Coupling of acceptor-substituted diazo compounds and tertiary thioamides: synthesis of enamino carbonyl compounds and their pharmacological evaluation.

This paper describes the synthesis of enamino carbonyl compounds by the copper(i)-catalyzed coupling of acceptor-substituted diazo compounds and tertiary thioamides. We plan to use this method to synthesize indolizidine (-)-237D analogs to find α6-selective antismoking agents. Therefore, we also performed α6-nAchRs binding studies of selected products.

Simulations of Promising Indolizidine-6-2 Nicotinic Acetylcholine Receptor Complexes.

Smoking-cessation drugs bind many off-target nicotinic acetylcholine receptors (nAChRs) and cause severe side effects if they are based on nicotine. New drugs that bind only those receptors, such as α6β2* nAChR, implicated in nicotine addiction would avoid the off-target binding. Indolizidine (-)-237D (IND (-)-237D), a bicyclic alkaloid, has been shown to block α6β2* containing nAChRs and functionally inhibit the nicotine-evoked dopamine release.

Heart rate reactivity and current post-traumatic stress disorder when data are missing.

Aims: This study demonstrates that auxiliary and exclusion criteria variables increase the effectiveness of missing imputation in correcting underestimation of physiologic reactivity in relation to post-traumatic stress disorder (PTSD) caused by deleting cases with missing physiologic data.

Methods: This study used data from survivors of the 1995 Oklahoma City bombing and imputed missing heart rate data using auxiliary and exclusion criteria variables. Logistic regression was used to examine heart rate reactivity in relation to current PTSD.