Mp. Singh et al., SYNTHESIS AND IN-VITRO ANTIMICROBIAL ACTIVITY OF 3-HETEROARYLSULPHONYLMETHYL CEPHEMS - A NEW CLASS OF CEPHALOSPORINS, European journal of medicinal chemistry, 30(2), 1995, pp. 157-164
A series of 3-heteroarylsulphonylmethyl and 3-heteroarylsulphenylmethy
l cephems were prepared and tested for antimicrobial activities. In co
ntrast to the adverse effect of oxidized ring sulphur of penams and ce
phems on antimicrobial activities, the oxidized side-chain sulphur of
3-mercaptoheteroaryl cephems retained Gram-negative and slightly decre
ased Gram-positive activity. The chemical nature of the moieties subst
ituted at C-7 and C-3 positions also influenced the antibacterial acti
vity and spectrum. Compounds with thienyl substitution at C-7 and sulp
honylmethylthiazoles or sulphonylmethylthiadiazoles at C-3 exhibited g
ood differentials in antibacterial activity vet-sus their unoxidized c
ounterparts.