5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds. ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed enhanced cytotoxic effects for [IV] over 5-FU.
Axial spondyloarthritis (axSpA) is a chronic rheumatic inflammatory disease affecting mainly the spine and sacroiliac joints. Since the copper-to-zinc ratio (Cu/Zn) indicates an inflammatory response, the change in ratio is expected to correlate with axSpA. This study compared levels of Cu/Zn in the serum of axSpA patients. Serum samples were obtained from 53 patients with axSpA divided according to biological treatment into cohorts A and B, and 28 healthy control as cohort C. Serum levels of Cu and Zn were determined first by a fully automated chemistry analyzer TC-Matrix Plus, then the ratio was obtained. The elevated serum Cu concentration means of cohort B (189.32 ± 13.808 µg/dL) compared to cohort A (168.85 ± 7.244 µg/dL) a
... Show MoreSeventy five E. coli isolates were collected from urine of patients with urinary tract infections in AL-Kadhimia and AL-Yarmook teaching hospitals in Baghdad for a period between 22/11/2009 to 15/3/2010, from these samples twenty five isolates were selected according to their pattern of the highest resistance as these showing multi-drug resistances and tested to specify their minimum inhibitory concentration for (meropenem, gentamicin and amikacin), meropenem was found having the lowest MIC comparing with others. This study also includes in vitro effects of various combinations of three types of antimicrobials (meropenem, gentamicin and amikacin) against twenty five E. c
... Show MoreThe optical absorption data of Hydrogenated Amorphous Silicon was analyzed using a Dunstan model of optical absorption in amorphous semiconductors. This model introduces disorder into the band-band absorption through a linear exponential distribution of local energy gaps, and it accounts for both the Urbach and Tauc regions of the optical absorption edge.Compared to other models of similar bases, such as the O’Leary and Guerra models, it is simpler to understand mathematically and has a physical meaning. The optical absorption data of Jackson et al and Maurer et al were successfully interpreted using Dunstan’s model. Useful physical parameters are extracted especially the band to the band energy gap , which is the energy gap in the a
... Show MoreLasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.
This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits.
Schiff base ligand (H2CANPT) was prepared by two steps: first, by the condensation of curcumin with 4-amino antipyrin produces4,4'-(((1E,3Z,5Z,6E)-1,7-bis(4-hydroxy-3- methoxyphenyl)hepta-1,6-diene-3,5-diylidene)bis(azanylylidene))bis(1,5-dimethyl-2-phenyl- 1,2-dihydro-3H-pyrazol-3-one) (CANP). Second, by the condensation of (CANP) with L-tyrosine produces2,2'-(((3Z,3'Z)-(((1E,3Z,5Z,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta 1,6-diene-3,5-diylidene)bis(azanylylidene))bis(1,5-dimethyl-2-phenyl-1,2-dihydro-3-H-pyrazole- 4-yl-3-ylidene))bis(azanylylidene))bis(3-(4-hydroxyphenyl)propanoic acid) (H2CANPT). The resulted Schiff comported as hexadentate coordinated with (N4O2) atoms, then it was treated with some transition and non-transaction met
... Show MoreThe discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met
... Show MoreNew heterocyclic derivatives of quinoline are reported. Reaction of quinoline-2-thiol 4 with hydrazine hydrate gave 2-hydrazionoquinoline 5. Treatment of 5 with CS2 in pyridine afforded 1,2,4-triazolo-[4,3-a]- quinolin-1-2H-thione 6, whereas the reaction of 5 with carboxylic acids namely formic acid or acetic acid, yielded the 1,2,4-triazol-[4,3-a]-quinolin 7 or 5-methyl-1,2,4-triazolo [4,3-a]-quinoline 8 through ring closure. Diazotization of 5 under acidic conditions produced the fused tetrazole compound 9, tetrzolo-[1,5-a]- quinoline. Moreover, treatment of 5 with active methlyene compounds gave two pyrazole derivatives 10 and 11. Azomethines 12a-e were prepared through condensation of 5 with aromatic aldehydes or ketones.