A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s was written by Subasinghe, Nalin L.;Travins, Jeremy M.;Ali, Farah;Huang, Hui;Ballentine, Shelley K.;Marugan, Juan Jose;Khalil, Ehab;Hufnagel, Heather R.;Bone, Roger F.;DesJarlais, Renee L.;Crysler, Carl S.;Ninan, Nisha;Cummings, Maxwell D.;Molloy, Christopher J.;Tomczuk, Bruce E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Safety of 2-(Chloromethyl)-1,3-difluorobenzene This article mentions the following:
Inhibiting the classical pathway of complement activation by attenuating the proteolytic activity of the serine protease C1s is a potential strategy for the therapeutic intervention in disease states such as hereditary angioedema, ischemia-reperfusion injury, and acute transplant rejection. A series of (arylsulfonyl)-2-thiophene carboxamidine inhibitors of C1s were synthesized and evaluated for C1s inhibitory activity. A potent compound, 4-[[7-bromo-1-[(2,5-difluorophenyl)methyl]-1H-benzimidazol-5-yl]sulfonyl]-5-(methylthio)-2-thiophene-carboximidamide, had a Ki of 10 nM and >1000-fold selectivity over uPA, tPA, FXa, thrombin, and plasmin. In the experiment, the researchers used many compounds, for example, 2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4Safety of 2-(Chloromethyl)-1,3-difluorobenzene).
2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Safety of 2-(Chloromethyl)-1,3-difluorobenzene
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics