazo[1,2-a]pyridines by using iodine and NH₄OAc in good yields. The structures of the titled compounds were characterized by the elemental analysis, ¹H NMR, ¹³C NMR, IR, and mass spectral analysis. All the titled compounds were screened for their in vitro antibacterial and antifungal activities by using streptomycin and Nystatin as standard drugs. The compounds 3k , 3l , 3g , and 3c exhibited potent activity against the tested bacterial strains and 3k , 3l , and 3c exhibited potent activity against the tested fungal strains than the reference drugs.     

Microwave assisted selective synthesis of (<Emphasis Type="Italic">E</Emphasis>)-1-(4-Chloro-7-hydroxy-2-aryl-2<Emphasis Type="Italic">H</Emphasis>-chromen-6-yl)-3-arylprop-2-en-1-ones and their antimicrobial activity

A series of new (E)-1-(4-chloro-7-hydroxy-2-aryl-2H-chromen-6-yl)-3-arylprop-2-en-1-ones (2a–2f) have been synthesized by selective mono cyclization of 4,6-dicinnamoyl resorcinols (1a–1f) using Vilsmeier–Haack reagent under conventional heating and microwave irradiation. The structures of the synthesized compounds have been elucidated by elemental analysis, IR, ¹H NMR, ¹³C NMR and Mass spectral data. The synthesized compounds were tested in vitro for antimicrobial activity.     

Indole-fused spirochromenes as potential anti-tubercular agents: design,synthesis and in vitro evaluation

Molecular Diversity - As part of an ongoing effort to develop new anti-tubercular agents, a series of novel indole-fused spirochromene hybrids (7a–l) were efficiently synthesized in excellent...     

Structure-based virtual screening of small-molecule antagonists of platelet integrin αIIbβ3 that do not prime the receptor to bind ligand

Integrin αIIbβ3 has emerged as an important therapeutic target for thrombotic vascular diseases owing to its pivotal role in mediating platelet aggregation through interaction with adhesive ligands. In the search for effective anti-thrombotic agents that can be administered orally without inducing the high-affinity ligand binding state, we recently discovered via high-throughput screening of 33,264 compounds a novel, αIIbβ3-selective inhibitor (RUC-1) of adenosine-5′-diphosphate (ADP) -induced platelet aggregation that exhibits a different chemical scaffold and mode of binding with respect to classical Arg-Gly-Asp (RGD)-mimicking αIIbβ3 antagonists. Most importantly, RUC-1 and its higher-affinity derivative, RUC-2, do not induce major conformational changes in the protein β3 subunit or prime the receptor to bind ligand. To identify additional αIIbβ3-selective chemotypes that inhibit platelet aggregation through similar mechanisms, we screened in silico over 2.5 million commercially available, ‘lead-like’ small molecules based on complementarity to the predicted binding mode of RUC-2 into the RUC-1-αIIbβ3 crystal structure. This first reported structure-based virtual screening application to the αIIbβ3 integrin led to the identification of 2 αIIbβ3-selective antagonists out of 4 tested, which compares favorably with the 0.003?% “hit rate” of our previous high-throughput chemical screening study. The newly identified compounds, like RUC-1 and RUC-2, showed specificity for αIIbβ3 compared to αVβ3 and did not prime the receptor to bind ligand. They thus may hold promise as αIIbβ3 antagonist therapeutic scaffolds.     

Synthesis of Biaryl Derivatives of Spirofurochromanone in Water and Their Anticancer Activity

Russian Journal of General Chemistry - Biaryl derivatives of spirofurochromanones have been synthesised from 4-bromophenyl derivatives of spirofurochromanones upon catalysis by Pd/C in water....