In our previous papers1»2), we described the structure-activity relationships of 6-(heterocyclyl)methylene penam sulfones (1) as a new class of /3-lactamase inhibitors and proposed a mechanism of enzyme inactivation for series 1. In continuation of these studies with series 1, we pursued the closely related structures in series 2, since they should follow a similar mechanistic pathway and shoul...

Eight N-(4-hydroxycarbamoylbenzyl)-1,2,4,9-tetrahydro-3-thia-9-azafluorenes were efficiently prepared as sulfur analogues of Tubastatin A and thus evaluated as new HDAC6 inhibitors. All compounds exhibited potency against HDAC6, and four of them were active in the nanomolar range (IC(50) = 1.9-22 nM). Further analysis revealed that the sulfone derivatives (designated as Tubathians) are superior...

An abstract should be given he current assignments of the 11.3-μm feature are dicussed. An unbiased survey of correlation charts suggests that the olefinic group R2C=CH2 is a good alternative candidate. For the 12.7-μm feature, the best fits are provided by nitrites, R-O-N=O, and amines, R-N=H2. Sulfones, SO2, exhibit strong features near 7.7 and 8.6 μm, which may contribute to the UIBs. These ...

F. Vinyl Sulfones and Other Michael Acceptors 4683 G. Azodicarboxamides 4695 IV. Acylating Agents 4695 A. Aza-peptides 4695 B. Carbamates 4699 C. Peptidyl Acyl Hydroxamates 4700 D. â-Lactams and Related Inhibitors 4704 E. Heterocyclic Inhibitors 4714 1. Isocoumarins 4715 2. Benzoxazinones 4722 3. Saccharins 4725 4. Miscellaneous Heterocyclic Inhibitors 4728 V. Phosphonylation Agents 4728 A. Pep...

A convenient microwave irradiation protocol was utilized for the synthesis of b-ketosulfones 1-5 in good yields. These sulfones reacted with alkenes through a radical oxidative cyclization mediated by Mn(OAc)3. Dihydrofurans 6-10 were obtained in moderate to good yields starting from 1,1-disubstituted alkenes. Dihydrofurans 11-15 were synthesized in moderate yields and unexpected cyclopropanes ...

The cyclo-addition reaction of diazomethane with a,/3-unsaturated sulfones is described. Divinyl sulfone and phenyl vinyl sulfone give 1or 2-pyrazolines depending on the reaction conditions. cisand /rans-l,2-Bis(methylsulfonyl)ethene form pyrazolines, which on reaction with either triethylamine or excess of diazomethane lead to substituted pyrazoles. The addition of diazomethane to doüble bonds...

The cyclo-addition reaction of diazomethane with a,/3-unsaturated sulfones is described. Divinyl sulfone and phenyl vinyl sulfone give 1or 2-pyrazolines depending on the reaction conditions. cisand /rans-l,2-Bis(methylsulfonyl)ethene form pyrazolines, which on reaction with either triethylamine or excess of diazomethane lead to substituted pyrazoles. The addition of diazomethane to doüble bonds...

In the sterically hindered title compound, C26H17ClN2O6S, the carbazole ring has a maximum deviation from planarity of 0.067 (4) Å for the C atom connected to the aldehyde group. The carbazole moiety forms a dihedral angle of 72.8 (1)° with the nitro-substituted benzene ring. The O atom of the meth-oxy group deviates by 0.186 (1) Å from the adjacent carbazole moiety. The phenyl-sulfonyl group f...

In the sulfone mol-ecule of the title compound, C(12)H(12)N(2)O(2)S·C(2)H(3)N, the two benzene rings are oriented at a dihedral angle of 80.69 (3)°. Weak intra-molecular C-H⋯O hydrogen bonds result in the formation of two five-membered rings, which both have envelope conformations. In the crystal structure, inter-molecular N-H⋯O hydrogen bonds link the mol-ecules.

The introduction of the complex sulfone derivatives marked a considerable advance in the treatment of leprosy, but it also meant a period of some confusion while the various kinds of derivatives were on trial. The period of trial has, in the main, ended by the acceptance of the majority of the parent substance, DDS, as the drug of choice. It is noted, however, that at the BELRA conference on su...