2-(4-Oxo-3-phenyl-1,3-thiazolidin-2-ylidene)malononitrile

The authors would like to thank the American University in Cairo for providing financial support to complete this work.Peer reviewedPublisher PD

Crystal structure of 2-cyano- N

In the title compound, C9H13N3O, the cyclohexylidene ring adopts a chair conformation and the bond-angle sum at the C atom linked to the N atom is 359.6°. The cyanoacetohydrazide grouping is close to planar (r.m.s. deviation for the non-H atoms = 0.031 Å) and subtends a dihedral angle of 64.08 (4)° with the four C atoms forming the seat of the chair. The C=O and N—H groups are in a syn conformation (O—C—N—H = −5°). In the crystal, inversion dimers linked by pairs of N—H...O hydrogen bonds generate R22(8) loops; this dimer linkage is reinforced by a pair of C—H...O interactions, which generate R22(14) loops. The dimers are linked by C—H...Nc (c = cyanide) interactions into [100] ladders, which feature C(4) chains and R44(20) loops

Impact of opioid-free analgesia on pain severity and patient satisfaction after discharge from surgery: multispecialty, prospective cohort study in 25 countries

Background: Balancing opioid stewardship and the need for adequate analgesia following discharge after surgery is challenging. This study aimed to compare the outcomes for patients discharged with opioid versus opioid-free analgesia after common surgical procedures.Methods: This international, multicentre, prospective cohort study collected data from patients undergoing common acute and elective general surgical, urological, gynaecological, and orthopaedic procedures. The primary outcomes were patient-reported time in severe pain measured on a numerical analogue scale from 0 to 100% and patient-reported satisfaction with pain relief during the first week following discharge. Data were collected by in-hospital chart review and patient telephone interview 1 week after discharge.Results: The study recruited 4273 patients from 144 centres in 25 countries; 1311 patients (30.7%) were prescribed opioid analgesia at discharge. Patients reported being in severe pain for 10 (i.q.r. 1-30)% of the first week after discharge and rated satisfaction with analgesia as 90 (i.q.r. 80-100) of 100. After adjustment for confounders, opioid analgesia on discharge was independently associated with increased pain severity (risk ratio 1.52, 95% c.i. 1.31 to 1.76; P < 0.001) and re-presentation to healthcare providers owing to side-effects of medication (OR 2.38, 95% c.i. 1.36 to 4.17; P = 0.004), but not with satisfaction with analgesia (beta coefficient 0.92, 95% c.i. -1.52 to 3.36; P = 0.468) compared with opioid-free analgesia. Although opioid prescribing varied greatly between high-income and low- and middle-income countries, patient-reported outcomes did not.Conclusion: Opioid analgesia prescription on surgical discharge is associated with a higher risk of re-presentation owing to side-effects of medication and increased patient-reported pain, but not with changes in patient-reported satisfaction. Opioid-free discharge analgesia should be adopted routinely

Synthesis, structure activity relationships and biological activity evaluation of novel spirocyclic thiazolidin-4-ones as potential anti-breast cancer and epidermal growth factor receptor inhibitors

A series of triazaspiro[4.5]dec-8-ene benzylidine derivatives containing thiazolidinone ring system (6-18) have been designed, synthesized and their biological activities evaluated as potential epidermal growth factor receptor inhibitors. Among them, 9-amino-2-(4-nitrobenzylidene)-3-oxo-4-phenyl-7-thioxo- 1-thia-4,6,8-triazaspiro[4.5]dec-8-ene-10-carbonitrile (18) displayed the most potent inhibitory activity (IC50=6.355 μM). Antiproliferative assay results indicated that compound 18 exhibited moderate antiproliferative activity against MCF-7 cell line in vitro; with GI50 value of 30.6 μM. In addition, compounds 7 and 15 displayed the highest antiproliferative activity at a common GI50 value of 10.8 μM. Docking simulation was performed to determine the probable binding model and to pursuit information regarding the activity of compound 18. Based on the preliminary results, compound 18 could be used as an attractive building block for designing potential epidermal growth factor receptor inhibitors. © Georg Thieme Verlag KG Stuttgart New York

Crystal structure of 2-cyano-N′-(cyclohexylidene)acetohydrazide

In the title compound, C9H13N3O, the cyclohexylidene ring adopts a chair conformation and the bond-angle sum at the C atom linked to the N atom is 359.6°. The cyanoacetohydrazide grouping is close to planar (r.m.s. deviation for the non-H atoms = 0.031 Å) and subtends a dihedral angle of 64.08 (4)° with the four C atoms forming the seat of the chair. The C=O and N—H groups are in a syn conformation (O—C—N—H = −5°). In the crystal, inversion dimers linked by pairs of N—H...O hydrogen bonds generate R22(8) loops; this dimer linkage is reinforced by a pair of C—H...O interactions, which generate R22(14) loops. The dimers are linked by C—H...Nc (c = cyanide) interactions into [100] ladders, which feature C(4) chains and R44(20) loops