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Sulfonamide Derivatives (sulfonamide + derivative)

Distribution by Scientific Domains
Medical Sciences50%
Chemistry50%

Selected Abstracts

Novel Sulfonamide Derivatives as Inhibitors of Histone Deacetylase

HELVETICA CHIMICA ACTA, Issue 7 2005

Inhibition of the enzyme histone deacetylase (HDAC) is emerging as a novel approach to the treatment of cancer. A series of novel sulfonamide derivatives were synthesized and evaluated for their ability to inhibit human HDAC. Compounds were identified which are potent enzyme inhibitors, with IC50 values in the low nanomolar range against enzyme obtained from HeLa cell extracts, and with antiproliferative effects in cell culture. Extensive characterization of the structure,activity relationships of this series identified key requirements for activity. These include the direction of the sulfonamide bond and substitution patterns on the central phenyl ring. The alkyl spacer between the aromatic head group and the sulfonamide functionality also influenced the HDAC inhibitory activity. One of these compounds, m11.1, also designated PXD101, has entered clinical trials for solid tumors and haematological malignancies. [source]

Celecoxib-induced photoallergic drug eruption

INTERNATIONAL JOURNAL OF DERMATOLOGY, Issue 6 2004
Ayca Cordan Yazici MD
Photoallergic dermatitis is caused by a photosensitizing substance plus sunlight exposure in a sensitized person. If the photosensitizer is delivered internally, it is called a photoallergic drug reaction. Celecoxib is a new generation non-steroidal anti-inflammatory drug and sulfonamide derivative. We report a photoallergic drug eruption associated with the introduction of celecoxib. To our knowledge, this is the first report of photoallergic drug reaction associated with celecoxib. [source]

Cross-reactivity among p -amino group compounds in sulfonamide fixed drug eruption: diagnostic value of patch testing

CONTACT DERMATITIS, Issue 2 2004
P. Tornero
We studied 28 patients with fixed drug eruption (FDE) caused by sulfonamide antibiotics to investigate cross-reactivity between sulfonamide derivatives and p -amino compounds and to explore the usefulness of patch testing, as an alternative to controlled oral challenge testing (COCT), in diagnosis within this clinical area. COCT with sulfamethoxazole (SMX), sulfadiazine (SDZ), sulfamethizole (SMZ), furosemide (FU), procaine (PRO) and glipizide (GPZ) was performed. Patch testing (PT) with SMX and SDZ was carried out. In all patients, the diagnosis of FDE was confirmed by positive COCT and allergy to trimethoprim ruled out by COCT. 42.8 and 31.8% of the SMX-induced FDE patients reacted to SMZ and SDZ, respectively. All patients (n = 28) tolerated FU, PRO and GPZ. COCT performed with the 3 sulfonamide antibiotics in 12 patients was positive in 2 subjects with the 3 drugs, in 2 patients only with SMX and SMZ and in the remaining 8, SMX was the only causative drug. PT was positive in 5 of 25 patients positive on COCT. The probability of obtaining a positive PT was higher among patients who had a residual lesion than that among those who lacked this. Cross-reactivity between different sulfonamide antibiotics is thus variable, being most likely between SMX and SMZ. We have found no cross-reactivity between sulfonamide antibiotics and other sulfonamide derivatives or p -amino drugs in FDE. PT is a useful tool in the diagnosis of FDE, especially if there are residual lesions, because it avoided the need for COCT in 20% of patients. [source]

Novel Sulfonamide Derivatives as Inhibitors of Histone Deacetylase

HELVETICA CHIMICA ACTA, Issue 7 2005

Inhibition of the enzyme histone deacetylase (HDAC) is emerging as a novel approach to the treatment of cancer. A series of novel sulfonamide derivatives were synthesized and evaluated for their ability to inhibit human HDAC. Compounds were identified which are potent enzyme inhibitors, with IC50 values in the low nanomolar range against enzyme obtained from HeLa cell extracts, and with antiproliferative effects in cell culture. Extensive characterization of the structure,activity relationships of this series identified key requirements for activity. These include the direction of the sulfonamide bond and substitution patterns on the central phenyl ring. The alkyl spacer between the aromatic head group and the sulfonamide functionality also influenced the HDAC inhibitory activity. One of these compounds, m11.1, also designated PXD101, has entered clinical trials for solid tumors and haematological malignancies. [source]

Novel derivatives of the benzo[b][1,6]naphthyridine system

JOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 2 2006
Leslie W. Deady
An efficient synthesis of 2-hydroxy-6-methylbenzo[b][1,6]naphthyridin-1(2H)-one was devised. The hydroxy group was alkylated, acylated and replaced by hydrogen. Electrophilic nitration, bromination and chlorosulfonation occurred readily in the 4-position. From the last, various sulfonamide derivatives were prepared. A selection of the products was screened by the National Cancer Institute. Cytotoxicities were generally low. [source]