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Synthesis of antifungal isoindole (5-methyl-isoxazole-3-yl)-[2-(5-methyl-isoxazol-3-yl)2,3-dihydro-isoindol-1-ylidene]amine  [PDF]
Shar S. Al-Shihry
Molbank , 2005, DOI: 10.3390/m447
Abstract: No abstract available
Microwave-Assisted Synthesis of Novel 2,3-Dihydro-4-Pyridinones  [PDF]
Bahjat A. Saeed,Rita S. Elias,Wisam A. Radhi
Molecules , 2010, DOI: 10.3390/molecules15118425
Abstract: Novel 2,3-dihydro-4-pyridinones were synthesized via the reaction of curcumin and primary amines or amine acetates under microwave irradiation. Montmorillonite K-10 was used as a catalyst. Reaction times did not exceed 120 s. The structures of the compounds were established by elemental analysis and from their mass, 1H- and 13C-NMR spectra.
Assessment of the In Vivo Genotoxicity of New Lead Compounds to Treat Sickle Cell Disease  [PDF]
Jean Leandro Dos Santos,Priscila Longhin Bosquesi,Eliana Aparecida Varanda,Lídia Moreira Lima,Man Chin Chung
Molecules , 2011, DOI: 10.3390/molecules16042982
Abstract: The compounds 1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl nitrate (C1), (1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl nitrate (C2), 3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)benzyl nitrate (C3), 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-hydroxy-benzenesulfonamide (C4), 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)benzyl nitrate (C5), and 2-[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)phenyl]ethyl nitrate (C6) were evaluated with a micronucleus test using mouse peripheral blood to identify new candidate drugs for the treatment of sickle cell disease (SCD) that are safer than hydroxyurea. The compounds induced an average frequency of micronucleated reticulocytes (MNRET) of less than six per 1,000 cells at 12.5, 25, 50, and 100 mg/kg, whereas hydroxyurea induced an average MNRET frequency of 7.8, 9.8, 15, and 33.7 per 1000 cells respectively, at the same concentrations. Compounds C1–C6 are new non-genotoxic in vivo candidate drugs for the treatment of SCD symptoms.
Mutagenicity of New Lead Compounds to Treat Sickle Cell Disease Symptoms in a Salmonella/Microsome Assay  [PDF]
Jean Leandro Dos Santos,Eliana A. Varanda,Lídia Moreira Lima,Chung Man Chin
International Journal of Molecular Sciences , 2010, DOI: 10.3390/ijms11020779
Abstract: A series of phthalimide derivatives planned as drugs candidates to treat the symptoms of sickle cell anemia were evaluated in a mutagenicity test using strains of Salmonella typhimurium TA100 and TA102, without and with addition of S9 mixture, with the aim to identify the best structural requirements for a drug candidate without genotoxic activity. The compounds (1,3-dioxo-1,3-dihydro-2 H-isoindol-2-yl)methyl nitrate ( 1); (1,3-dioxo-1,3-dihydro-2 H-isoindol-2-yl)ethyl nitrate ( 2); 3-(1,3-dioxo-1,3-dihydro-2 H-iso-indol-2-yl)benzyl nitrate ( 3); 4-(1,3-dioxo-1,3-dihydro-2 H-isoindol-2-yl)- N-hydroxy-benzenesulfonamide ( 4); 4-(1,3-dioxo-1,3-dihydro-2 H-isoindol-2-yl)benzyl nitrate ( 5) and 2-[4-(1,3-dioxo-1,3-dihydro-2 H-isoindol-2-yl)phenyl]ethyl nitrate ( 6) presented mutagenic potency ranging between 0-4,803 revertants/μmol. These results allowed us to propose that a methyl spacer linked to a nitrate ester subunit associated to meta aromatic substitution decreases mutagenicity.
One-Pot Synthesis of Novel 2,3-Dihydro-1H-indazoles  [PDF]
Gary W. Breton,Antonio J. Lepore
Molecules , 2011, DOI: 10.3390/molecules16119553
Abstract: A copper(I)-mediated one-pot synthesis of 2,3-dihydro-1H-indazole heterocycles has been developed. This synthetic route provides the desired indazoles in moderate to good yields (55%–72%) which are substantially better than those achievable with an alternative two-step reaction sequence. The reaction is tolerant of functionality on the aromatic ring.
Benzyl 3-dehydroxy-1,2,5-oxadiazolo[3′,4′:2,3]oleanolate  [cached]
Jun Hu,Xiaoyun Gong,Ruji Wang,Yong Ju
Acta Crystallographica Section E , 2009, DOI: 10.1107/s1600536809026695
Abstract: The title compound, C37H50N2O3, is a benzyl ester derivative of oleanolic acid, a pentacyclic triterpene, with a five-membered oxadiazole ring fused to the ring A. The triterpene A and C rings adopt slightly distorted half-chair conformations, whereas the remaining three six-membered rings are in chair forms.
(3′R)-3′-Benzyl-2′,3′-dihydro-1H-spiro[indole-3,1′-naphtho[2,3-c]pyrrole]-2,4′,9′-trione  [cached]
Garima Sharma,S. Vasanth Kumar,Habibah A. Wahab,Mohd Mustaqim Rosli
Acta Crystallographica Section E , 2012, DOI: 10.1107/s1600536812036227
Abstract: In the title compound, C26H18N2O3, the maximum deviations from planarity for the tetrahydro-1H-naphtho[2,3-c]pyrrole and indoline rings systems are 0.091 (1) and 0.012 (2) , respectively. These ring systems make a dihedral angle of 89.95 (6)° with each other and they make dihedral angles of 73.42 (8) and 71.28 (9)°, respectively, with the benzene ring. In the crystal, inversion dimers linked by pairs of N—H...O hydrogen bonds generate R22(8) loops and C—H...O interactions connect the dimers into corrugated sheets lying parallel to the bc plane.
1-{[(2,3-Dihydro-1H-inden-2-yl)oxy]methyl}quinazoline-2,4(1H,3H)-dione  [cached]
Nasser R. El-Brollosy,Necmi Dege,Güneş Demirtaş,Mohamed I. Attia
Acta Crystallographica Section E , 2012, DOI: 10.1107/s1600536812022350
Abstract: In the title molecule, C18H16N2O3, the five-membered ring has an envelope conformation, with the substituted C atom deviating by 0.342 (4) from the mean plane P calculated for the remainder of the non-H atoms of the 2,3-dihydro-1H-indene fragment. The mean planes of quinazoline-2,4(1H,3H)-dione fragment and P form a dihedral angle of 59.08 (4)°. In the crystal, pairs of N—H...O hydrogen bonds link molecules into inversion dimers, and weak C—H...O hydrogen bonds and π–π interactions between the benzene rings of the quinazoline ring systems [centroid–centroid distance = 3.538 (3) ] further consolidate the packing.
2,3-Dihydro-1H-cyclopenta[b]quinoline Derivatives as Acetylcholinesterase Inhibitors—Synthesis, Radiolabeling and Biodistribution  [PDF]
Pawe? Szymański,Alice Lázni?ková,Milan Lázni?ek,Marek Bajda,Barbara Malawska,Magdalena Markowicz,El?bieta Mikiciuk-Olasik
International Journal of Molecular Sciences , 2012, DOI: 10.3390/ijms130810067
Abstract: In the present study we describe the synthesis and biological assessment of new tacrine analogs in the course of inhibition of acetylcholinesterase. The obtained molecules were synthesized in a condensation reaction between activated 6-BOC-hydrazinopyridine-3-carboxylic acid and 8-aminoalkyl derivatives of 2,3-dihydro-1 H-cyclopenta[b]quinoline. Activities of the newly synthesized compounds were estimated by means of Ellman’s method. Compound 6h (IC 50 = 3.65 nM) was found to be most active. All obtained novel compounds present comparable activity to that of tacrine towards acetylcholinesterase (AChE) and, simultaneously, lower activity towards butyrylcholinesterase (BChE). Apart from 6a, all synthesized compounds are characterized by a higher affinity for AChE and a lower affinity for BChE in comparison with tacrine. Among all obtained molecules, compound 6h presented the highest selectivity towards inhibition of acetylcholinesterase. Molecular modeling showed that all compounds demonstrated a similar binding mode with AChE and interacted with catalytic and peripheral sites of AChE. Also, a biodistribution study of compound 6a radiolabeled with 99mTc was performed.
3-Amino-N-benzyl-6-(4-fluorophenyl)thieno[2,3-b]pyridine-2-carboxamide  [cached]
Jin-Ni Zhao,Sheng-Yong Yang,Li Yang
Acta Crystallographica Section E , 2012, DOI: 10.1107/s160053681202212x
Abstract: In the title compound, C21H16FN3OS, the thieno[2,3-b]pyridine system forms dihedral angles of 10.57 (12) and 83.87 (5)° with the fluorophenyl ring at the 6-position and the phenyl ring of the benzyl group, respectively. In the crystal, molecules are linked by weak N—H...N anf N—H...O hydrogen bonds and π–π stacking interactions involving fluorophenyl rings of adjacent molecules, with a centroid–centroid distance of 3.648 (10) . In addition, intramolecular N—H...S and N—H...O hydrogen bonds contribute to the stability of the molecular conformation.
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