X-ray diffraction data are reported for two mesoionic 1,2,3,4-thiatriazolium-5-aminides. The data for the thiatriazole ring are consistent with those for similar compounds published previously. The C5-N6 bond in compound 1 is about 1.26 Å in length and about 1.32 Å for compound 2, showing that t...
1,2,3,4-Thiatriazole is a relatively rare heterocyclic system. In the present chapter we have compared the data from recent publications with an overview of previous work. Thus, the previous chapters in CHEC(1984) and CHEC-II(1996) should be read together with the following chapter in order to g...
The nature of [3H] {1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride} (GBR 12935) binding to human platelets was investigated. A common property of the inhibitors of this binding was their association with the cytochrome P-450 system. cis-Flupenthixol and {1-[2-[bis(4-f...
SU-12080 and phentolamine reduce the inhibitory responses of the isolated rabbit ileum to epinephrine, norepinephrine and phenylephrine and block the stimulation of the isolated rabbit uterus to these agonists. The drugs are effective in equimolar doses. SU-12080 and phentolamine do not affect t...
L-5-Hydroxytryptophan (5HTP) induces in guinea pigs a myoclonic jerking which is dependent upon stimulation of brainstem 5-hydroxytryptamine (5HT) receptors. We have investigated the ability of 5HT precursors and a range of synthetic 5HT agonists to produce myoclonus. The 5HT precursors and 5HT ...
The piperazine derivatives include 1-benzylpiperazine (BZP), 1,3-trifluoromethylphenylpiperazine (TFMPP), 1-(3-chlorophenyl) piperazine (mCPP) and 1-(4-methoxyphenyl) piperazine (MeOPP); a full summary of their chemical properties is presented in the ‘Physical Descriptions’ section. These nove...
In this study, using molecular hybridization approach, fourteen novel 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives (7a–n) were designed as inhibitor of HIV-1 RT. The binding affinity of the designed compounds with HIV-1 RT as well as their drug-likeness behavior was pr...
Piperazine is a promising scaffold for drug development due to its broad spectrum of biological activities. Based on this, the new piperazine-containing compound LQFM018 (2) [ethyl 4-((1-(4-chlorophenyl)-1H-pyrazol-4-yl)methyl)piperazine-1-carboxylate] was synthetized and some biological activit...
From leaves of Jaborosa bergii five new withanolides were isolated and studied by spectroscopic (1H and 13C NMR, MS) and chemical methods. The new products were characterized as the epoxylactol and epoxylactone derivatives of 27-deoxy-2,3-dihydrojaborosalactone A having hydroxyl groups at C-14β...
Ginkgo biloba cell suspension cultures were used to bioconvert sinenxan A, 2α,5α,10β,14β-tetra-acetoxy-4(20), 11-taxadiene, a taxoid isolated from callus tissue cultures of Taxus spp. Besides two major products, 9α-hydroxy-2α,5α,10β,14β-tetra-acetoxy-4(20), 11-taxadiene 1 and 9α,10β-d...
Ginkgo biloba cell suspension cultures were used to biotransform 2α,5α,10β,14β-tetra-acetoxy-4(20),11-taxadiene. Two novel compounds were obtained and their structures were identified as 9α-hydroxyl-2α,5α,10β,14β-tetra-acetoxy-4(20), 11-taxadiene 1 and 9α, 10β-dihydroxyl-2α,5α,14β-...
An efficient approach to 14β-H antiprogestins is described. The key step of the synthesis is a cleavage of 17-silyl dienol ethers 7 respectively 12, which are generated from the corresponding Δ14-17-ketones, with hydrogen fluoride-pyridine complex. This method gave access to 14β-H analogs of ...
Numerous bioactive glycosteroids are characterized by aglycones bearing a 14β-hydroxy pregnane skeleton like boucerin and isoramanone. In general, the syntheses of the latter are achieved by acidic hydrolysis of the corresponding glycosteroids. These aglycones were also obtained by a combined N...
This article describes a new, convenient, improved synthesis of the 2-debenzoyl-2-m-methoxybenzoyl-7-triethylsilyl-13-oxo-14β-hydroxybaccatin III 1,14-carbonate, the key intermediate in the synthesis of two new second-generation antitumor taxanes.
Caralluma and Hoodia are genera of succulent plants belonging to the subfamily of Asclepiadoideae in the family of Apocynaceae. Caralluma is distributed in dry regions of tropical Asia and Africa, majority of species being indigenous to the Indian subcontinent and the Arabian Peninsula. The genu...
The production of the anticancer drug Taxol in Taxus (yew) cell cultures is often accompanied by the formation of side-route polyoxygenated taxoid metabolites bearing a 14β-hydroxyl group. The recent acquisition of several new semisynthetic taxoid intermediates enabled the screening of a family...
Cardenolides are composed of a steroid nucleus and a five-membered unsaturated lactone (butenolide) ring at C-17β. It is assumed that the butenolide ring is formed from a pregnane 21-O-malonyl hemiester after a condensation reaction between the methylenic group of the malonic acid residue and t...
The block copolymers of poly(d-lactide)-b-poly(butylene succinate)-b-poly(d-lactide) (PDLA-b-PBS-b-PDLA) were added into PLLA matrix to enhance the toughness of PLLA by solution casting method. The properties of the films were investigated by wide angle X-ray diffractometry (WAXD), differential ...
In this work, poly(l-lactide)/poly(d-lactide)/nanocrystalline cellulose (PLLA/PDLA/NCC) stereocomplex blends were prepared using a solution blending method. The effect of NCC on the crystallization kinetics of symmetric PLLA/PDLA blend was systematically investigated. The incorporation of NCC si...
It is an effective strategy to improve the heat resistance of polylactide (PLA) via forming stereocomplex crystals (SCs) in poly(l-lactide) (PLLA)/poly(d-lactide) (PDLA) blend. In this work, pentearythritol (PENTA), which is an environment-friendly polyhydroxy compound for food packaging, is sel...
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