The substitution reactions of the 2,2′-biquinoline (biq) complex cis-[Rh(biq)2Cl2]Cl with Br−, I−, OH−, NH3, pyridine (py), CN−, NO2−, SCN−, ethylenediamine (en), 2,2′-bipyridine (bipy) and dimethylglyoxime (dmgmH2) have been investigated. The new complexes cis-[Rh(biq)2ICl]I, cis-[Rh(biq)2(OH...
The substitution reactions of the title complex cis-[Rh(pq)2C12]Cl with I−, ethylenediamine (en), 2,2′-bipyridine (bipy), the oxalate dianion (ox), pyridine (py) and NO2− have been investigated. The new complexes cis-[Rh(pq)2ICl]I·2H2O, [Rh(pq)(H2O)(en)Cl](PF6)2, [Rh(pq)2(bipy)](PF6)3·2H2O, [...
A formal total synthesis of the hasubanonine alkaloid cepharamine (3b) from 7,8-dimethoxy-2- tetralone has been accomplished. A key intermediate in the synthesis was 3-methyl-1.2.4.5-tetrahydrobenz[e]indole 4a which was prepared by a one step ring expansion reaction of cyclopropyl ketone 8b effe...
Here, we have established a simple and an efficient methodology for the synthesis of spirocyclic α-amino acids as well as spirosulfones starting with readily available active methylene compounds (AMCs). The key di-bromo building blocks were assembled by reacting various active methylene compoun...
The complexes of hydroxycitronellal (o-aminobenzoic acid) copper(II) (Cu(II)-HXAB) and salicylaldehyde (o-aminobenzoic acid) copper(II) (Cu(II)-SHAB) were used as neutral carriers in PVC-based membrane ion-selective electrodes. The electrode based on Cu(II)-HXAB exhibited near-Nernstian potentia...
Mixed complexes of the type: Cd(Han)2(Him)4, Cd(Han)2(Him)5, Cd(Han)2(4-MeHim)4, Cd(Han)2(1,2-diMeim)2 (where Han = NH2C6H4COO−, Him = imidazole, 4-MeHim = 4-methylimidazole, 1,2-diMeim = 1,2-dimethylimidazole) have been synthesized and characterized by IR spectroscopic and X-ray powder diffract...
In the present work, a new para-ferrocenylbenzoate copper(I) complex (a4) has been synthesized and characterized by numerous spectroscopic techniques such as: FT-IR, AAS, and CHNS analysis. Moreover, the single-crystal X-ray structure of the compound a4 was also explored. The DNA binding potency...
Two ternary copper(II) complexes of N,N,N′,N'-tetramethylethylenediamine (tmen = C6H16N2) with benzoic acid and p-aminobenzoic acid, having the formula [Cu(tmen)(BA)2(H2O)2] (1), and [Cu(tmen)(pABA)2]. 1/2 CH3OH (2) {(Where BA1− = benzoate1− (C6H5CO21−), pABA1− = p-aminobenzoate1- (p-H2NC6...
Folic acid (FA) is an essential micronutrient but its delivery and bioavailability is a problem due to its inherent instability at various conditions. A robust protective encapsulation system for folic acid is highly desirable. This work reports the use of the divalent copper in complex with alg...
A new series of 1,3,4-oxadiazole-3(2H)-carboxamide derivatives have been synthesized by direct heterocyclization reaction of substituted benzoylisocyanate with various aroylhydrazones as novel monoamine oxidase inhibitors (MAOIs). The target molecules have been identified on the basis of satisfa...
Synthesis of carbamates from substituted ureas and organic carbonates has been demonstrated using di-n-butyltin oxide (DBTO) as a catalyst. Reactivity pattern of ureas indicated that substituents on ureas have no significant effect on the carbamate yields. While, the carbonate reactivity pattern...
A novel calmodulin (CaM) antagonist DY-9760e, (3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate), with an apparent neuroprotective effect in vivo, potently inhibits CaM-dependent nitric oxide synthase in situ. In ...
ABSTRACTThe interindividual pharmacokinetic variability of the α4β1 integrin antagonist 4-[1-[3-Chloro-4-[N′-(2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidine-2-yl]methoxybenzoic acid (D01-4582) was observed in beagles. The involvement of albumin genetic polymorphism in this v...
DY-9760e, 3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate, a novel calmodulin (CaM) antagonist, possesses neuroprotective activity. In the current study, we examined the effects of DY-9760e on nitric oxide syntha...
The novel calmodulin (CaM) antagonist DY-9760e (3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate) with an apparent neuroprotective effect in vivo preferentially inhibits neuronal nitric oxide synthase (nNOS), Ca2+...
A high-performance liquid chromatographic method for the determination of a novel calmodulin antagonist, 3-{2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl]ethyl}-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate, DY-9760e and its major metabolite, 3-{2-[4-(3-chloro-2-met...
We here assessed the effects of 3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl] ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate (DY-9760e), a novel calmodulin antagonist, on infarct size in the rat heart subjected to ischemia/reperfusion. Rats were subjected ...
The Fourier transform infrared (FT-IR) and Fourier transform Raman (FT-Raman) of N-(4-Chloro-3-methylphenyl)-2-phenylacetamide (N4C3M2P) were recorded in the regions 4000–400 cm−1 and 4000–100 cm−1 respectively, in the solid phase. The molecular structures, vibrational wave numbers, infrared i...
The Raman (3500–50 cm−1) and infrared (4000–200 cm−1) spectra of 3-chloro, 4-chloro and 5-chloro-2-methylphenyl isocyanates have been measured. Ab initio and density functional theory calculations, at the levels of RHF/6-311G* and B3LYP/6-311G*, have been performed: energies, optimized geometr...
A dynamic kinetic resolution method based on the formation of covalent diastereomeric intermediates was elaborated for the preparation of enantiomerically enriched 1-substituted-3-methyl-3-phospholene oxides. The 3-phospholene oxides were first converted to the corresponding chloro-3-phospholeni...
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