- 2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: Synthesis, carbonic anhydrase inhibition and evaluation in the rabbit
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Novel non-chiral 2H-thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6- sulfonamide 1,1-dioxides were synthesized for evaluation as potential candidates for the treatment of glaucoma. All of the compounds prepared were potent high affinity inhibitors of human carbonic anhydrase II, K(i) 50 values ranging from 4.25 to 73.6 nM. Of the compounds evaluated for their ability to lower intraocular pressure in naturally hypertensive Dutch-belted rabbits, 5a, 17a3, 17b1, 17b2, 17h2 and 17i1 showed significant efficacy (> 20% decrease) in this model following topical ocular administration. (C) 2000 Elsevier Science Ltd.
- Chen, Hwang-Hsing,Gross, Sharon,Liao, John,McLaughlin, Marsha,Dean, Tom,Sly, William S.,May, Jesse A.
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p. 957 - 975
(2007/10/03)
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- A convenient synthesis of the novel 5H-thieno[2,3-e]-4,1,2- oxathiazepine ring system via an alkoxycarbenium ion intermediate
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3-(Methoxymethoxymethyl)-2-thiophenesulfonamides and 3-hydroxymethyl-N- methoxymethyl-2-thiophenesulfonamides have been shown to undergo cyclization when treated under anhydrous acidic conditions to provide the novel 2,3- dihydro-5H-thieno[2,3-e]-4,1,2-oxathiazepine ring system. Incorporation of a primary sulfonamide group into position seven of the molecule provided compounds which inhibit human carbonic anhydrase II.
- Dantanarayana, Anura P.,DuPre, Brian,May, Jesse A.,Lynch, Vincent M.
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- Herbicidal acetals and ketals
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Novel furan- and thiophenesulfonamides such as 3-(1,3-dioxolan-2-yl)-N-[(4-methoxy-6-methyl-1,3-5-triazin-2-yl)aminocarbonyl]-2-thiophenesulfonamide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-(1,3-dioxolan-2-yl)-2-thiophenesulfonamide are highly active pre-emergent and/or post-emergent herbicides.
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