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At least 361 records · Page 20Linked to original sources
PubMed2005

Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents.

A new series of antituberculosis agents 6-9 was designed, synthesized and evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv and clinical isolates in an agar dilution method. Compound 9h showed comparable in vitro activity (MIC) to isoniazid against M. tuberculosis H37Rv and clinical isolates (sensitive strains) and superior activity against resistant strains of M. tuberculosis.

Antitubercular Agents↗
PubMed1999

Carbonic anhydrase inhibitors. Water-soluble, topically effective intraocular pressure lowering agents derived from isonicotinic acid and aromatic/heterocyclic sulfonamides: is the tail more important than the ring?

Reaction of twenty aromatic/heterocyclic sulfonamides containing a free amino, imino, hydrazino or hydroxyl group, with isonicotinoyl chloride afforded a series of water-soluble compounds (as hydrochloride or triflate salts). The new derivatives were examined as inhibitors of three carbonic anhydrase (CA) isozymes, CA I, II (cytosolic forms) and IV (membrane-bound form). Efficient inhibition was observed against all three isozymes, but especially against CA II and CA IV (K(I) in the nanomolar range), the two isozymes known to play a critical role in aqueous humor secretion within the ciliary processes of the eye. Some of the most potent inhibitors synthesized were applied as 2% water solutions directly into the eye of normotensive or glaucomatous albino rabbits. Very strong intraocular pressure (IOP) lowering was observed for many of them, and the active drug was detected in eye tissues and fluids. According to others the IOP lowering effect of topically effective antiglaucoma sulfonamides is due to the intrinsic nature of the specific heterocyclic sulfonamide considered, among which the thienothiopyran-2-sulfonamide derivatives represent the best studied case e.g. dorzolamide. In order to prove that the tail (in this case the isonicotinoyl moiety) conferring water solubility to a sulfonamide CA inhibitor is more important than the ring to which the sulfonamido group is grafted a dorzolamide derivative to which the isonicotinoyl moiety was attached was also prepared. This new compound is more water soluble than dorzolamide (as hydrochloride salt), behaves as a strong CA II inhibitor and acts similarly to the parent derivative in lowering IOP in experimental animals. Thus, it seems that the tail conferring water solubility is more important for topical activity as an antiglaucoma drug than the heterocyclic/aromatic ring to which the sulfonamido moiety is attached.

Administration, Topical↗
PubMed2002

Design and structural extension of a supramolecular inclusion-compound host made by the formation of dimers of isonicotinic acid and thiocyanato coordinating bridges.

A new host design for an inclusion compound with a preference for large planar aromatic guest molecules has been proposed. Our host design includes a rectangular cavity made using a long and a short building block based on the concept of supramolecular chemistry. The long building block facilitates the inclusion of large guests, and the short building block prevents the formation of an interpenetrated structure, which is often observed in frameworks with large void spaces. The long building block is made when dimers of 4-pyridinecarboxylic acid (isoH) form through hydrogen bonding between the two carboxylic acid moieties. This isoH dimer can link two transition metal centers using the N atoms at both ends to act as a long building block. For the short building block, the thiocyanato ion was used. This makes a bent bridge between two metal centers to form a 1D double-chain [M(SCN)2]infinity complex. From the self-assembly of isoH, SCN- and Ni2+, a 2D network of [Ni(SCN)2(isoH)2]infinity, in which the 1D [Ni(SCN)2]infinity complexes are linked by the isoH dimers, is built up. The rectangular cavity is formed as a mesh within the 2D network. The crystal of our inclusion compound has a layered structure of 2D networks, and a 1D channel-like cavity penetrating the layered 2D networks is formed where guests may be included. Moreover, our host design has the advantage of easy extension of the host structure. Replacement of isoH with another component and use of three components is possible for making the long building block. In the latter case, a linear spacer having two carboxy groups is inserted into the isoH dimer to form a long building block with a trimer structure. Based on our host design, a series of new inclusion compounds were synthesized. The crystal structures of three compounds were determined by single crystal X-ray diffraction. These were a biphenyl inclusion compound [Ni(SCN)2(isoH)2].1/2C12H10 (the basic case), a 9,10-dichloroanthracene inclusion compound [Ni(SCN)2(acrylH)2].1/2C14H8Cl2, where isoH is replaced with 3-(4-pyridinyl)-2-propenoic acid (acrylH), and a perylene inclusion compound [Ni(SCN)2(isoH)2(fumaricH2)].1/2C20H12, whose long building block is a trimer inserted with fumaric acid (fumaricH2) as a linear spacer.

Journal Article↗