Abstract
A series of 2-thio- and 2-seleno-acetamides bearing the benzenesulfonamide moiety were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against different pathogenic bacteria such as the Vibrio cholerae (VchCA-α and VchCA-β), Burkholderia pseudomallei (BpsCA-β and BpsCA-γ), Mycobacterium tuberculosis (Rv3723-β) and the Salmonella enterica serovar Typhimurium (StCA2-β). The molecules represent interesting leads worth developing as innovative antibacterial agents since they possess new mechanism of action and isoform selectivity preferentially against the bacterial expressed CAs. The identification of potent and selective inhibitors of bacterial CAs may lead to tools also useful for deciphering the physiological role(s) of such proteins.
Highlights
A series of 2-thio- and 2-seleno-acetamides bearing the benzenesulfonamide moiety were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against different pathogenic bacteria such as the Vibrio cholerae (VchCA-α and VchCA-β), Burkholderia pseudomallei (BpsCA-β and BpsCA-γ), Mycobacterium tuberculosis (Rv3723-β) and the Salmonella enterica serovar Typhimurium (StCA2-β)
Infectious diseases caused by human pathogens namely bacteria, fungi and virus are among the major challenges for humankind
Chemistry We focused our attention onto the study of substituted 2-thio- and 2-seleno-acetamides bearing the benzeWneesfuolcfuosneadmouidreatmteontiieotny.oWnteo sthoeusgthudt ytooef msupblsotiytu2te-cdh2l-otrhoioa-caentadm2-isdeelesn2oa-–acce,toabmtiadiensebdeaarcicnogrding to prtehveiboeunszleyneresuplofornteadmipdreomceodieutyre
Summary
Infectious diseases caused by human pathogens namely bacteria, fungi and virus are among the major challenges for humankind. A large number of bacteria, in recent years, showed increasing resistance to the more common antibiotics clinically used [1,2,3]. Despite the progresses in fundamental knowledge on various pathogens, the current chemotherapy still is unsatisfactory due to limited efficacy, long-term treatment, drug resistance and undesired side effects. There is an urgent need for the development of new and efficient drugs against human affecting pathogens. B20t2a0i,n21i,nxgFOaRnPtiE-EiRnfReEcVtIiEvWe agents with a new mechanism of action when com2poaf r8ed to classical antibiotics [7]. These essential enzymes are a superfamily of metalloenzymes which catalyze the reavneerwsibalpephryoadcrhatfioornoobftaCinOin2ginanHti2-iCnfOec3t[iv8e].aTgoendtastwe,itshevaennewgemnetcihcaanlliysmdiosftiancctitofnamwihleienscwomerpearrepdorted and wtoercelanssaimcaeldanatsibαio- t(ipcsre[s7e]n. Tanodda-tpe,osseivtievnegBenaecttiecrailaly, dmisotinnoctafnamdidlieicsowtyerleedons plantrse,pfuorntegdi aanndd Awrecrhe aneaam),eγd-a(sBαac- t(eprrieas,ecnytainnovbeartcetberraiateas,npdroAtorczhoaae, aa)lg, aδe-,, ζcy-,toθp-l(aisnmmoafrginreeendipaltaonmtss,) and η- CAadnsicd(optiyrnolemtdoaoznnoysagpbrleaalnmotn-sn,gefigunangtgitvioeatnBhdaectAPelrraicash)ma, eoβad-)i,(uiγnm-bs(opBtpah)ctg[e9rra–ima1,2-cn].yeagnaotibvaectaenrdia-panodsitiAvrechBaaecate),riδa,-,mζo-,nθo-a(nidn
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