238 research outputs found
Formation of 3,3,4-trimethyl-1,7-dibromonorbornane-2-one: a spectroscopic and computational Study
The structure and origin of the major by-product in the synthesis of 8-bromocamphor from (+)-3,3,8-tribromocamphor has been confirmed using NMR, coset and single crystal X-ray analysis and DFT-level computational techniques
Synthesis of N-Substituted phosphoramidic acid esters as “reverse” fosmidomycin analogues
An efficient synthetic pathway to a series of novel “reverse” fosmidomycin analogues has been developed, commencing from substituted benzylamines. In these analogues, the fosmidomycin hydroxamate moiety is reversed and the tetrahedral methylene carbon adjacent to the phosphonate moiety is replaced by a nitrogen atom bearing different benzyl groups. The resulting phosphonate esters were designed as potential antimalarial “pro-drugs”
The crystal structure of 2-oxo-2H-chromen-4-yl acetate, C11H8O4
C11H8O4, monoclinic, P21/c (no. 14), a = 4.5947(2) Å, b = 10.5414(3) Å, c = 19.1611(7) Å, β = 94.084(2)°, V = 925.70(6) Å3, Z = 4, Rgt(F) = 0.0376, wRref(F 2) = 0.1109,T = 200(2) K.CCDC no.: 190638
The crystal structure of 2-oxo-2H-chromen-4-yl acetate, C11H8O4
C11H8O4, monoclinic, P21/c (no. 14), a = 4.5947(2) Å, b = 10.5414(3) Å, c = 19.1611(7) Å, β = 94.084(2)°, V = 925.70(6) Å3, Z = 4, Rgt(F) = 0.0376, wRref(F 2) = 0.1109,T = 200(2) K.CCDC no.: 190638
Synthesis and biological evaluation of bis-N2, N2′-(4-hydroxycoumarin-3-yl) ethylidene]-2, 3-dihydroxysuccinodihydrazides
A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity
Synthesis and biological screening of diethyl [N-(thiazol-2-yl)carbamoyl]methylphosphonates
A three-step synthesis, involving condensation of bromomethyl aryl ketones with urea to afford 2- aminothiazoles, their chloroacetylation and subsequent solvent-free Arbuzov phosphonation has afforded a series of novel diethyl [N-(thiazol-2-yl)carbamoyl]methylphosphonates 3a-3f in good overall yields; the 4- carboxythiazole analogue 3g was obtained by selective hydrolysis of the corresponding ethyl ester 3f. The phosphonate esters exhibited significant anti-cancer activity (nM - low ÎĽM IC50 values) against SH-SY5Y cells and, in one case, 7.6 ÎĽM MIC90 anti-TB activity against the virulent M. tuberculosis H37Rv strain; the chloroacetamido precursors all exhibited some antimalarial (PfLDH) activity, three with IC50 values in the range 1.0 - 8.9 ÎĽM.Rhodes University for financial support and a bursary (E.O.O.) and the South African
Medical Research Council (SAMRC) for support with funds from National Treasury under its Economic
Competitiveness and Support Package.http://www.arkat-usa.orgPharmacolog
Synthesis and anti-parasitic activity of C-benzylated (N-arylcarbamoyl) alkylphosphonate esters
Unexpected substituent-dependent regioselectivty challenges in the synthesis of C-benzylated (N-arylcarbamoyl)phosphonate esters have been resolved. The C-benzylated N-furfurylcarbamoyl derivative showed low micromolar PfLDH inhibition, while one of the C-benzylated N-arylcarbamoyl analogues was active against Nagana Trypanosoma brucei parasites which are responsible for African trypanosomiasis in cattle
Tibialis posterior in health and disease: a review of structure and function with specific reference to electromyographic studies
Tibialis posterior has a vital role during gait as the primary dynamic stabiliser of the medial longitudinal arch; however, the muscle and tendon are prone to dysfunction with several conditions. We present an overview of tibialis posterior muscle and tendon anatomy with images from cadaveric work on fresh frozen limbs and a review of current evidence that define normal and abnormal tibialis posterior muscle activation during gait. A video is available that demonstrates ultrasound guided intra-muscular insertion techniques for tibialis posterior electromyography
Iliotibial band release as an adjunct to the surgical management of patellar stress fracture in the athlete: a case report and review of the literature
Stress fracture of the patella is rare. In this report, a case of patellar stress fracture occurring in an amateur athlete is presented, and an operative adjunct to the surgical management of this condition is proposed
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