Naphthalimido derivatives as antifolate thymidylate synthase inhibitors

A new series of N-(substituted)benzyl-1,8-naphthalimides 4, structurally related to the previously reported thymidylate synthase (TS) inhibitor naphthaleins 3, were synthesized and compounds tested for their inhibition of several species of TS. Moreover, their in vitro cytotoxicity together with antimycotic and antibacterial properties were assayed. While no activity was detected in the antibacterial tests, the m-nitro (4ae) and the p-nitro (4af) derivatives were found able to partially inhibit TS at low micromolar concentrations. Introduction of nitro or (substituted)-amino groups in position 4 of the naphthalic ring always led to less active compounds.     

Determination of subpopulations of T- and B-lymphocytes in human blood using an immunofluorescence method

The immunofluorescent technique for assaying T- and B-lymphocyte subpopulations, using monoclonal (OCT3, OCT4, OCT8) and monospecific antibodies is described. The results of immunocompetent cell determinations in normal subjects and in patients are presented. A conclusion is made that use of universal immunofluorescent method for assays of the lymphocyte subpopulations widens the possibilities of diagnosis of immunodeficiency states.     

The late examination results in children with pylorospasm and dyskinesia of the proximal sections of the small intestine]

The article analyses the late-term results of examination of 46 children with neurogenous dyskinesias of the gastrointestinal tract which were recognised in infancy for the first time. The author believes that the functional, motor-evacuation, and sphincter disorders of the proximal parts of the digestive tube lead to the development of organic noninfectious diseases of the gastroduodenal system.     

Synthesis and antihypoxic activity of 1,2,4-triazoles, 1,3-dithiane-1,1,3,3-tetraoxides,and 1,4-benzothiazin-3(4H)-one

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 26, No. 2, pp. 38–41, February, 1992.