d-Isochondordendrine isolated from Cyclea barbate Miers, 400-800 rng/kg ig inhibited the increased vascular permeability induced by ip 0.7% acetic acid in mice or histamine ic 0.05ug/0.05ml in rats. It markedly inhibited the swelling of mouse ear induced by xylene and the edema produced by injection of 1 % carrageenin , fresh egg white or 2.5% formaldehyde 0.lml beneath the plantar surface of hind paw in intact or adrenalectomized rats. It was effective in the cotton-pellet grahuloma inhibition test in rats after daily medica- tion for 6 d. d-lsochondrodendrine could significantly rnduce the leukocyte removal caused by 1 % carrageenin and the fever induced by sc 7% yeast suspension 3 ml/kg in rats

A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria. Compound 33a (IMBZ18G) is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant (MDR) Gram-negative strains, with a highly druglike nature. The checkerboard assay reveals its significant synergistic effect with β-lactamase inhibitor avibactam, and the MIC values against MDR enterobacteria were reduced up to 4-512 folds. X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and C β-lactamases. Accordingly, preclinical studies of 33a alone and 33a‒avibactam combination as potential innovative candidates are actively going on, in the treatment of β-lactamase-producing MDR Gram-negative bacterial infections.