"The project aims to design compounds with antimycobacterial activity. It is based on the idea that the specific molecular fragments (pharmacophores) bear biological activity. Recently we have found that an alkylsulfanyl group bound to the heterocycles nucleus is one of the pharmacophores of antimycobacterial activity. A number of derivatives of pyridine, benzimidazole, benzothiazole, and benzoxazole, which we have recently prepared, show significant antimycobacterial activity in vitro evaluation. Regarding the spectrum of the antimycobacterial activity, the substances exhibited efficacy both against M. tuberculosis and on mycobacteria other than M. tuberculosis (MOTT). The proposed project aims to model the structure of compounds bearing the alkylsulfanyl moiety. In the synthetic part of the project, a large number of alkylsulfanyl derivatives of various heterocycles will be prepared, in which the benzyl moiety of the molecule will be modified. The physico-chemical and quantum-chemical"@en . "16"^^ . . "16"^^ . . . . . "http://www.isvav.cz/projectDetail.do?rowId=GA203/02/0082"^^ . . . . "Development of new antimycobacterial agents with low toxicity"@en . . . "1"^^ . "Neuvedeno."@en . . "The project was concerned with the development of new antituberculotics from the group of alkylsulfanyl derivatives of nitrogen heterocycles. The compounds with significant activity and wide spectrum of antimycobacterial activity were prepared. The compo"@en . "1"^^ . "Projekt byl zam\u011B\u0159en na v\u00FDvoj nov\u00FDch antituberkulotik ze skupiny alkylsulfanyl deriv\u00E1t\u016F dus\u00EDkat\u00FDch heterocykl\u016F. Poda\u0159ilo se p\u0159ipravit slou\u010Deniny se signifikantn\u00ED aktivitou a \u0161irok\u00FDm spektrem antimykobakteri\u00E1ln\u00ED aktivity. L\u00E1tky jsou \u00FA\u010Dinn\u00E9 jak proti M. tub"@cs . . . "V\u00FDvoj nov\u00FDch antimykobakteri\u00E1ln\u00EDch l\u00E1tek s n\u00EDzkou akutn\u00ED toxicitou" . . . "0"^^ . . "2008-06-02+02:00"^^ . . "Projekt je zam\u011B\u0159en na v\u00FDvoj l\u00E1tek s antimykobakteri\u00E1ln\u00ED aktivitou. Za biologickou aktivitu l\u00E1tky je zodpov\u011Bdn\u00FD specifick\u00FD molekulov\u00FD fragment (farmakofor). Z na\u0161ich posledn\u00EDch studi\u00ED vyplynulo, \u017Ee jedn\u00EDm z farmakofor\u016F antimykobakteri\u00E1ln\u00ED aktivity je alkylsulfanyl skupina v\u00E1zan\u00E1 na heterocyklick\u00E9 j\u00E1dro. \u0158ada alkylsulfanyl deriv\u00E1t\u016F pyridinu, benzimidazolu, benzothiazolu, benzoxazolu, p\u0159ipraven\u00FDch n\u00E1mi v ned\u00E1vn\u00E9 dob\u011B, vykazuje signifikantn\u00ED antimykobakteri\u00E1ln\u00ED aktivitu p\u0159i hodnocen\u00ED in vitro. Z hlediska spektra antimykobakteri\u00E1ln\u00EDho \u00FA\u010Dinku l\u00E1tky vykazuj\u00ED \u00FA\u010Dinnost na kmen M. tuberculosis i na podm\u00EDn\u011Bn\u00E9 patogenn\u00EDmi (PPM) kmeny mykobakteri\u00ED. C\u00EDlem navrhovan\u00E9ho projektu je modelov\u00E1n\u00ED struktury slou\u010Denin s alkylsulfanylov\u00FDm \u0159et\u011Bzcem v molekule. V syntetick\u00E9 \u010D\u00E1sti projektu bude p\u0159ipraveno velk\u00E9 mno\u017Estv\u00ED alkylsulfanyl deriv\u00E1t\u016F r\u016Fzn\u00FDch heterocykl\u016F, u kter\u00FDch bude modif\u00EDkov\u00E1na benzylov\u00E1 \u010D\u00E1st molekuly. Budou studov\u00E1ny jejich fyzik\u00E1ln\u011B-chemick\u00E9 a kvantov\u011B-chemick\u00E9 parametry teoretick\u00FDmi i" . . "GA203/02/0082" . .