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Biomedical subjects

M Seth

Publications and source records attributed to M Seth.

26 records · Page 2Linked to original sources

Molecular interaction of nonsteroidal compounds with uterine progesterone receptor (Part I).

Progesterone-receptor binding affinity of some nonsteroidal molecules was assessed by competitive protein binding assay in rabbit as well as human uterine cytosol in vitro. Of 40 compounds belonging to 5 different series tested, 3-(p-anisoyl)-2-chloro-6, 7-dimethoxy-quinoline exhibited around 50% inhibition whereas 2-(p-anisoyl) naphthalene and 3-substituted phenyl-1-(3-(2-chloro-6, 7-dialkoxy) quinolinyl)prop-2-en-1-one showed around 20% inhibition in 3H-progesterone binding for rabbit and human uterine progesterone receptor.

Animals↗

Syntheses and anthelmintic activity of alkyl 5(6)-(substituted-carbamoyl)- and 5(6)-(disubstituted-carbamoyl)benzimidazole-2-carbamates and related compounds.

A number of alkyl 5(6)-(substituted-carbamoyl)- and 5(6)-(disubstituted-carbamoyl)benzimidazole-2-carbamates and related compounds have been synthesized, and their anthelmintic activity against various intestinal helminths of experimental animals have been evaluated. A large percentage of the compounds synthesized showed noteworthy activity against Ancylostoma ceylanicum and at higher doses against Hymenolepsis nana infections. Compared to the alkyl 5(6)-(substituted-carbamoyl)benzimidazole-2-carbamates, the disubstituted carbamoyl analogues were found to exhibit better anthelmintic activity. The most active compound of the series, namely, methyl 5(6)-[(N-2-pyridylpiperazino)carbamoyl]benzimidazole-2-carbamate (90), has been screened against intestinal helminths in higher animals and as a micro- and macrofilaricidal agent. Compound 90 has been identified as a broad-spectrum anthelmintic agent. Compound 90 has been identified as a broad-spectrum anthelmintic in view of its efficacy against A. ceylanicum (hamsters and dogs), H. nana (rats), Nippostrongylus brasiliensis (rats), Syphacia obvelata (mice), A. tubaeformis (cat), Toxocara spp. (cat), and Litomosoides carinii (cotton rat).

Ancylostomiasis↗

Specific interaction of some non-steroidal compounds with the progesterone binding site of uteroglobin.

Uteroglobin binds progesterone with high affinity. A few substituted diphenyl ketones were observed to inhibit uteroglobin-progesterone binding in a dose-dependent manner. 4,4'-Dimethoxy-2-hydroxy benzophenone had relatively higher affinity for uteroglobin. The structure-activity relationship amongst the substituted diphenyl ketones indicated considerable sensitivity towards minor structural modifications. These observations offer a tool to investigate nonsteroidal compounds in relation to progesterone related functions of uteroglobin in pregnancy.

Animals↗

Fertility impairment in females--present status.

Various approaches towards the control of fertility in females have been discussed. The salient observations made in the field of reproductive physiology which may generate new leads for the development of agents capable of inhibiting pregnancy, are described. The discussion concerning the oestrogen and progesterone receptors is directed towards designing new antifertility agents. The different areas of fertility control covered in this survey are of importance for basic and applied research.

Cervix Mucus↗

Chemotherapy of filariasis--on the search of new agents effective on the reproductive system of female adult worms.

The design and synthesis of a series of alkyl 5(6)-substituted benzimidazole-2-carbamates (1-13), 7-chloro-4-(4-substituted phenyl)aminoquinolines (14-16), 1,2-dimethyl-3-methoxy-carbonyl-4,5-disubstituted pyrroles (17-19) and some compounds belonging to the class pimelonitrile (20), dihydroquinoline (21), pyridine (22), pyridoquinoline (23) and tetrahydro-pyrimidine (24) have been carried out as possible antifilarial agents. All these compounds have been evaluated for their activity against male and female adult worms of Litomosoides carinii in cotton rats. The effect of these compounds was also observed on the reproductive system (condition of developing microfilariae and their release from uterus) of adult female worms. In this study, three types of compounds were discovered: (a) those which showed activity on both the male and female adult worms and also had sterilizing effects on surviving adult females (1-3, 6-9, 13, 19), (b) those which only sterilized the adult females (14-16, 21, 24), and (c) those which had no effect on female reproduction but killed only adult worms (4, 5, 11, 12, 17, 18, 20, 22, 23). This tends to open up a new avenue in the chemotherapy of filariasis and the future scope of work on chemosterilization of adult females has been discussed.

Animals↗