Chemoselective Nitration of Aromatic Sulfonamides With Tert-Butyl Nitrite.
Chemoselective nitration of aromatic sulfonamides with tert-butyl nitrite.
Filed under: Drug and Alcohol Rehabilitation
Chem Commun (Camb). 2012 Nov 30;
Kilpatrick B, Heller M, Arns S
A methodology for the efficient conversion of aromatic sulfonamides into their mono-nitro derivatives using tert-butyl nitrite is reported. The reaction exhibits a high degree of chemoselectivity for sulfonamide functionalized aryl systems, even in the presence of other sensitive or potentially reactive functionalities.
HubMed – drug
Feasibility and Acceptability of Screening and Brief Interventions to Address Alcohol and Other Drug Use among Patients Presenting for Emergency Services in Cape Town, South Africa.
Filed under: Drug and Alcohol Rehabilitation
Adv Prev Med. 2012; 2012: 569153
Myers B, Stein DJ, Mtukushe B, Sorsdahl K
Despite evidence from high income countries, it is not known whether screening and brief interventions (SBI) for alcohol and other drug (AOD) use are feasible to implement in low and middle income countries. This paper describes the feasibility and acceptability of a peer-led SBI for AOD-using patients presenting with injuries at emergency services in Cape Town, South Africa. Data were extracted from program records on the number of eligible patients screened and the number of program refusals. A questionnaire examined preliminary responses to the intervention for 30 patients who had completed the program and 10 emergency personnel. Peer counselors were also interviewed to identify barriers to implementation. Of the 1458 patients screened, 21% (305) met inclusion criteria, of which 74% (225) were enrolled in the intervention. Of the 30 patients interviewed, most (83%) found the program useful. Emergency personnel were supportive of the program but felt that visibility and reach could improve. Peer counselors identified the need for better integration of the program into emergency services and for additional training and support. In conclusion, with limited additional resources, peer-led SBIs for AOD use are feasible to conduct in South African emergency services and are acceptable to patients and emergency personnel.
HubMed – drug
Developing effective health interventions for women who inject drugs: key areas and recommendations for program development and policy.
Filed under: Drug and Alcohol Rehabilitation
Adv Prev Med. 2012; 2012: 269123
Pinkham S, Stoicescu C, Myers B
Women who inject drugs face multiple gender-specific health risks and barriers to healthcare access. These gendered factors may contribute to elevated rates of HIV for this population. Though few countries systematically collect gender-disaggregated data related to injecting drug use, evidence indicates that there are large populations of women who inject drugs and who are in need of improved health services, including HIV prevention. Research on the effectiveness of interventions specifically tailored for women who inject drugs, along with the experience of programs working with this subpopulation, suggests that HIV risk practices need to be addressed within the larger context of women’s lives. Multifaceted interventions that address relationship dynamics, housing, employment, and the needs of children may have more success in reducing risky practices than interventions that focus exclusively on injecting practices and condom use. Improved sexual and reproductive healthcare for women who use drugs is an area in need of development and should be better integrated into basic harm reduction programs.
HubMed – drug
Expedient construction of small molecule macroarrays via sequential palladium- and copper-mediated reactions and their ex situ biological testing.
Filed under: Drug and Alcohol Rehabilitation
Chem Sci. 2012 May; 3(5): 1555-1561
Frei R, Breitbach AS, Blackwell HE
We report the highly efficient syntheses of a series of focused libraries in the small molecule macroarray format using Suzuki-Miyaura and copper-catalyzed azide-alkyne cycloaddition (or “click”) reactions. The libraries were based on stilbene and triazole scaffolds, which are known to have a broad range of biological activities, including quorum-sensing (QS) modulation in bacteria. The library products were generated in parallel on the macroarray in extremely short reaction times (~10-20 min) and isolated in excellent purities. Biological testing of one macroarray library post-cleavage (ex situ) revealed several potent agonists of the QS receptor, LuxR, in Vibrio fischeri. These synthetic agonists, in contrast to others that we have reported, were only active in the presence of the native QS signal in V. fischeri, which is suggestive of a different mode of activity. Notably, the results presented herein showcase the ready compatibility of the macroarray platform with chemical reactions that are commonly utilized in small molecule probe and drug discovery today. As such, this work serves to expand the utility of the small molecule macroarray as a rapid and operationally straightforward approach toward the synthesis and screening of bioactive agents.
HubMed – drug
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