31 results about "Antituberculars" patented technology

A steroidal compound n-hexyl-p-stigmasteryloxy-benzoate is reported as a novel potent antitubercular drug.

The invention discloses an isoniazid thiadiazine thione derivative, which solves the problem that the existing derivative has poor lipid solubility of active ingredient, and can not dissolve in water or can not highly disperse. The structure of the derivative can be presented by INH-THTT-R-THTT-INH, wherein ING represents the structure of isoniazid of antitubercular drug, THTT is a ring structure, and R is linear chain, non-linear chain or annular alkyl compound containing two primary amines (including alkyl structures of different substituent groups). The derivative can be prepared into highly-dispersed drug delivery system, including the dosage form of liposome, solid lipid nanospheres, niosomes, micro emulsion and the like. The derivative can not only improve the lipid solubility of isoniazid, but also hydrolyze and release isoniazid active compound in vivo, increases the penetrability of isoniazid cell, reduces the tolerance of isoniazid during therapy and improves the curative effect.

Invention provides antitubercular compounds selected from propargylated 1,2,3 triazoles of Formula I, wherein, X is sulfur(S) or a sulphone (A), n, m represent independently an integer O or 1, with the provision that when ‘n’ is 1, ‘m’ is 1; R1 is hydrogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group; halogen; or aryl group optionally substituted with —OCH3, halogen, and nitro; R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is C1-C6 alkyl optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl allyl or propargyl groups consisting of 1 to 6 carbon atoms; with the provision that when ‘m’ is 1, and ‘n’ is zero; R1 is selected from the group consisting of hydrogen, halogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group or aryl group optionally substituted with —OCH3, halogen, and nitro, R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is selected from the group consisting of halogen, C1-C6 linear or branched alkyl group optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, wherein the heterocyclic ring may further be substituted with halogen, alkyl, arylalkyl.