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Biomedical subjects

K S Jain

Publications and source records attributed to K S Jain.

9 recordsLinked to original sources

Uncommon high-risk lesions of the breast diagnosed at stereotactic core-needle biopsy: clinical importance.

PURPOSE: To assess the outcome of papillary lesions, radial scars, or lobular carcinoma in situ (LCIS) diagnosed at stereotactic core-needle biopsy (SCNB). MATERIALS AND METHODS: Retrospective review of 1,236 lesions sampled with SCNB yielded 22 papillary lesions, nine radial scars, and five LCIS lesions. Diffuse lesions such as papillomatosis, papillary ductal hyperplasia, papillary ductal carcinoma in situ (DCIS), and atypical lobular hyperplasia were not included. The mammographic findings, associated histologic features, and outcome were assessed for each case. RESULTS: Sixteen papillary lesions were diagnosed as benign at SCNB. Of these, five were benign at excision, and 10 were unremarkable at mammographic follow-up. At excision of an unusual lesion containing a microscopic papillary lesion, DCIS was found. Three of four papillary lesions suspicious at SCNB proved to be papillary carcinomas; the fourth had no residual carcinoma at excision. Eight of nine radial scars were excised, which revealed atypical hyperplasia in four scars but no malignancies. One LCIS lesion was found at excision to contain DCIS. CONCLUSION: Benign or malignant papillary lesions were accurately diagnosed with SCNB in the majority of cases. Cases diagnosed as suspicious for malignancy or with atypia or unusual associated histologic findings should be excised. No malignancies were found at excision of radial scars diagnosed at SCNB. Surgical removal of these lesions following SCNB may not be routinely necessary. DCIS was found in one lesion diagnosed as LCIS at SCNB, which suggests that removal of these lesions may be prudent.

Adult↗

Synthesis and QSAR of some 3-amino-2-(substituted)aminomethyl-5,6-disubstituted thieno[2,3-d]pyrimidin-4(3H)-ones as novel H1-receptor antagonists.

The present study describes the synthesis and quantitative structure activity relationships (QSAR) of novel 3-amino-2-(substituted)aminomethyl-5,6-disubstitutedthieno[2,3-d] pyrimidin-4(3H)-ones for their potent H1-receptor antagonist activity on the guinea pig ileum. With the IC50 values in the range of 10(-5) gms/lit, all the compounds tested were found to possess ten fold higher affinity to the H1-receptor than diphenhydramine and cetirizine, but lower than astemizole and loratidine. The sedative potential of these compounds was found to be lower than cetirizine and astemizole but comparable to loratidine. The QSAR study indicates a parabolic relationship of the biological activity mainly with the steric parameters and partly with the lipophilic parameters.

Animals↗

Mechanism of the antihyperlipaemic activity and pharmacokinetics of 2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidin-4(3H)-o ne.

The pharmacokinetics and the mechanism of action of the antihyperlipaemic compound 2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidin-4(3H)-on e (CAS 89587-03-3, LM-1554) have been studied. Serum concentrations were determined by reverse phase HPLC using methanol : water (60 : 40) as the solvent system. The results of pharmacokinetic studies suggest that the compound LM-1554 is poorly absorbed from the gastrointestinal tract after the oral administration in dogs and rabbits. The volume of distribution (Vd) was found to be low. The poor bioavailability (3-4%) and low volume of distribution of the compound LM-1554 suggest the gastrointestinal tract as the site of action for the antihyperlipaemic activity. This hypothesis is substantiated by the observations that the compound was found active in rabbits only when administered orally and found inactive by the parenteral route. Further, the cholesterol levels were found to increase in blood samples collected from the portal vein after oral administration of cholesterol in coconut oil to rats. This increase was found to be prevented by the compound LM-1554. In conclusion, the compound LM-1554 has a potential to be developed as an antihyperlipaemic agent. The mechanism of action of the compound LM-1554 appears to consist in the inhibition of cholesterol absorption in the gastrointestinal tract.

Administration, Oral↗

Synthesis and quantitative structure-activity relationships of antihyperlipaemic 2-substituted thieno[3,2-d]pyrimidin-4(3H)-ones.

The synthesis, antihyperlipaemic evaluation and quantitative structure-activity relationships (QSAR) of two series of thieno[3,2-d]pyrimidin-4-one derivatives are reported. While most of the compounds in these series were found to exhibit antihyperlipaemic activity, the QSAR study of these two series indicated a positive influence of only the electronic nature of the 2-substitutents on the biological activity. The lipophilic and the steric parameters did not appear to be significant.

Animals↗

Synthesis and pharmacological study of antihyperlipaemic activity of 2-substituted thieno(2,3-d)pyrimidin-4(3H)-ones.

A series of 2-substituted thieno(2,3-d)pyrimidin-4-(3H) ones (1-15) was prepared by the reaction of thiophene ortho-aminoester (IV) with a variety of nitriles (V) under acidic conditions, and screened for antihyperlipaemic activity in various animal models. While most of these compounds were found active, 2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d) pyrimidin-4(3H)-one (5) was found to be the most active of all. The serum triglyceride lowering activity exhibited by 5 was found comparable to that of clofibrate and riboflavin tetrabutyrate. Compound 5 was also found to be safe as indicated by acute and chronic toxicity studies in mice and rats.

Animals↗