2-(1-[(4-Chloro/methylphenylsulfonylamino)alkyl]-5-thioxo-4,5-dihydro-1,3,4-oxadiazoles (4a-e) were synthesized, in four steps, via the sulfonyl derivatives of l-amino acids (l-alanine, l-methionine and l-phenylalanine) 1a-e, the esters 2a-e, the hydrazides 3a-e and finally the cyclization to 4a-e. Alkylation of 4a-e with 1.0 mole eq. of substituted benzyl halides furnished S-benzyl derivatives 5a-t, while 1.1 mole eq. yielded major 5a-t and minor amount of 6a-d. Alternatively, treatment of 4a-e with 2.0 mole eq. of substituted benzyl halides furnished 6a-d only. The structures of 5b and 5l were further confirmed by single crystal X-ray analysis. Compounds 5a-t and 6a-d showed no selective inhibition against HIV-1 and HIV-2 replication in MT-4 cells. However, 5f and 5j-5q exhibited some inhibitory activity against both types with EC(50) values (>11.50 - >13.00 µg/mL). These results suggest that the structural modifications of these compounds might lead to the development of new antiviral agents. The quantum structure-activity relationship of these novel structural congeners is discussed.
The enantiomerically pure title compound, C11H15NO4S, contains a pyramidal N atom with an S—N bond length of 1.6262 (8) Å. In the crystal, molecules are linked to form chains parallel to the a axis by the hydrogen bond from NH to the carbonyl oxygen. C—H⋯O interactions are also present.
The title compound, C18H18ClN3O3S2, adopts by folding the form of a distorted disc. Interplanar angles are 29.51 (7) and 63.43 (7)° from the five-membered ring to the aromatic systems and 34.80 (6)° between these two latter rings. The absolute configuration was confirmed by determination of the Flack parameter. In the crystal, the molecules are linked by four hydrogen bonds, one classical (N—H⋯N) and three ‘weak’ (C—H⋯O), forming layers parallel to the ac plane; these are in turn linked in the third dimension by Cl⋯N [3.1689 (16) Å] and Cl⋯O [3.3148 (13) Å] contacts to the heterocyclic ring.
Background De Garengeot's hernia (DGH) is a Femoral Hernia that contains an appendix and has been named after Rene De Garengeot, a French surgeon in 1731. It is a rare entity that is mostly identified as an incidental finding during exploration of an incarcerated Femoral Hernia and even rarer is the incidence of a gangrenous appendix in these cases. Case An 81 years-old female patient presented to Accident & Emergency complaining of a progressively tender enlarging mass in the right groin region, associated with local inflammation. CT scan of abdomen and pelvis (CTAP) performed showed suspected perforated caecum with large groin abscess. She underwent groin exploration which confirmed femoral hernia sac containing a gangrenous appendix with a surrounding abscess. The abscess cavity extended from the right groin to medial aspect of thigh. Appendectomy was performed, abscess cavity drained and washed with normal saline/ Betadine followed by suture repair of the femoral hernia defect . She made an uneventful recovery following the surgery. Discussion DGH itself is rare surgical pathology with an incidence of about 0.18% to 0.13%, however, the presentation like our case is even rarer. Emergency surgery is the definitive treatment of DGH to avoid any complications. During surgery, appendectomy and femoral hernia repair are performed consecutively. In conclusion, appendicitis within a femoral hernia often lacks a classical presentation. CTAP can be helpful in diagnosis, however there can be limitations. Appendectomy with mesh-free hernia repair is an acceptable treatment for DGH. Keywords De Garengeot hernia, Incarcerated femoral hernia
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